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Application of Microspheres -: Introduction :- : -: 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. ADVANTAGE OF MICROSPHERES: : 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 POLYMER Used for Microspheres preparation: : POLYMER Used for Microspheres preparation: The administration parameters that can be satisfactorily controlled are as follow: : 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 General Method of Preparation: : 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 A) Single Emulsion Technique : 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) Microspheres in org.phase Microspheres in org.phase Centrifugation,washing,separation Microspheres : Microspheres in org.phase Microspheres in org.phase Centrifugation,washing,separation Microspheres B) Double Emulsion Technique : 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 Separation,washing, dryingMICROSPHERES : Separation,washing, dryingMICROSPHERES C)Polymerization : C)Polymerization A)Normal Polymerization: Normal Polymerization is done by bulk, suspension, pption,emulsion and polymerization process. Bulk polymerization: Monomer Bioactive material Initiator Heated to initiate polymerization Initiator accelerate rate of raction Polymer(Block) Moulded/fragmented MICROSPHERES B)Suspension polymerization : B)Suspension polymerization Monomer Bioactive material Initiator Dispersion in water and stebilizer Droplet Vigorous ,Aggitation Polymerization by Heat Hardened microspheres Separation&Drying MICROSP HERES 3) Emulsion Polymerisation : 3) Emulsion Polymerisation 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 D)Phase Sepration Coacervation : 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 MICROSPHERES E)Spray Drying : 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 solvent are removed by vacuum drying F)Solvent Extraction : 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 Characterization of Microspheres : Characterization 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 Slide 20: 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. Application of Microspheres : Application of Microspheres Microspheres in Vaccine delivery Targeting of Drug Magnetic Microspheres Immunomicrospheres Microsponges: Topical Porous Microspheres Imaging Surface modifide Microspheres Slide 22: THANK YOU You do not have the permission to view this presentation. In order to view it, please contact the author of the presentation.