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Wajhiuddin M.Pharm II nd sem Dept. of Pharmaceutics Govt. college of pharmacy AurangabadSlide 2: 2 CONTENTS: Introduction objective Material(s) used Prerequisites for ideal micro particulate carriers General methods of preparation Loading of Drug Release kinetics Characterization Applications ReferencesSlide 3: 3 Introduction : Microspheres are discrete spherical particles ranging in average particle size from 1 to 50microns. Characteristically free flowing powders consisting of proteins or synthetic polymers which are biodegradable in nature and ideally having a particle size less than 200 μm. Objective The drug should be delivered to specific target sites at a rate and concentration Minimise the side effect Patient compliance during the drug deliverySlide 4: 4 Carrier : one of the most important entities essentially required for successful transportation of the loaded drug(s). Carrier systems used for Targeted DrugDelivery 1. Colloidal carriers a .Vesicular systems E g : Liposome, Niosomes, Virosomes b. Microparticulate systems E g :Microspheres, Nanoparticles 2. Cellular carriers E g: Resealed erythrocytes, antibodies 3. Polymer based system E g: MucoadhesiveSlide 5: 5 Use of carrierSlide 6: 6 Material(s) Polymers used for making microspheres are of two types: 1. Synthetic polymers a. Non-biodegradable polymers e.g . Poly methyl methacrylate (PMMA) Acrolein Glycidyl methacrylate Epoxy polymers b. Biodegradable polymers e.g . Lactides, Glycolides & their co polymers Polyalkyl cyano acrylates Poly anhydridesSlide 7: 7 Material(s) Polymers used for making microspheres are of two types: 1. Synthetic polymers a. Non-biodegradable polymers e.g . Poly methyl methacrylate (PMMA) Acrolein Glycidyl methacrylate Epoxy polymers b.Biodegradable polymers e.g . Lactides, Glycolides & their co polymers Polyalkyl cyano acrylates Poly anhydridesSlide 8: 2. Natural polymers a. Proteins: e.g Albumin, Gelatin, and Collagen b. Carbohydrates: e.g Agarose, Carrageenan, Chitosan, Starch c. Chemically modified carbohydrates: e.g Poly dextran, Poly starch Contd.Slide 9: 9 MICROSPHERESSlide 10: 10 Photograph of Eudragit S-100 coated core microspheres MICROSPHERESSlide 11: 11 Prerequisites for Ideal Microparticulate Carriers Control of content release Increase of therapeutic efficiency Protection of drug Reduction of toxicity Biocompatibility Sterilizability Relative stability Water solubility or dispersability Targetability Longer duration of actionSlide 12: 12 1. Single emulsion technique 2. Double emulsion technique 3. Polymerization techniques 4. Phase separation coacervation technique 5. Spray drying and spray congealing and 6. Solvent extraction Methods Loading of Drug Two methods principally used 1.During the preparation of microspheres 2.After the formation of microspheres by incubating them with the drug and proteinSlide 13: 13 Liberation of drug by polymer erosion or degradation Diffusion through pores 5mg of microspheres were put in a small vial containing 25 mL of buffer, the release medium. The vial was rotated at 60 rpm and, was maintained at 37 ± 0.2°C in a thermostat water bath. The drug content of the release medium was determined using UV spectrophotometry at 281 nm. Drug Release KineticsSlide 14: 14 Physicochemical evaluation/ Characterization : Particle size and shape Density determination Isoelectric point Electron spectroscopy for chemical analysis Attenuated Total reflectance fourier transform-infrared spectroscopy Surface carboxylic acid residue Surface Amino acid residue Release studies Capture efficiency %Entrapment =Actual content/Theoretical content×100 10.Angle of contactSlide 15: Application 1. Microspheres in vaccine delivery 2.Microspheres in Antigen release 3.Monoclonal Antibodies mediated Microspheres 4.Imaging 5.Topical porous microsphers 15Slide 16: 16 NANOPARTICLES Introduction Nanoparticles are defined as particulate dispersions or solid particles with a size in the range of 10-1000nm. Depending upon the method of preparation, nanoparticles, nanospheres or nanocapsules can be obtained. Nanocapsules : Are systems in which the drug is confined to a cavity surrounded by a unique polymer membrane. Nanospheres : Are matrix systems in which the drug is physically and uniformly dispersed.Slide 18: 18 Purpose : To control particle size and Surface properties Release of pharmacologically active agents in order to achieve the site-specific action of the drug Advantages Both passive and active drug targeting can be easily manipulated after parenteral administration They control and sustain release of the drug Reduction in side effectsSlide 19: 19 4. Site-specific targeting can be achieved by attaching targeting ligands 5. various routes of administration like oral, nasal, parenteral ,intra-ocular etc. is possible Disadvantages 1. Small size and large surface area can lead to particle particle aggregation 2. Handling of nanoparticles is difficult in liquid and dry forms 3. Small particles size and large surface area causes limited drug loading and burst release Contd.Slide 20: 20 Methods of Drug deliverySlide 21: 21 Equipments for Nanoparticles 1.Homogenizer 2.Ultra Sonicator 3.Mills 4.Spray Milling 5.Supercritical Fluid Technology 6.Electrospray 7.Ultracentrifugation 8.NanofiltrationSlide 22: Pharmaceutical Aspects of Nanoparticles Purification Freeze drying Sterlizaton Characterization/Evaluation Particle size Charge determination Surface hydrophobicity Carrier-drug interaction Release profile Drug stabilitySlide 23: Applications 1. Nanoparticles for Tumor targeting 2. Nanoparticles for gene delivery 3. For vaccine adjuvant 4. For DNA delivery 5. Used for crosses Blood Brain Barrier 6. Nanoparticles for oral delivery of peptides and proteins 7 .Nanoparticles to epithelial cells in the GI tract using ligands 23Slide 24: 24 Marketed preparation DOXIL Drug target to cancer cellsSlide 25: 25 REFERENCE Vyas, S. P and khar, R.K, Edited Targeted and controlled drug delivery. CBS Publishers and Distributers, New Delhi, 2002, 351. Nanoparticles-Targeting Neurotherapeutic Agents Through The Blood Brain Barrier,Shivakumar H.G, Gowda D.V, Krishna R.S.M, Das. D. www.sciencedirect.com Patel, Priyal. "Nanotechnology." Drug Delivery Technology. 5. Chen Y, Dalwadi G, Benson H. Drug delivery across the blood-brain barrier. Current Drug Delivery 2004; 161-376.Slide 26: 26 You do not have the permission to view this presentation. In order to view it, please contact the author of the presentation.