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Biodegradable polymer in drug delivery

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Biodegradable polymer in drug delivery

  1. 1. Biodegradable polymers in drug delivery system Presented By Guided By MS. KRUTIKA H. PARDESHI MR.A.D.SAVKARE M.Pharm(Pharmaceutics) (Assistant professor) Sem -I, Roll no. 37 NDMVP SAMAJ’S COLLEGE OF PHARMACY, NASHIK M.Pharm Semester I -seminar
  2. 2. CONTENT • Introduction to Polymers • Classification of polymers • Biodegradable polymers - Definition - Classification - Examples - Mechanism of action - Need of biodegradable polymer - Advantages and disadvantages - Applications • Chitosan as a polymer - Introduction - Chemistry - Applications • conclusion • References 2
  3. 3. • Polymers • Polymer means -“many parts” • Definition – “Polymer is a substance of high molar mass that is composed of repeating structural units” Example – Ethyl cellulose Carboxy-methyl cellulose Poly (vinyl alcohol) Polyethylene etc. 3 Ethylene Polyethylene
  4. 4. • Classification 4
  5. 5. 5 • Natural polymers obtained from natural plants, animal, microbial sources.eg. Cotton, Silk, Wool. • Semi synthetic and synthetic obtained from synthetic route of polymerization.eg. PE,PVC. 1. Based on origin of source • Linear • Branched • cross-linked 2. Based on structure 3. Based on molecular forces 4. Based on mode of polymerization
  6. 6. • Biodegradablepolymers 6 • Polymers that are degradable in vivo, either enzymatically or non enzymatically, to produce biocompatible or nontoxic by-products. • By products are metabolized and removed from the body via normal metabolic pathways. • Example- 1.poly vinyl alcohol 2. poly lactic acid 3. poly glycolic acid 4. pectin 5. collagen 6. starch etc.
  7. 7. • Classification 7
  8. 8. 1. Agroresources 8 • POLYSACCHARIDE :- • Most abundant complex carbohydrate. • Structural element- glycosidic bond • Example- starch, chitin, chitosan , pectin, etc. • PROTEIN :- • Renewable resources produce by animal, plant, bacteria. • Example- soya protein, casein, collagen, chymotrypsin.
  9. 9. 2. From micro-organisms POLYHYDROXY ALKONATE (PHA) POLYHYDROXY BUTYRATE (PHB) -Some organisms accumulate PHA from 30% to 80% of their cellular dry weight. -The general formula of the monomer unit is -[O-CH(R)-CH2-CO]- -Mechanical properties of PHA : Rigid brittle plastics to flexible plastics. -PHAs are wholly biodegradable. -Biodegradation occurs via linkage break by esterase enzyme. -The R alkyl substituent group is methyl. -PHB is highly crystalline. Its melting temperature is 180 °C. -The pure homopolymer is a brittle material. -PHB is susceptible to thermal degradation at temperatures in the region of the melting point -PHB is degraded by numerous microorganisms (bacteria, fungi and algae) -The hydrolytic degradation yields to the formation of 3-hydroxy butyric acid, which is normal constituent of blood. 9
  10. 10. 3. From biotechnologicalsynthesis PGA(POLYGLYCOLIDE) • PGA is the simplest linear aliphatic polyester. It is prepared by ring opening polymerization of a cyclic lactone, glycolide. • It is highly crystalline, and thus is not soluble in most organic solvents. It has a high melting point (220-225 °C) • PGA has excellent mechanical properties. • Its biomedical applications are limited by its low solubility and its high rate of degradation yielding acidic products. 10
  11. 11. PLA(POLYLACTIDE) • PLA , a cyclic dimer of lactic acid, is usually obtained from polycondensation of D- or L-lactic acid or from ring opening polymerization of lactide. • Two optical forms exist: D-lactide and L-lactide(natural), and synthetic blend is DL-lactide. • PLA is a hydrophobic polymer due to the presence of –CH3 side groups • PLA has disadvantages of brittleness and poor thermal stability. • PLA can be plasticized with citrate ester or low molecular polyethylene glycol to improve the chain mobility and to favour its crystallization. 11
  12. 12. • Synthetic route :- i) ring opening polymerization :- high molecular weight PLAs with better mechanical properties obtained. ii) solid state polymerization iii)solution polymerization or chain extension. • The biodegradability of PLA can enhanced by graft copolymerization of L-lactide onto chitosan using ring opening polymerization and tin as a catalyst. 12
  13. 13. 4. Conventionalsynthesisfrom oil products POLYCAPROLACTONE(PCL) • A semi-crystalline linear polymer obtained from ring-opening polymerization of ε-caprolactone in presence of tin octoate catalyst. • PCL is soluble in a wide range of solvents. • its melting point is 60 – 65 °C. PCL is a semi-rigid material at room temperature. • Enzymes and fungi easily biodegrade PCL. To improve the degradation rate, several copolymers with lactide or glycolide have been prepared . 13
  14. 14. POLY-ESTER AMIDES • Copolymers with amide and ester groups are found to be readily degraded. • The rate of degradation increases with increasing ester content. • Aliphatic poly(ester-amide)s have been synthesized from 1.6 - hexanediol, glycine and di-acids with a various number of methylene groups varying from 2 to 8. • All these polymers are highly crystalline. 14
  15. 15. • Mechanismofdrugreleasefrombiodegradablepolymer 15 COMBINATIONHYDROLYSIS BULK EROSION SURFACE EROSION ENZYMATIC
  16. 16. • BIOEROSION 16 1) Bulk erosion - Degradation takes place throughout the whole of the sample. - Ingress of water is faster than the rate of degradation E.g. : Polylactic acid (PLA) Polyglycolic acid (PGA) 2) Surface erosion -Sample is eroded from the surface. -Mass loss is faster than the ingress of water into the bulk E.g.: Polyanhydrides polyorthoester
  17. 17. • RELEASEOFDRUGFROMSRTABLET USING HYDROPHILLICMETRIXFORMINGPOLYMER 17
  18. 18. • NEED OFBIODEGRADABLEPOLYMER 1) Achieving controlled drug delivery. 2) No need for a second surgery for removal of Polymers. 18
  19. 19. • ADVANTAGES& DISADVANTAGES • ADVANTAGES • DISADVANTAGES • Localized delivery of drug • Sustained delivery of drug • Stabilization of drug • Decrease in dosing frequency • Reduce side effects • Improved patient compliance • Presence of substances that may be issued in the body [monomers (toxic), catalysts, additives] after Degradation • A “burst effect” or high initial drug release soon after administration is typical of most system. 19
  20. 20. • APPLICATIONS • Polymer system for gene therapy. • Biodegradable polymer for ocular, tissue engineering, vascular, orthopedic, skin adhesive & surgical glues. • Bio degradable drug system for therapeutic agents such as anti tumor, antipsychotic agent, anti-inflammatory agent. • Polymeric materials are used in and on soil to improve aeration, and promote plant growth and health. • Many biomaterials, especially heart valve replacements and blood vessels, are made of polymers like Dacron, Teflon and polyurethane. 20
  21. 21. POLYMER APPLICATION • Collagen In wound repairing • Chitosan Gelling agent • Dextran Plasma volume expander • Lectins As a mucoadhesive • Cyclodextrins, guar gum, pectin, insulin Delivery of drug to colon • Rosin As an adhesive in TDDS 21
  22. 22. CHITOSAN AS A POLYMER 22
  23. 23. • INTRODUCTION • Chitosan is a natural cationic biopolymer consequent commencing the hydrolysis of chitin. • Obtained from ecologically sound natural sources, namely crab and shrimp shell wastes. • Together with chitin, Chitosan is well thought-out the second most profuse polysaccharide subsequent to cellulose. • Chitosan is derived by the alkaline deacetylation of chitin • Chitin is an amino polysaccharide (combination of sugar and protein). 23
  24. 24. • CHEMISTRY • Chitosan is chemically (Poly[-(1, 4)-2-amino-2-deoxy-D- glucopiranose]) • Chitosan isolated from shells of shrimp, crab and lobster by treating the shells with 2.5 N NaOH at 750°C and with 1.7 N HCl at room temperature for 6 hours • The polymer differs from chitin in that a majority of the N- acetyl groups in Chitosan is hydrolyzed. • The degree of hydrolysis has a significant effect on the solubility and rheological properties of the polymer. 24
  25. 25. • APPLICATIONS • GENERAL PHARMACEUTICAL APPLICATIONS OF CHITOSAN a) Chitosan by itself is haemostatic (stops bleeding), some derivatives such as sulphated Chitosan are anticoagulants. By utilizing the haemostatic effect, Chitosan bandages and sponges we prepared for surgical treatment and wound protection. b) It has a capacity of forming film and has been suggested as a biopolymer of choice for the development of contact lenses (soft and hard contact lenses). 25
  26. 26. c) It has been used for the manufacturing of ocular bandage lenses used a protective device for acutely or chronically traumatized eyes. d) It is also useful as artificial kidney membranes because of their suitable permeability and high tensile strength. e) Used in antacids and antiulcer drugs, wound and burn healing properties, immobilization of enzymes and living cell and in ophthalmology. 26
  27. 27. Amongthepharmaceuticalapplicationsithasbeenused asa: 1. Diluents in direct compression of tablets. 2. Binder in wet granulation 3. Slow-release of drugs from tablets and granules 4. Drug carrier in micro particle systems 5. Films controlling drug release 6. Preparation of hydrogels. 7. Wetting agent And Disintegrant 8. Agent for increasing viscosity in solutions. 9. Bio adhesive polymer 10. Site-specific drug delivery (e.g. to the stomach or colon) 11. Absorption enhancer (e.g. for nasal or oral drug delivery) 12. Carrier in relation to vaccine delivery or gene therapy 27
  28. 28. • Conclusion • Biodegradable polymer are naturally degradable polymer widely use in pharmaceutical formulation. • Biopolymers limit carbon dioxide emissions during creation, and degrade to organic matter after disposal. • Biodegradable polymers have received much more attention in the last decades due their potential applications in the fields related to environmental protection and the maintenance of physical health. 28
  29. 29. • To improve the properties of biodegradable polymers, a lot of methods have been developed, such as block copolymerization or grafting. These methods improve both the biodegradation rate and the mechanical properties of the final products. • Physical blending is another route to prepare biodegradable materials with different morphologies and physical characteristics. • Recently different studies have been reported concerning the use of nanoclay with biodegradable polymers, especially with starch. • Nano-biocomposites or bio-nanocomposites are under investigation. • Bio-polymers hold great promises for formulation development in future. 29
  30. 30. • References 1. N. K. Jain,2005, “Progress in controlled and novel drug delivery systems” CBS Publishers and Distributors , Pg no.11-14. 2. S.P. Vyas, Roop K. Khar, 2002, “Controlled drug delivery : Concept and Advances”, Vallabh Prakashan, Pg.no.97-151. 3. Sangamesh Kumbhar, et.al., 2014, “Natural and synthetic biomedical polymers”, Elsevier publication, Pg.no.280-285. 4. Ashwin Kumar, et.al., 2011, “Biodegradable Polymers and Its Applications” , International Journal of Bioscience, Biochemistry and Bioinformatics, Vol.3,Pg.no.173- 176. 5. Isabelle Vroman and Lan Tighzert,2009, “Biodegradable Polymers”, Science & medicine,Vol.2, Pg.no.307-344. 30
  31. 31. 6. Laxmi S. Nair, et.al., 2007, “Biodegradable polymer as biomaterial”, Science direct, Elsevier publication, Pg.no.762-798. 7. K. Kavitha, et.al., 2011, “Chitosan polymer as carrier in various pharmaceutical formulation : brief review”, International Journal of Applied Biology and Pharmaceutical Technology, Vol.2,Pg.no.249-258. 8. Angelica Diaz, et.al., 2014, “Synthesis, Properties and Applications of Biodegradable Polymers Derived from Diols and Dicarboxylic Acids: From Polyesters to Poly(ester amide)s’”, International Journal of Molecular Sciences, Pg.no.7064-7123. 31
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