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-:Contents of Seminar :Introduction Advantage Polymar used for preparation General Method of Preparation Characterization of Microspheres. Application of Microspheres
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-: Introduction : Microspheres are solid , approximately spherical particles ranging 1-1000m 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, Visit www.bpharmstuf.com 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 Visit www.bpharmstuf.com
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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 Extraction
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A) Single Emulsion Technique

Aqous solution /suspension of polymer(natural polymer) stirring / sonication dispersion in orgenic phase oil/chcl3 cross linking

Heat denaturation (by adding dispersion To heated oil)

chemical crosslinking (butanol,HCHO,Glutaraldehyde)

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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
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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

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B)Suspension polymerization
Monomer Bioactive material Initiator

Dispersion in water and stebilizer Droplet

Vigorous ,Aggitation Polymerization by Heat

Hardened microspheres Separation&Drying

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3) Emulsion Polymerisation
Monomer/ Bioactive material Aq.Solution of NaOH, Initiator, Surfactant , Stabilizer

Dispersion with vigorous stirring Micellar sol. Of Polymer in aqueous medium Polymarization Microspheres formation

MICROSPHERES
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D)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
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Phase Sepration Coacervation

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E)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 Visit www.bpharmstuf.com 19 solvent are removed by vacuum drying

F)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

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Solvent extraction apparatusS

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Characterization of Microspheres
 Partical size & shape  Surface chemistry by Electron Spectroscopy
The Surface chemistry of microspheres can be determine using the analaysis It provide a mens of electron spectroscopy for chemical

determination of atomic composition of the surface.

 Release study
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 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 Microspheres
 Microspheres in Vaccine delivery  Targeting of Drug  Magnetic Microspheres  Immunomicrospheres  Microsponges: Topical Porous Microspheres  Imaging  Surface modifide Microspheres
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REFERENCES
http://www.daviddarling.info/encyclopedia/M /microsphere.html www.rsc.org/chemistryworld/News/2010/.../2 2071001.asp www.physorg.com/news187971041.htm REZA ARSHADY- MICROSPHERES MICROCAPSULES &LIPOSOMES

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