WELCOME
ROUTES OF ADMINISTRATION OF BIOTECH PRODUCTS:
PARENTERAL ROUTES CONSIDERING NANOPARTICLES
& MICROEMULSION
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PRESENTED BY
GROUP MEMBERS REGISTRATION NO
Rachana Sarkar 12103022
Susmita Ghosh 12103023
Furhatun-Noor 12103048
Priyanka Florina Karmokar 12103050
Tajrian Rahman 12103059
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CONTENTS
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Microemulsion
– Advantages and disadvantges of microemulsion
– Classification
– Preparation
– Application
– Overview of parenteral microemulsion and their in-vivo
advantages
– Microemulsion based marketed product
CONTENTS
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BIOTECH PRODUCTS
Biotech is the term used for
biotechnology or products
produced by biotechnology.
True biotech products are
manufactured in live biological
systems known as expression
systems.
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ROUTE OF ADMINISTRATION OF BIOTECH DRUG PRODUCTS
Route of Administratio
n
Oral Parenteral Nasal Transmucosal
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PARENTERAL ROUTE OF ADMINISTRATION
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PARENTERAL DRUG DELIVERY SYSTEM OF BIOTECH PRODUCT
The drug carrier systems used for defined and controlled delivery of drug through this route can be: Particulates Soluble carriers (Macromolecules) Others
There are different types of particulate carrier systems .These are: Microspheres Microcapsules Nanoparticles Aquasomes Liposomes Emulsions
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IMPORTANCE OF PARTICULATE CARRIERS IN BIOTECH DRUG PODUCTS
Importance
Increased patient efficacy
Increased specific
localization
Decreased toxic side
effects
Reduced dose
Controlled bio
distribution
Modulated pharmacoki
netics
Improved patient
compliance
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NANOPARTICLES
Nanoparticles are the end products of a wide variety of physical, chemical and biological processes some of which are novel and radically different, others of which are quite commonplace.
Nanoparticles may be defined as submicron (<1µm) colloidal systems, generally, but not necessarily, made of polymers (biodegradable or not).
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Nanoparticles
Nanospheres (Matrix type
structure in which a drug is
dispersed)
Nanocapsules (Membrane wall structure with an
oil core containing drug)
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ADVANTAGES OF NANOPARTICLES
Can be administered by parenteral, oral, nasal, ocular routes.
By attaching specific ligands on to their surfaces, nano particles can be used for directing the drugs to specific target cells.
Improves stability and therapeutic index and reduce toxic effects.
Both active & passive drug targeting can be achieved by manipulating the particle size and surface characteristics of nano particles
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ADVANTAGES OF NANOPARTICLES
Small size & large surface area can lead to particle aggregation .
Physical handling of nano particles is difficult in liquid and dry forms.
Limited drug loading.
Toxic metabolites may form.
DISADVANTAGES OF NANOPARTICLES
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TYPES OF NANOCARRIERS
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PREPARATION OF POLYMERIC NANOPARTICLES
Preparation Methods
Polymerization Preformed Polymer
Supercritical Fluid
Technique
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Polymerization
Dispersion Polymerization
Emulsion Polymerization
PREPARATION OF POLYMERIC NANOPARTICLES
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Pref
orm
ed P
olym
erSolvent
Evaporation
Solvent Displacement
Salting out
PREPARATION OF POLYMERIC NANOPARTICLES
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APPLICATIONS OF NANOPARTICLES
Nanomedicine
Chemicals & Cosmetics Food Science Materials Electronics
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APPLICATION OF NANOPARTICLES IN MEDICINE
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SELECTED NANOPARTICLE BASED PARENTERAL THERAPEUTICS APPROVED BY FDA
AMBISONE ABRAXANE
MACGUEN SOMAVERT
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SELECTED NANOPARTICLE BASED PARENTERAL THERAPEUTICS APPROVED BY FDA
Brand Name Nanoparticle Component
Company Indication
Abraxane paclitaxel (taxol) boundalbumin nanoparticles
AbraxisBioScience
AstraZeneca
metastatic breastcancer patientswho have failed
combinationtherapy
Ambisome Amphotericin B liposomes
Gilead Sciences
Fungal infection
Macugen pegylated anti-VEGFaptamer
OSIPharmaceutical
sPfizer
neovascular age-related macular
degeneration
Somavert pegvisomant (PEG-hGH) NektarPfizer
Nacromegaly
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WHAT IS MICROEMULSION?
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MICOEMULSION is a-
Homogenous
Transparent
Thermodynamically stable
dispersion of water & oil
Stabilized by Surfactant
Co-surfactant is combined
Diameter of droplets between
100Å to1000Å.
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HISTORY & DEVELOPMENT OF MICROEMULSION
INVENTORS CONTRIBUTION YEAR
Hoar & Schulman Introduce the concept of “MICROEMULSION” by generating clear
phase solution
1943
Schulman Coined the term “ MICROEMULSION”
1959
Rodawald First commercial “MICROEMULSION” was dicovered
1928
Danielson & Lindman
Definition of MICROEMULSIONprovided 1981
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COMPARISON BETWEEN EMULSION & MICROEMULSION
Thermodynamically unstable. In due time phases it is separate
out. It is cloudy. Require large input of energy
during its preparation. higher cost.
Droplet size > 500 nm Interfacial tension: high High viscosity
MICROMULSION
Thermodynamically stable. In due time phases it is not
separate out. It is transparent. Require low input of energy
during its preparation. relatively low cost.
Droplet size 10-200 nm Interfacial tension: ultra low Low viscosity with Newtonian
behavior.
EMULSION
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COMPARISON BETWEEN EMULSION & MICROEMULSION
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ADVANTAGES OF MICROEMULSION BASED SYSTEM
Increases the rate of absorption .
Eliminates variability in absorption
Helps to solubilize lipophilic drug
Provides a aqueous dosage form for water insoluble drugs
Increases bioavailability
Various routes like topical, oral and intravenous can be
used to deliver the product
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• Rapid and efficient penetration of the drug moiety.
• Helpful in taste masking
• Provides protection from hydrolysis and oxidation
• Liquid dosage form increases patient compliance.
• Less amount of energy requirement.
ADVANTAGES OF MICROEMULSION BASED SYSTEM
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Large concentration of surfactant and co-surfactant are required.
Limited solubilizing capacity for high-melting substances.
The surfactant must be nontoxic for using pharmaceutical
applications.
Microemulsion stability is influenced by environmental
parameters.
DISADVANTAGES OF MICROEMULSION BASED SYSTEM
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CLASSIFICATION OF MICROEMULSION
• With two phases , the lower
• o/w type
Winsor I
• With two phases, the upper
• w/o type
Winsor II• With
three phases, the middle
• o/w+w/o type
Winsor III
• In a Single phase, with oil, water & surfactant
Winsor IV
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CLASSIFICATION OF MICROEMULSION
Types of Microemulsion
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COMPONENTS OF MICROEMULSION
Aqueous Phase
• Water
Oil Phase
• Isopropyl Myristate
• Mineral oil
• Olive oil• Oleic acid
Surfactant
• Tween 80• Tween 40• Span 40• Lecithin
Co-surfactant
• PEG 400• Propylene
glycol• Ethylene
glycol• Glycerol
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PREPARATION OF MICROEMULSION
Preparation Method of
Microemulsion
Phase Titration Method
Phase Inversion Method
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PHASE TITRATION METHOD
Aqueous Phase Titration Method
Oil+Surfactant+Co-surfactant
Titration with water
Stirring
Clear dispersion
Microemulsion
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PHASE INVERSION METHOD
Carried out upon addition of excess of the dispersed phase
or in response to temperature.
Drastic physical changes occur.
Water droplet added to oil phase
Stabilizing o/w to w/o microemulsion
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APPLICATIONS OF MICROEMULSION
Microemulsion
Drug Delivery System
Biotechnology
Cosmetics
PharmaceuticalsAgrochemicals
Food Science
Others
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MICROEMULSION IN DRUG DELIVERY SYSTEMS
Applications
Parenteral Administration.
Oral drug delivery.
Topical drug delivery.
Ocular and pulmonary
delivery.
Micro-emulsions in
biotechnology
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OVERVIEW OF PARENTERAL MICROEMULSION AND THEIR IN-VIVO ADVANTAGES
DRUG NAME IN-VIVO ADVANTAGE
Paclitaxel Less hypersensitivity reaction, higher AUC value and prolonged circulation as compared with Taxol
Flurbiprofen Prolonged circulation and higher AUC values as compared with the solution
Clonixic acid Less painful as compared with marketed formulation
Vincristine Higher efficacy, survival rate and lesser side effects as compared with free drug
Ibuprofen Prolonged circulation and higher AUC values as compared with the solution.Source: Katiyar et al., 2013
Source: (Nagarsenkar et al., 2008).Source: (Nagarsenkar et al., 2008).
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MICROEMULSION BASED MARKETED PRODUCT
Brand Name Composition Manufacturer
Sandimmune Neoral® Cyclosporin A Novartis
Norvir ® Ritonavir Roche laboratories
Fortovase ® Saquinavir Roche laboratories
White Glow Mulberry Extract Lotus Herbals
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Enhancing the efficacy of existing of drug is an ongoing process in
pharmaceutical research.
Multiferous materials and principles have been employed to generate
polymer-based particulate systems and rigid, semi-rigid and vescicular
lipoidal colloid drug delivery vehicles.
Microemulsion has achieved a favorable position because of their non
particulate nature, components of bio-origin and provisions for
modifications in the constructs so that they can be tailored to suit the
target site.
CONCLUSION
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REFERENCE
• Bhowmik D, Harish.GB, Kumar, Aravind G. MICROEMULSIFYING DRUG DELIVERY
SYSTEM-NEW ERA OF DRUG DELIVERY SYSTEM. Indian Journal of Research in
Pharmacy and Biotechnology, 2013; 1(1): 47.
• Ghosh PK, Murthy RS, “Microemulsions: A potential drug delivery system”, Current
Drug Delivery, 3(2), 2006, 167-180.
• Jha SK, Dey S, Karki R. Microemulsions- Potential Carrier for Improved Drug
Delivery. Asian Journal of Biomedical and Pharmaceutical Sciences, 2011; 1 (1): 5-9.
• Katiyar BS, Katiyar SS, Mishra PS, Sailaja DL. Microemulsions: A Novel Drug Carrier
System. International Journal of Pharmaceutical Sciences Review and Research, May
– Jun 2013; 20(2): 138-148.
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