Challenges in trancorneal drug

delivery

Presented by

Bibin Mathew

MPharm IP(2nd Sem)

Introduction

Ocular pharmacokinetics

Pathway of the drug after instillation

Challenges related to routes of administration

Barriers to drug absorption

Conventional ocular drug delivery constraints

Nasolacrimal drainage

Approaches to overcome constraints of conventional dosage form

Novel ocular drug delivery

Marketed formulations

Conclusion

Medication is applied to the surface of the eye for two purposes

diams To treat the surface of eye

diams To provide intraocular treatment

90 ocular market conventional dosage form

5 of applied drug penetrates

Major challenge remains to past the protective ocular

barriers

Good corneal penetration

Prolong contact time with corneal tissue

Simplicity of instillation for the patient

Non irritative and comfortable form

Appropriate rheological properties

Ocular pharmacokinetics

Ocular structure with routes of drug kinetics

Systemic administration

Limited penetration potential systemic

toxicity

Intraocular implants

Increased risk of retinal detachment and

intravitrealhemorrahge

Intravitreal injections

Increased risk of retinal detachment hemorrhage

and catracts

Topical application

Limited penetration (5) rapid tear

washout poor patient compliance

Flow of lacrimal fluid removes instilledcompounds from the surface of eye

Excess volume is flown to thenasolacrimal duct rapidly

Corneal barrier is formed uponmaturation of epithelial cells

Most apical corneal epithelial cells fromtight junctions that limit the paracellulardrug permeation

These barriers have two parts

Blood retina barrier

Blood-aqueous barrier

Volume

Lacrimation

Tear dilution

Blinking

BARRIERS

Drug loss from ocular surface Lacrimal fluid eye barrier

Blood ocular barriers Others

CORNEL AREA

Drug interaction

Drug protein interaction

Instilled dose

Corneal absorption

Normal tear turn overInduced lacrimation

Conjunctival absorption

Consists of a secretory distributive and collection part

Secretory portion composed of the lacrimalgland Tears are spread over the ocular surfaceby the eyelids during blinking

Collecting system consists of the canaliculithe lacrimal sac the nasolacrimal duct whichhas opening in the inferior

The basal tear flow is of about 12 microlmin(range 05ndash22 microlmin) Reflex stimulationmay increase lacrimation a hundred-fold times

Nasolacrimal drainage

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Introduction

Ocular pharmacokinetics

Pathway of the drug after instillation

Challenges related to routes of administration

Barriers to drug absorption

Conventional ocular drug delivery constraints

Nasolacrimal drainage

Approaches to overcome constraints of conventional dosage form

Novel ocular drug delivery

Marketed formulations

Conclusion

Medication is applied to the surface of the eye for two purposes

diams To treat the surface of eye

diams To provide intraocular treatment

90 ocular market conventional dosage form

5 of applied drug penetrates

Major challenge remains to past the protective ocular

barriers

Good corneal penetration

Prolong contact time with corneal tissue

Simplicity of instillation for the patient

Non irritative and comfortable form

Appropriate rheological properties

Ocular pharmacokinetics

Ocular structure with routes of drug kinetics

Systemic administration

Limited penetration potential systemic

toxicity

Intraocular implants

Increased risk of retinal detachment and

intravitrealhemorrahge

Intravitreal injections

Increased risk of retinal detachment hemorrhage

and catracts

Topical application

Limited penetration (5) rapid tear

washout poor patient compliance

Flow of lacrimal fluid removes instilledcompounds from the surface of eye

Excess volume is flown to thenasolacrimal duct rapidly

Corneal barrier is formed uponmaturation of epithelial cells

Most apical corneal epithelial cells fromtight junctions that limit the paracellulardrug permeation

These barriers have two parts

Blood retina barrier

Blood-aqueous barrier

Volume

Lacrimation

Tear dilution

Blinking

BARRIERS

Drug loss from ocular surface Lacrimal fluid eye barrier

Blood ocular barriers Others

CORNEL AREA

Drug interaction

Drug protein interaction

Instilled dose

Corneal absorption

Normal tear turn overInduced lacrimation

Conjunctival absorption

Consists of a secretory distributive and collection part

Secretory portion composed of the lacrimalgland Tears are spread over the ocular surfaceby the eyelids during blinking

Collecting system consists of the canaliculithe lacrimal sac the nasolacrimal duct whichhas opening in the inferior

The basal tear flow is of about 12 microlmin(range 05ndash22 microlmin) Reflex stimulationmay increase lacrimation a hundred-fold times

Nasolacrimal drainage

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Medication is applied to the surface of the eye for two purposes

diams To treat the surface of eye

diams To provide intraocular treatment

90 ocular market conventional dosage form

5 of applied drug penetrates

Major challenge remains to past the protective ocular

barriers

Good corneal penetration

Prolong contact time with corneal tissue

Simplicity of instillation for the patient

Non irritative and comfortable form

Appropriate rheological properties

Ocular pharmacokinetics

Ocular structure with routes of drug kinetics

Systemic administration

Limited penetration potential systemic

toxicity

Intraocular implants

Increased risk of retinal detachment and

intravitrealhemorrahge

Intravitreal injections

Increased risk of retinal detachment hemorrhage

and catracts

Topical application

Limited penetration (5) rapid tear

washout poor patient compliance

Flow of lacrimal fluid removes instilledcompounds from the surface of eye

Excess volume is flown to thenasolacrimal duct rapidly

Corneal barrier is formed uponmaturation of epithelial cells

Most apical corneal epithelial cells fromtight junctions that limit the paracellulardrug permeation

These barriers have two parts

Blood retina barrier

Blood-aqueous barrier

Volume

Lacrimation

Tear dilution

Blinking

BARRIERS

Drug loss from ocular surface Lacrimal fluid eye barrier

Blood ocular barriers Others

CORNEL AREA

Drug interaction

Drug protein interaction

Instilled dose

Corneal absorption

Normal tear turn overInduced lacrimation

Conjunctival absorption

Consists of a secretory distributive and collection part

Secretory portion composed of the lacrimalgland Tears are spread over the ocular surfaceby the eyelids during blinking

Collecting system consists of the canaliculithe lacrimal sac the nasolacrimal duct whichhas opening in the inferior

The basal tear flow is of about 12 microlmin(range 05ndash22 microlmin) Reflex stimulationmay increase lacrimation a hundred-fold times

Nasolacrimal drainage

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Good corneal penetration

Prolong contact time with corneal tissue

Simplicity of instillation for the patient

Non irritative and comfortable form

Appropriate rheological properties

Ocular pharmacokinetics

Ocular structure with routes of drug kinetics

Systemic administration

Limited penetration potential systemic

toxicity

Intraocular implants

Increased risk of retinal detachment and

intravitrealhemorrahge

Intravitreal injections

Increased risk of retinal detachment hemorrhage

and catracts

Topical application

Limited penetration (5) rapid tear

washout poor patient compliance

Flow of lacrimal fluid removes instilledcompounds from the surface of eye

Excess volume is flown to thenasolacrimal duct rapidly

Corneal barrier is formed uponmaturation of epithelial cells

Most apical corneal epithelial cells fromtight junctions that limit the paracellulardrug permeation

These barriers have two parts

Blood retina barrier

Blood-aqueous barrier

Volume

Lacrimation

Tear dilution

Blinking

BARRIERS

Drug loss from ocular surface Lacrimal fluid eye barrier

Blood ocular barriers Others

CORNEL AREA

Drug interaction

Drug protein interaction

Instilled dose

Corneal absorption

Normal tear turn overInduced lacrimation

Conjunctival absorption

Consists of a secretory distributive and collection part

Secretory portion composed of the lacrimalgland Tears are spread over the ocular surfaceby the eyelids during blinking

Collecting system consists of the canaliculithe lacrimal sac the nasolacrimal duct whichhas opening in the inferior

The basal tear flow is of about 12 microlmin(range 05ndash22 microlmin) Reflex stimulationmay increase lacrimation a hundred-fold times

Nasolacrimal drainage

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Ocular pharmacokinetics

Ocular structure with routes of drug kinetics

Systemic administration

Limited penetration potential systemic

toxicity

Intraocular implants

Increased risk of retinal detachment and

intravitrealhemorrahge

Intravitreal injections

Increased risk of retinal detachment hemorrhage

and catracts

Topical application

Limited penetration (5) rapid tear

washout poor patient compliance

Flow of lacrimal fluid removes instilledcompounds from the surface of eye

Excess volume is flown to thenasolacrimal duct rapidly

Corneal barrier is formed uponmaturation of epithelial cells

Most apical corneal epithelial cells fromtight junctions that limit the paracellulardrug permeation

These barriers have two parts

Blood retina barrier

Blood-aqueous barrier

Volume

Lacrimation

Tear dilution

Blinking

BARRIERS

Drug loss from ocular surface Lacrimal fluid eye barrier

Blood ocular barriers Others

CORNEL AREA

Drug interaction

Drug protein interaction

Instilled dose

Corneal absorption

Normal tear turn overInduced lacrimation

Conjunctival absorption

Consists of a secretory distributive and collection part

Secretory portion composed of the lacrimalgland Tears are spread over the ocular surfaceby the eyelids during blinking

Collecting system consists of the canaliculithe lacrimal sac the nasolacrimal duct whichhas opening in the inferior

The basal tear flow is of about 12 microlmin(range 05ndash22 microlmin) Reflex stimulationmay increase lacrimation a hundred-fold times

Nasolacrimal drainage

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Systemic administration

Limited penetration potential systemic

toxicity

Intraocular implants

Increased risk of retinal detachment and

intravitrealhemorrahge

Intravitreal injections

Increased risk of retinal detachment hemorrhage

and catracts

Topical application

Limited penetration (5) rapid tear

washout poor patient compliance

Flow of lacrimal fluid removes instilledcompounds from the surface of eye

Excess volume is flown to thenasolacrimal duct rapidly

Corneal barrier is formed uponmaturation of epithelial cells

Most apical corneal epithelial cells fromtight junctions that limit the paracellulardrug permeation

These barriers have two parts

Blood retina barrier

Blood-aqueous barrier

Volume

Lacrimation

Tear dilution

Blinking

BARRIERS

Drug loss from ocular surface Lacrimal fluid eye barrier

Blood ocular barriers Others

CORNEL AREA

Drug interaction

Drug protein interaction

Instilled dose

Corneal absorption

Normal tear turn overInduced lacrimation

Conjunctival absorption

Consists of a secretory distributive and collection part

Secretory portion composed of the lacrimalgland Tears are spread over the ocular surfaceby the eyelids during blinking

Collecting system consists of the canaliculithe lacrimal sac the nasolacrimal duct whichhas opening in the inferior

The basal tear flow is of about 12 microlmin(range 05ndash22 microlmin) Reflex stimulationmay increase lacrimation a hundred-fold times

Nasolacrimal drainage

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Flow of lacrimal fluid removes instilledcompounds from the surface of eye

Excess volume is flown to thenasolacrimal duct rapidly

Corneal barrier is formed uponmaturation of epithelial cells

Most apical corneal epithelial cells fromtight junctions that limit the paracellulardrug permeation

These barriers have two parts

Blood retina barrier

Blood-aqueous barrier

Volume

Lacrimation

Tear dilution

Blinking

BARRIERS

Drug loss from ocular surface Lacrimal fluid eye barrier

Blood ocular barriers Others

CORNEL AREA

Drug interaction

Drug protein interaction

Instilled dose

Corneal absorption

Normal tear turn overInduced lacrimation

Conjunctival absorption

Consists of a secretory distributive and collection part

Secretory portion composed of the lacrimalgland Tears are spread over the ocular surfaceby the eyelids during blinking

Collecting system consists of the canaliculithe lacrimal sac the nasolacrimal duct whichhas opening in the inferior

The basal tear flow is of about 12 microlmin(range 05ndash22 microlmin) Reflex stimulationmay increase lacrimation a hundred-fold times

Nasolacrimal drainage

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

CORNEL AREA

Drug interaction

Drug protein interaction

Instilled dose

Corneal absorption

Normal tear turn overInduced lacrimation

Conjunctival absorption

Consists of a secretory distributive and collection part

Secretory portion composed of the lacrimalgland Tears are spread over the ocular surfaceby the eyelids during blinking

Collecting system consists of the canaliculithe lacrimal sac the nasolacrimal duct whichhas opening in the inferior

The basal tear flow is of about 12 microlmin(range 05ndash22 microlmin) Reflex stimulationmay increase lacrimation a hundred-fold times

Nasolacrimal drainage

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Consists of a secretory distributive and collection part

Secretory portion composed of the lacrimalgland Tears are spread over the ocular surfaceby the eyelids during blinking

Collecting system consists of the canaliculithe lacrimal sac the nasolacrimal duct whichhas opening in the inferior

The basal tear flow is of about 12 microlmin(range 05ndash22 microlmin) Reflex stimulationmay increase lacrimation a hundred-fold times

Nasolacrimal drainage

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Attainment of optimaldrug concentration

Enhance the poor bioavailability of drugs

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

To increase bioavailability and duration of ocular

drugs

Use of DDS which provide the controlled and continuous delivery

Maximizing corneal drug absorption and minimizing precorneal drug loss

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

1Viscosity enhancers

Solution Viscosity Solution Drainage

Enhances viscosity of the formulation

Slows elimination rate from the precorneal area and enhance contact time

Generally hydrophilic polymers- e Methyl cellulose polyvinyl alcohols

polyacrylic acids sodium carboxy methyl cellulose etc

A minimum viscosity of 20 cSt is needed for optimum corneal absorption

Approaches to overcome constraints of

conventional dosage form

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

2 Prodrugs

Prodrugs enhance corneal drug permeability through modification of the

hydrophilic or lipophilicity of the drug

The method includes modification of chemical structure of the drug molecule

thus making it selective site specific and a safe ocular drug delivery system

Drugs with increased penetrability through prodrug formulations are

epinehrine phenylephrine timolol pilocarpine

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Dipivefrine prodrug of epinephrine has 17 times better ability to penetrate

across the cornea Thus is because dipivefrine is 600times more lipophilic

(at pH 72) than epinephrine

Phenylephrine hydrochloride prodrug of phenylephrine raised the amount

of phenylephrine in the aqueous humor by 6-8 times and improved

mydriatic activity four fold

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Poor aqueous stability

Post aqueous solubility

Eye irritation

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Polymereric mucoadhesive vehicle retained in the eye due to non-

covalent bonding with conjuctival mucine

Mucine is capable of picking of 40-80 times of weight of water

Thus prolongs the residence time of drug in the conjuctival sac

Mucoadhesives contain the dosage form which remains adhered to

cornea until the polymer is degraded or mucus replaces itself

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Types-

1) Naturally Occurring Mucoadhesives- Lectins Fibronectins

2) Synthetic Mucoadhesives-PVACarbopol carboxy methyl

cellulose cross-linked polyacrylic acid

Drugs incarporated in to this are pilocarpine lidocaine

benzocaine and prednisolone acetate

Mucoadhesives

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Objectives

To reduce the frequency of administration

To provide controlled continuous drug delivery

To prolong the pre ocular retention

To avoid or minimize the initial drug concentration peak in the

aqueous humor

To avoid periods of under-dosing that may occur between eye

drop instillation

Novel ocular drug delivery system

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Novel ocular drug delivery system

Advantages

Sustained andor controlled drug release

Site-specific targeting

Protect the drug from chemical or enzymatic hydrolysis

Increasing contact time and thus improving bioavailability

Better patient compliance

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Vesicle composed of phospholipid bilayer enclosing

aqueous compartment in alternate fashion

Types 1MLV

2ULV

Polar drugs are incorporated in aqueous compartment while lipophilic drugs

are intercalated into the liposome membrane

Phospholipids used- Phosphotidylcholine Phosphotidic acid Sphingomyline

PhosphotidyleserineCardiolipine

LIPOSOMES

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Behaviour of liposomes as an ocular drug delivery system is due to their

surface charge

Degree of association of liposomes with corneal surface decreased in

order

MLV+ gt SUV+ gt MLV- gt SUV- gtMLV gt SUV

Eg Ocular formulation of Acetazolamide using liposome

Percentage entrapment efficency was 2927 4106 and

4958 for negatively neutral and positively charged

liposomes

Portion of drug released after 9h was 1336338 and 267

for negatively neutral and positively charged liposomes

LIPOSOMES

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

ADVANTAGES DISADVANTAGES

Drugs delivered intact to

various body tissues

Liposomes can be used for both

hydrophilic and hydrophobic

drug

Possibility of targeting and

decrease drug toxicity

The size charge and other

characteristics can be altered

according to drug and desired

tissue

Short shelf life

They need many modification

for drug delivery to special

organs

Cost

Limited drug capacity

Sterilization problems

LIPOSOMES

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Niosomes are non-ionic surfactant based multilamellar(gt005microm)small

unilamellar(0025-005microm) or large unilamellar vesicles(gt01microm)

Structural components used

bull Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)

bull Cholesterol

Niosomes

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

No difficulty of insertion

No tissue irritation and damage

Provide patient compliance

Biocompatible and have minimum side effects

Prevent the metabolism of drugs from the enzymes

Prolong and sustained release of drug

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Developed by Alza Corporation

Oval flexible ocular insert

Release Rate 20-40mghr

for 7day

Consist of-

Part Material

Drug Reservoir Pilocarpine

Carrier material Alginic acid

Rate controller Ethylene vinyl acetate

copolymer

Energy Source Conc Of Pilocarpine

Delivery Portal Copolymer membrane

Ocusert

Implantable systems

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

2 Contact lenses

Presoaked Hydrophilic lens

Drug Release within 1st 30 Min

Alternate approach incorporate drug either as solution or suspension of

solid monomer mixture

Release rate is up to 180 hr

3 Diffusional Inserts

Central reservoir of drug enclosed in Semi permeable or micro porous

membrane for diffusion of drug

Diffusion is controlled by lacrimal fluid penetrating through it

It prevents continues decrease in release rate due to barrier

Contact lens

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

4Lacrisert Sterile Rod Shaped device

Composition HPC without preservative

Weight5mg

DimensionDiameter125mm Length35mm

Use-Dry eye treatment Keratitis Sicca

5SODI Soluble Ocular Drug Insert

Small water soluble developed for Cosmonauts who could not use their eye drop in liquid condition

Composition Acryl amide Vinyl Pyrolidone Ethylacrylate

Weight 15-16 mg

Softens in 10-15 sec

In 10-15 min turns in viscous liquid

After 30-60min Becomes Polymeric Solution

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Poor patient compliance

Need of surgery

Difficulty in self insertion

Visulex system

OcuPhor

Visulex system

OcuPhor

Process in which direct current drives ions into cells or tissues

Positive charge they are driven into the tissues at the anode ifnegative charge at the cathode

Fast painless safe and results in the delivery of a high

concentration of the drug to a specific site

Ocular iontophoresis has gained significant interest recently due

to its non-invasive nature of delivery to both anterior and posterior

segment

Iontophoresis

CYCLODEXTRINS

Cyclodextrins (CDs) forming inclusion complexes with many

guest molecules

Aqueous solubility of hydrophobic drugs can be enhanced

without changing their molecular structure

They increase corneal permeation of drugs and increase ocular

bioavailability of poorly water soluble drugs

Insignificant dissociation of the administered complex

within the residence time in the precorneal fluid to release

the free drug into the tear film and at the corneal surface

Precorneal fluid was found to be too low to cause any

significant dissociation of the administered complex

Ophthalmic Solution Corresponding

Commercial Product

Concentration of

Active Ingredient

Uses

Adrenergic

Epinephrine bitartrate Epitrate Opthalmic

Solution (Ayerst)

2 Chronic open angle

glaucoma

Naphazoline HCl Naphcon Forte (Alcon) 01 Topical ocular

vasoconstricter

Anesthetic

Proparcaine HCl Ophthaine Opthalmic

Solution (Squibb)

05

Rapid acting local

anestheticTetracaine HCl Anacel Sterile

Opthalmic Solution

(Professional

Pharmacel)

05

Antibacterial

Chloramphenicol Ophthochlor Opthalmic

Solution (Parked avis)

05 Used for superficial

infections of eye due to

susceptible

microorganism

Gentamicin Sulfate Garamycin Opthalmic

Solution (Schering)

03

Marketed formulations

Anticholinergic

Atropine Sulfate Isopto Atropine

Opthalmic Solution

(Alcon)

0125 to 4

Used to produce

mydriasis and

cycloplegiaHomatropine HBr Isopto Homatropine

Opthalmic Solution

(Alcon)

2 and 5

Anti-inflammatory

Dexamethasone

sodium phosphate

opothalmic solution

Decadron Phosphate

(Merck

SharpampDohme)

01

Combats

inflammation due to

mechanicalchemical

or immunologic

causes

Prednisolone sodium

phosphate

Metreton Opthalmic

(Schering)

055

Cholinergic

Pilocarpine HCl Carbine Opthalmic

(Alcon)

025 to 10 Used as a miotic in

treating glaucoma

Marketed formulations

Ophthalmic

ointment

Commercial

product

Concentration of

active ingredient

Category

Atropine sulfate Atropine sulphate

ophthalmic

ointment

05 and 10 Parasympatholytic

Dexamethasone

sodium phosphate

Decadron phosphate

ophthalmic

ointment (Merk

Sharp ampDohme)

005 Antiinflammatory

Idoxuridine

Opthalmic ointment

Stoxil Opthalmic

ointment (Smith

kline )

05 Antiviral

Sulfisoxazole

diolamine

Gantrisin Opthalmic

Ointment (Roche)

4 Antibacterial

Marketed formulations

Drug Product Uses

Timolol maleate Timoptic-XE (MERCK amp

CO Inc)

Non-selective beta-

adrenergic

receptor blocking agent

Azithromycin AzaSite (InSite Vision) Antibacterial

Pilocarpine

hydrochloride

Pilopine HS Alcon

Laboratories

Lidocaine hydrochloride Akten Ocular surface anesthesia

Ganciclovir Virgan Acute herpetic

keratitis

Interleukin-2 (IL-2) Cytoryn Activates the

systemic antitumor immunity

Marketed formulations of In-situ drug delivery

1Optrex Actimist Eye Spray (Optima-Pharma Germany)

Ingrediants- Soy Lecithin Sodium Chloride Ethanol Phenoxyethanol

Pro-Vitamin B5 (Dexpanthenol) Vitamin A Palmitate Vitamin E Purified

Water

Use- Repair and restore dry irritated eyes

Working

2Dry eyes mist (Boots pharmaceuticals)

Use Soothes and relieves dry eyes

Moisturises eyes and lids

Ingrediants

Liposomate isoflavonoids Sodium hyaluronate Camomile extract N

hydroxymethylglycinate Isotonic buffer solution

Marketed Products of liposomes

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied

CYCLODEXTRINS

Cyclodextrins (CDs) forming inclusion complexes with many

guest molecules

Aqueous solubility of hydrophobic drugs can be enhanced

without changing their molecular structure

They increase corneal permeation of drugs and increase ocular

bioavailability of poorly water soluble drugs

Insignificant dissociation of the administered complex

within the residence time in the precorneal fluid to release

the free drug into the tear film and at the corneal surface

Precorneal fluid was found to be too low to cause any

significant dissociation of the administered complex

Ophthalmic Solution Corresponding

Commercial Product

Concentration of

Active Ingredient

Uses

Adrenergic

Epinephrine bitartrate Epitrate Opthalmic

Solution (Ayerst)

2 Chronic open angle

glaucoma

Naphazoline HCl Naphcon Forte (Alcon) 01 Topical ocular

vasoconstricter

Anesthetic

Proparcaine HCl Ophthaine Opthalmic

Solution (Squibb)

05

Rapid acting local

anestheticTetracaine HCl Anacel Sterile

Opthalmic Solution

(Professional

Pharmacel)

05

Antibacterial

Chloramphenicol Ophthochlor Opthalmic

Solution (Parked avis)

05 Used for superficial

infections of eye due to

susceptible

microorganism

Gentamicin Sulfate Garamycin Opthalmic

Solution (Schering)

03

Marketed formulations

Anticholinergic

Atropine Sulfate Isopto Atropine

Opthalmic Solution

(Alcon)

0125 to 4

Used to produce

mydriasis and

cycloplegiaHomatropine HBr Isopto Homatropine

Opthalmic Solution

(Alcon)

2 and 5

Anti-inflammatory

Dexamethasone

sodium phosphate

opothalmic solution

Decadron Phosphate

(Merck

SharpampDohme)

01

Combats

inflammation due to

mechanicalchemical

or immunologic

causes

Prednisolone sodium

phosphate

Metreton Opthalmic

(Schering)

055

Cholinergic

Pilocarpine HCl Carbine Opthalmic

(Alcon)

025 to 10 Used as a miotic in

treating glaucoma

Marketed formulations

Ophthalmic

ointment

Commercial

product

Concentration of

active ingredient

Category

Atropine sulfate Atropine sulphate

ophthalmic

ointment

05 and 10 Parasympatholytic

Dexamethasone

sodium phosphate

Decadron phosphate

ophthalmic

ointment (Merk

Sharp ampDohme)

005 Antiinflammatory

Idoxuridine

Opthalmic ointment

Stoxil Opthalmic

ointment (Smith

kline )

05 Antiviral

Sulfisoxazole

diolamine

Gantrisin Opthalmic

Ointment (Roche)

4 Antibacterial

Marketed formulations

Drug Product Uses

Timolol maleate Timoptic-XE (MERCK amp

CO Inc)

Non-selective beta-

adrenergic

receptor blocking agent

Azithromycin AzaSite (InSite Vision) Antibacterial

Pilocarpine

hydrochloride

Pilopine HS Alcon

Laboratories

Lidocaine hydrochloride Akten Ocular surface anesthesia

Ganciclovir Virgan Acute herpetic

keratitis

Interleukin-2 (IL-2) Cytoryn Activates the

systemic antitumor immunity

Marketed formulations of In-situ drug delivery

1Optrex Actimist Eye Spray (Optima-Pharma Germany)

Ingrediants- Soy Lecithin Sodium Chloride Ethanol Phenoxyethanol

Pro-Vitamin B5 (Dexpanthenol) Vitamin A Palmitate Vitamin E Purified

Water

Use- Repair and restore dry irritated eyes

Working

2Dry eyes mist (Boots pharmaceuticals)

Use Soothes and relieves dry eyes

Moisturises eyes and lids

Ingrediants

Liposomate isoflavonoids Sodium hyaluronate Camomile extract N

hydroxymethylglycinate Isotonic buffer solution

Marketed Products of liposomes

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied

Insignificant dissociation of the administered complex

within the residence time in the precorneal fluid to release

the free drug into the tear film and at the corneal surface

Precorneal fluid was found to be too low to cause any

significant dissociation of the administered complex

Ophthalmic Solution Corresponding

Commercial Product

Concentration of

Active Ingredient

Uses

Adrenergic

Epinephrine bitartrate Epitrate Opthalmic

Solution (Ayerst)

2 Chronic open angle

glaucoma

Naphazoline HCl Naphcon Forte (Alcon) 01 Topical ocular

vasoconstricter

Anesthetic

Proparcaine HCl Ophthaine Opthalmic

Solution (Squibb)

05

Rapid acting local

anestheticTetracaine HCl Anacel Sterile

Opthalmic Solution

(Professional

Pharmacel)

05

Antibacterial

Chloramphenicol Ophthochlor Opthalmic

Solution (Parked avis)

05 Used for superficial

infections of eye due to

susceptible

microorganism

Gentamicin Sulfate Garamycin Opthalmic

Solution (Schering)

03

Marketed formulations

Anticholinergic

Atropine Sulfate Isopto Atropine

Opthalmic Solution

(Alcon)

0125 to 4

Used to produce

mydriasis and

cycloplegiaHomatropine HBr Isopto Homatropine

Opthalmic Solution

(Alcon)

2 and 5

Anti-inflammatory

Dexamethasone

sodium phosphate

opothalmic solution

Decadron Phosphate

(Merck

SharpampDohme)

01

Combats

inflammation due to

mechanicalchemical

or immunologic

causes

Prednisolone sodium

phosphate

Metreton Opthalmic

(Schering)

055

Cholinergic

Pilocarpine HCl Carbine Opthalmic

(Alcon)

025 to 10 Used as a miotic in

treating glaucoma

Marketed formulations

Ophthalmic

ointment

Commercial

product

Concentration of

active ingredient

Category

Atropine sulfate Atropine sulphate

ophthalmic

ointment

05 and 10 Parasympatholytic

Dexamethasone

sodium phosphate

Decadron phosphate

ophthalmic

ointment (Merk

Sharp ampDohme)

005 Antiinflammatory

Idoxuridine

Opthalmic ointment

Stoxil Opthalmic

ointment (Smith

kline )

05 Antiviral

Sulfisoxazole

diolamine

Gantrisin Opthalmic

Ointment (Roche)

4 Antibacterial

Marketed formulations

Drug Product Uses

Timolol maleate Timoptic-XE (MERCK amp

CO Inc)

Non-selective beta-

adrenergic

receptor blocking agent

Azithromycin AzaSite (InSite Vision) Antibacterial

Pilocarpine

hydrochloride

Pilopine HS Alcon

Laboratories

Lidocaine hydrochloride Akten Ocular surface anesthesia

Ganciclovir Virgan Acute herpetic

keratitis

Interleukin-2 (IL-2) Cytoryn Activates the

systemic antitumor immunity

Marketed formulations of In-situ drug delivery

1Optrex Actimist Eye Spray (Optima-Pharma Germany)

Ingrediants- Soy Lecithin Sodium Chloride Ethanol Phenoxyethanol

Pro-Vitamin B5 (Dexpanthenol) Vitamin A Palmitate Vitamin E Purified

Water

Use- Repair and restore dry irritated eyes

Working

2Dry eyes mist (Boots pharmaceuticals)

Use Soothes and relieves dry eyes

Moisturises eyes and lids

Ingrediants

Liposomate isoflavonoids Sodium hyaluronate Camomile extract N

hydroxymethylglycinate Isotonic buffer solution

Marketed Products of liposomes

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied

Ophthalmic Solution Corresponding

Commercial Product

Concentration of

Active Ingredient

Uses

Adrenergic

Epinephrine bitartrate Epitrate Opthalmic

Solution (Ayerst)

2 Chronic open angle

glaucoma

Naphazoline HCl Naphcon Forte (Alcon) 01 Topical ocular

vasoconstricter

Anesthetic

Proparcaine HCl Ophthaine Opthalmic

Solution (Squibb)

05

Rapid acting local

anestheticTetracaine HCl Anacel Sterile

Opthalmic Solution

(Professional

Pharmacel)

05

Antibacterial

Chloramphenicol Ophthochlor Opthalmic

Solution (Parked avis)

05 Used for superficial

infections of eye due to

susceptible

microorganism

Gentamicin Sulfate Garamycin Opthalmic

Solution (Schering)

03

Marketed formulations

Anticholinergic

Atropine Sulfate Isopto Atropine

Opthalmic Solution

(Alcon)

0125 to 4

Used to produce

mydriasis and

cycloplegiaHomatropine HBr Isopto Homatropine

Opthalmic Solution

(Alcon)

2 and 5

Anti-inflammatory

Dexamethasone

sodium phosphate

opothalmic solution

Decadron Phosphate

(Merck

SharpampDohme)

01

Combats

inflammation due to

mechanicalchemical

or immunologic

causes

Prednisolone sodium

phosphate

Metreton Opthalmic

(Schering)

055

Cholinergic

Pilocarpine HCl Carbine Opthalmic

(Alcon)

025 to 10 Used as a miotic in

treating glaucoma

Marketed formulations

Ophthalmic

ointment

Commercial

product

Concentration of

active ingredient

Category

Atropine sulfate Atropine sulphate

ophthalmic

ointment

05 and 10 Parasympatholytic

Dexamethasone

sodium phosphate

Decadron phosphate

ophthalmic

ointment (Merk

Sharp ampDohme)

005 Antiinflammatory

Idoxuridine

Opthalmic ointment

Stoxil Opthalmic

ointment (Smith

kline )

05 Antiviral

Sulfisoxazole

diolamine

Gantrisin Opthalmic

Ointment (Roche)

4 Antibacterial

Marketed formulations

Drug Product Uses

Timolol maleate Timoptic-XE (MERCK amp

CO Inc)

Non-selective beta-

adrenergic

receptor blocking agent

Azithromycin AzaSite (InSite Vision) Antibacterial

Pilocarpine

hydrochloride

Pilopine HS Alcon

Laboratories

Lidocaine hydrochloride Akten Ocular surface anesthesia

Ganciclovir Virgan Acute herpetic

keratitis

Interleukin-2 (IL-2) Cytoryn Activates the

systemic antitumor immunity

Marketed formulations of In-situ drug delivery

1Optrex Actimist Eye Spray (Optima-Pharma Germany)

Ingrediants- Soy Lecithin Sodium Chloride Ethanol Phenoxyethanol

Pro-Vitamin B5 (Dexpanthenol) Vitamin A Palmitate Vitamin E Purified

Water

Use- Repair and restore dry irritated eyes

Working

2Dry eyes mist (Boots pharmaceuticals)

Use Soothes and relieves dry eyes

Moisturises eyes and lids

Ingrediants

Liposomate isoflavonoids Sodium hyaluronate Camomile extract N

hydroxymethylglycinate Isotonic buffer solution

Marketed Products of liposomes

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied

Anticholinergic

Atropine Sulfate Isopto Atropine

Opthalmic Solution

(Alcon)

0125 to 4

Used to produce

mydriasis and

cycloplegiaHomatropine HBr Isopto Homatropine

Opthalmic Solution

(Alcon)

2 and 5

Anti-inflammatory

Dexamethasone

sodium phosphate

opothalmic solution

Decadron Phosphate

(Merck

SharpampDohme)

01

Combats

inflammation due to

mechanicalchemical

or immunologic

causes

Prednisolone sodium

phosphate

Metreton Opthalmic

(Schering)

055

Cholinergic

Pilocarpine HCl Carbine Opthalmic

(Alcon)

025 to 10 Used as a miotic in

treating glaucoma

Marketed formulations

Ophthalmic

ointment

Commercial

product

Concentration of

active ingredient

Category

Atropine sulfate Atropine sulphate

ophthalmic

ointment

05 and 10 Parasympatholytic

Dexamethasone

sodium phosphate

Decadron phosphate

ophthalmic

ointment (Merk

Sharp ampDohme)

005 Antiinflammatory

Idoxuridine

Opthalmic ointment

Stoxil Opthalmic

ointment (Smith

kline )

05 Antiviral

Sulfisoxazole

diolamine

Gantrisin Opthalmic

Ointment (Roche)

4 Antibacterial

Marketed formulations

Drug Product Uses

Timolol maleate Timoptic-XE (MERCK amp

CO Inc)

Non-selective beta-

adrenergic

receptor blocking agent

Azithromycin AzaSite (InSite Vision) Antibacterial

Pilocarpine

hydrochloride

Pilopine HS Alcon

Laboratories

Lidocaine hydrochloride Akten Ocular surface anesthesia

Ganciclovir Virgan Acute herpetic

keratitis

Interleukin-2 (IL-2) Cytoryn Activates the

systemic antitumor immunity

Marketed formulations of In-situ drug delivery

1Optrex Actimist Eye Spray (Optima-Pharma Germany)

Ingrediants- Soy Lecithin Sodium Chloride Ethanol Phenoxyethanol

Pro-Vitamin B5 (Dexpanthenol) Vitamin A Palmitate Vitamin E Purified

Water

Use- Repair and restore dry irritated eyes

Working

2Dry eyes mist (Boots pharmaceuticals)

Use Soothes and relieves dry eyes

Moisturises eyes and lids

Ingrediants

Liposomate isoflavonoids Sodium hyaluronate Camomile extract N

hydroxymethylglycinate Isotonic buffer solution

Marketed Products of liposomes

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied

Ophthalmic

ointment

Commercial

product

Concentration of

active ingredient

Category

Atropine sulfate Atropine sulphate

ophthalmic

ointment

05 and 10 Parasympatholytic

Dexamethasone

sodium phosphate

Decadron phosphate

ophthalmic

ointment (Merk

Sharp ampDohme)

005 Antiinflammatory

Idoxuridine

Opthalmic ointment

Stoxil Opthalmic

ointment (Smith

kline )

05 Antiviral

Sulfisoxazole

diolamine

Gantrisin Opthalmic

Ointment (Roche)

4 Antibacterial

Marketed formulations

Drug Product Uses

Timolol maleate Timoptic-XE (MERCK amp

CO Inc)

Non-selective beta-

adrenergic

receptor blocking agent

Azithromycin AzaSite (InSite Vision) Antibacterial

Pilocarpine

hydrochloride

Pilopine HS Alcon

Laboratories

Lidocaine hydrochloride Akten Ocular surface anesthesia

Ganciclovir Virgan Acute herpetic

keratitis

Interleukin-2 (IL-2) Cytoryn Activates the

systemic antitumor immunity

Marketed formulations of In-situ drug delivery

1Optrex Actimist Eye Spray (Optima-Pharma Germany)

Ingrediants- Soy Lecithin Sodium Chloride Ethanol Phenoxyethanol

Pro-Vitamin B5 (Dexpanthenol) Vitamin A Palmitate Vitamin E Purified

Water

Use- Repair and restore dry irritated eyes

Working

2Dry eyes mist (Boots pharmaceuticals)

Use Soothes and relieves dry eyes

Moisturises eyes and lids

Ingrediants

Liposomate isoflavonoids Sodium hyaluronate Camomile extract N

hydroxymethylglycinate Isotonic buffer solution

Marketed Products of liposomes

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied

Drug Product Uses

Timolol maleate Timoptic-XE (MERCK amp

CO Inc)

Non-selective beta-

adrenergic

receptor blocking agent

Azithromycin AzaSite (InSite Vision) Antibacterial

Pilocarpine

hydrochloride

Pilopine HS Alcon

Laboratories

Lidocaine hydrochloride Akten Ocular surface anesthesia

Ganciclovir Virgan Acute herpetic

keratitis

Interleukin-2 (IL-2) Cytoryn Activates the

systemic antitumor immunity

Marketed formulations of In-situ drug delivery

1Optrex Actimist Eye Spray (Optima-Pharma Germany)

Ingrediants- Soy Lecithin Sodium Chloride Ethanol Phenoxyethanol

Pro-Vitamin B5 (Dexpanthenol) Vitamin A Palmitate Vitamin E Purified

Water

Use- Repair and restore dry irritated eyes

Working

2Dry eyes mist (Boots pharmaceuticals)

Use Soothes and relieves dry eyes

Moisturises eyes and lids

Ingrediants

Liposomate isoflavonoids Sodium hyaluronate Camomile extract N

hydroxymethylglycinate Isotonic buffer solution

Marketed Products of liposomes

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied

1Optrex Actimist Eye Spray (Optima-Pharma Germany)

Ingrediants- Soy Lecithin Sodium Chloride Ethanol Phenoxyethanol

Pro-Vitamin B5 (Dexpanthenol) Vitamin A Palmitate Vitamin E Purified

Water

Use- Repair and restore dry irritated eyes

Working

2Dry eyes mist (Boots pharmaceuticals)

Use Soothes and relieves dry eyes

Moisturises eyes and lids

Ingrediants

Liposomate isoflavonoids Sodium hyaluronate Camomile extract N

hydroxymethylglycinate Isotonic buffer solution

Marketed Products of liposomes

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied

2Dry eyes mist (Boots pharmaceuticals)

Use Soothes and relieves dry eyes

Moisturises eyes and lids

Ingrediants

Liposomate isoflavonoids Sodium hyaluronate Camomile extract N

hydroxymethylglycinate Isotonic buffer solution

Marketed Products of liposomes

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied

Although eye drops represent 90 of all opthalmic dosage forms there is

significant effort directed towards new drug delivery systems

Most formulation efforts aim at maximizing ocular drug absorption

through prolongation of the drug residence time

Newer concepts of introducing vesicular prodrugs in situ gel inserts

iontophoresis viscosity and permeation enhancers have been explored

Among the novel delivery vesicular and in situ systems emerged to be

most exploited sections in ocular drug delivery

However for future prespective in depth knowledge about the

physicochemical characteristics of the drug molecule and expected

interaction and implication of entrapping has to be studied