micro spheres
DESCRIPTION
pharmacy powerpoint presentationsTRANSCRIPT
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-:Contents of Seminar :-
Introduction
Advantage
Polymar used for preparation
General Method of Preparation
Characterization of Microspheres.
Application of Microspheres2Visit www.bpharmstuf.com
-: Introduction :-
• Microspheres are solid , approximately spherical
particles ranging 1-1000µm in size.
• They are made up of polymeric substance in which
the drug is dispersed through out the microspheres
matrix.
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ADVANTAGE OF MICROSPHERES: They facilitate accurate delivery of small quantities of potent drug and
reduced concentration of drug at site other than the target organ or tissue.
They provide protection for unstable drug before and after
administration, prior to their availability at the site of action.
They provide the ability to manipulate the in vivo action of the drug,
pharmacokinetic profile, tissue distribution and cellular interaction of the
drug.
They enable controlled release of drug.
Ex: narcotic, antagonist, steroid hormones
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POLYMER Used for Microspheres preparation:
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The administration parameters that can be satisfactorily controlled are as follow:
• Taste and odour masking
• Conversion of oil and other liquids, facilitating ease of handling
• Protaction of the drug from the environment
• Delay of volatillisation
• Freedom from incompatibilities between drug and
excipients,especially the buffers
• Improvement of flow properties
• Safe handling of test masking
• Dispersion of water insoluble substance in aqueous media
• Production of sustained release, controlled release and targeted
medication
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General Method of Preparation:
a) Single Emulsion Technique
b) Double Emulsion Technique
c) Polymerization Technique
d) Phase Separation Coacervation
e) Spray drying &spray coating
f) Solvent Extraction8Visit www.bpharmstuf.com
A) Single Emulsion Technique Aqous solution /suspension of polymer(natural polymer)
stirring / sonication
dispersion in orgenic phase oil/chcl3
cross linking
Heat denaturation chemical crosslinking
(by adding dispersion (butanol,HCHO,Glutaraldehyde)
To heated oil)
Aqous solution /suspension of polymer(natural polymer)
stirring / sonication
dispersion in orgenic phase oil/chcl3
cross linking
Heat denaturation chemical crosslinking
(by adding dispersion (butanol,HCHO,Glutaraldehyde)
To heated oil)
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Microspheres in org.phase Microspheres in org.phase
Centrifugation,washing,separation
Microspheres
Microspheres in org.phase Microspheres in org.phase
Centrifugation,washing,separation
Microspheres
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Single Emulsion Technique
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B) Double Emulsion Technique
Aqueous solution of polymer
dispersion in oil/orgenic phase, vigorous homogenisation(sonication)
Primary emulsion(w/o)
addition of aqueous solution of PVA
W/O/W multipal emulsion
addition of large aq. Phase
MICROSPHERES in solution
Aqueous solution of polymer
dispersion in oil/orgenic phase, vigorous homogenisation(sonication)
Primary emulsion(w/o)
addition of aqueous solution of PVA
W/O/W multipal emulsion
addition of large aq. Phase
MICROSPHERES in solution
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Separation,washing, drying
MICROSPHERES
Separation,washing, drying
MICROSPHERES
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C)Polymerization
A)Normal Polymerization:Normal Polymerization is done by bulk, suspension, pption,emulsion and
polymerization process.
1.Bulk polymerization: Monomer Bioactive material Initiator Heated to initiate polymerization Initiator accelerate rate of raction
Polymer(Block) Moulded/fragmented
MICROSPHERES
A)Normal Polymerization:Normal Polymerization is done by bulk, suspension, pption,emulsion and
polymerization process.
1.Bulk polymerization: Monomer Bioactive material Initiator Heated to initiate polymerization Initiator accelerate rate of raction
Polymer(Block) Moulded/fragmented
MICROSPHERES14Visit www.bpharmstuf.com
B)Suspension polymerization
Monomer Bioactive material Initiator
Dispersion in water and stebilizer
Droplet
Vigorous ,Aggitation Polymerization by Heat
Hardened microspheres
Separation&Drying
MICROSP HERES
Monomer Bioactive material Initiator
Dispersion in water and stebilizer
Droplet
Vigorous ,Aggitation Polymerization by Heat
Hardened microspheres
Separation&Drying
MICROSP HERES
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3) Emulsion PolymerisationMonomer/ Aq.Solution of NaOH,
Bioactive material Initiator, Surfactant , Stabilizer
Dispersion with vigorous stirring
Micellar sol. Of Polymer in aqueous medium
Polymarization
Microspheres formation
MICROSPHERES
Monomer/ Aq.Solution of NaOH,
Bioactive material Initiator, Surfactant , Stabilizer
Dispersion with vigorous stirring
Micellar sol. Of Polymer in aqueous medium
Polymarization
Microspheres formation
MICROSPHERES 16Visit www.bpharmstuf.com
D)Phase Sepration CoacervationD)Phase Sepration Coacervation Aq./orgenic solution of polymer
Drug dispersed or dissolved in the polymer solution Phase sepration by salt addition, non solvent addition add. Incompatible polymer,etc Polymer rich globules Hardening microspheres in aqu./orgenic phase sepration/drying MICROSPHERES
Aq./orgenic solution of polymer
Drug dispersed or dissolved in the polymer solution Phase sepration by salt addition, non solvent addition add. Incompatible polymer,etc Polymer rich globules Hardening microspheres in aqu./orgenic phase sepration/drying MICROSPHERES 17Visit www.bpharmstuf.com
Phase Sepration Coacervation
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E)Spray DryingE)Spray Drying Polymer dissolve in volatile organic solvent(acetone,dichloromethane)
Drug dispersed in polymer solution under high speed homogenization
Atomized in a stream of hot air
Due to solvent evaporation small droplet or fine mist form
Leads to formation of Microspheres
Microspheres separated from hot air by cyclone separator,Trace of solvent are removed by vacuum drying
Polymer dissolve in volatile organic solvent(acetone,dichloromethane)
Drug dispersed in polymer solution under high speed homogenization
Atomized in a stream of hot air
Due to solvent evaporation small droplet or fine mist form
Leads to formation of Microspheres
Microspheres separated from hot air by cyclone separator,Trace of solvent are removed by vacuum drying 19Visit www.bpharmstuf.com
F)Solvent ExtractionF)Solvent Extraction Drug is dispersed in organic solvent
(water miscible organic solvent such as Isopropanol)
Polymer in organic solvent
Organic phase is removed by extraction with water (This process decreasing hardening time for microspheres)
Hardened microspheres
Drug is dispersed in organic solvent
(water miscible organic solvent such as Isopropanol)
Polymer in organic solvent
Organic phase is removed by extraction with water (This process decreasing hardening time for microspheres)
Hardened microspheres
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Solvent extraction apparatusS
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Characterization of MicrospheresCharacterization of Microspheres
Partical size & shape
Surface chemistry by Electron Spectroscopy
The Surface chemistry of microspheres can be determine using the
electron spectroscopy for chemical analaysis It provide a mens of
determination of atomic composition of the surface.
Release study
Usually carried out in phosphate saline buffer ph 7.4.
Two method 1) Rotating paddle dissolution apparatus.
2) Dialysis method 22Visit www.bpharmstuf.com
Iso electric point
Microelectrophoresis apparatus is used to measure
elecrophoretic mobility of microspheres from which
isoelectric point can be determine.
It can be correlated to surface charge or ion adsorption of
microspheres.
Density Determination
Density measured dy using a multivolume pychometer.
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Application of MicrospheresApplication of Microspheres
Microspheres in Vaccine delivery
Targeting of Drug
Magnetic Microspheres
Immunomicrospheres
Microsponges: Topical Porous Microspheres
Imaging
Surface modifide Microspheres 24Visit www.bpharmstuf.com
REFERENCES
• http://www.daviddarling.info/encyclopedia/M/microsphere.html
• www.rsc.org/chemistryworld/News/2010/.../22071001.asp
• www.physorg.com/news187971041.htm• REZA ARSHADY- MICROSPHERES
MICROCAPSULES &LIPOSOMES
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