Polymers Used In Pharmaceuticals: A Brief Review

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ISSN 2395-3411Available online at www.ijpacr.com233Review ArticlePolymers Used in Pharmaceuticals: A Brief ReviewPawar Dipali Sanjay*, Patrekar Prasad Vasantrao,Dhanawade Pooja Pandit, Dongare Sujata Dattaprasad and Mali Savita ShivajiDepartment of Pharmaceutics, Adarsh Institute of Pharmacy, Vita, Maharashtra, India.ABSTRACTPolymer have played indispensable roles in the preparation of pharmaceutical products.their applications rangewidely from material packaging to fabrication of the most sophisticated drug delivery devices. This review includesvarious polymers used in pharmaceutics based on their applications. The review focused on the use ofpharmaceutical polymers for controlled drug delivery applications. Advances in polymer science have led to thedevelopment of several novel drug delivery system. The review provides the overview of the mechanism of polymer,properties, characterization of polymer and future of polymer technology which should be considered are involved.Keywords: Classification of polymer, Biodegradable and non-biodegradable polymer, Physical properties.INTRODUCTIONDefinition of polymer“Polymers are long chain organic moleculesassembled from many smaller moleculescalled as monomer.‖ The polymer have been synthesized forspecific need and to solve problemsrelated with development of drug deliverysystem. Polymers have been mainly used tocontrol the drug release rate from theformulations. They are also used as taste maskingagent, stabilizer and protective agent inoral drug delivery. Polymers can bind the particles of a soliddosage form and also change the flowproperties of a liquid dosage form. Polymers are macromolecules havingvery large chains contain a variety offunctional groups, can be blended withother low and high molecular weightmaterial. Polymers are mostly applied in drugdelivery because they have uniqueproperties which have not been attainedby any other material.On the basis of surface and bulk propertiespolymers are have some application1) Indevelopmentofdrugdelivery/targeting technique toimprove the efficiency of drugtherapy.2) In development of new technologyin polymer based encapsulationand controlled drug releasesystem.3) To minimize side effect in medicaltreatment.4) In pharmaceutical field polymerused as binder, emulsifying agent,thickening agent etc.5) Polymer also used as film coatingto masking the unpleasant taste toenhance drug stability and inprotection and packaging.1,2CLASSIFICATION OF THE POLYMERA. Based on origina) Natural polymer Naturalpolymersarethesubstances which are obtained bynatural sources like plant and animalsources. Proteins, enzymes, muscle fibers,polymer polysaccharide, gummyexudates are the natural polymerswhich are used in formulatingpharmaceutical products. The well-known natural polymersarechitosan,carrageenan,isapghula, acacia, gelatin, agar,shellac, guar gum. The specific application of plantderived polymer in pharmaceuticalformulations include their use in themanufacture of solid monolithicmatrix systems, implants, andinjectable system as well as viscousliquid formulations. E.g.Proteins-collagen, keratin,albumin.International Journal of Pharma And Chemical Research I Volume 2 I Issue 4 I Oct – Dec I 2016

ISSN 2395-3411Available online at www.ijpacr.comCarbohydrates-starch,cellulose, glycogen.1Collageno Collagen is a major natural proteincomponent in mammals that isfabricatedfromglycine-proline(hydroxy) proline.o Collagen has been widely used inpharmaceutical applications due tothe fulfillment of many requirementsof a drug delivery system such asgoodbiocompatibility,lowantigenicity, and degradability uponimplantation.o Collagen gels are one of the firstnatural polymers to be used as apromising matrix for drug deliveryand tissue engineering.Fig. 1b) Synthetic polymer Synthetic polymers are industriallyproducedchemicalsubstancesconsisting of a number of moleculeslinked together with covalent bond. A wide variety of synthetic polymersare available with variation in mainchain as well as side chain. The most commonly used syntheticpolymerarepolytheneandpolystyrene. E.g.polyester,polyanhydrides,polyamides, polyglycolic acid.Polyglycolic acid (PGA) PGA is commonly obtained by ringopening polymerization of the cyclicdiester of glycolic acid, glycolide. PGA is a hard, tough, crystallinepolymer with a melting temperature of.225 C and a glass transitiontemperature, Tg, of 36 C. PGA has excellent fiber-formingproperties and was commercially234Exampleo The combination of liposomes andcollagen-based technologies hasBeen used.o In this case, drugs and otherbioactiveagentswerefirstlyencapsulated in the liposomes andthen embedded inside a depotcomposedofcollagen-basedsystems, including scaffolds andgels.o The combination of these twotechnologies (i.e., liposomes andcollagen-basedsystem)hasimproved storage stability, prolongedthe drug release rate, and increasedthe therapeutic efficacy.introduced in 1970 as the firstsynthetic absorbable suture under thetrade name Dexon . The low solubility and high meltingpoint of PGA limits its use for drugdelivery applications, since it cannotbe made into films, rods, capsules, ormicrospheres using solvent or melttechniques.b) Based on Bio-stability4Bio-degradable Polymers A bio-degradable polymer is apolymerinwhichthedegradation results from theaction of naturally occurringmicroorganismssuchasbacteria, fungi. Biodegradable polymers arehighlydesirableintheirconditions as they degrade inthe body to biologically inertand compatible molecules.International Journal of Pharma And Chemical Research I Volume 2 I Issue 4 I Oct – Dec I 2016

ISSN 2395-3411 Available online at www.ijpacr.comThesepolymerpolyester,carbohydrates, etc. includesproteins, Alginate Alginate also serves as anexample of a naturally occurringlinear polysaccharide.Alginate are widely used by manypharmaceutical scientist for drugdelivery due to its many uniquepropertiessuchasbiocompatibility, biodegradability,low toxicity, non-immunogenicity,water solubility, relatively lowcost, gelling ability, stabilizingproperties, and high viscosity inaqueous solutions.The cross linking methodologywasconductedatroomtemperature and physiologicalpH.The alginate based systems havebeen successfully used as amatrix for the encapsulation ofstem cells and for controlledrelease of proteins, genes, anddrugs.4Non-biodegradable polymer This polymers are used inpharmaceutical formulation toincrease the therapeutic efficacyof drug. This polymers is now days used indrug delivery system and tissueengineering.Followingarethenonbiodegradable polymers used inpharmaceutical formulationE.g. ethyl cellulose, HPMC, acrylicpolymer, poly (ethylene glycol).Polyethylene glycol (PEG) Polyethyleneglycolissynthesized by the interaction ofethylene oxide with water,ethylene glycol or ethylene glycololigomers. PEG is suitable for biologicalapplications because it is solublein water and has low intrinsictoxicity. The high hydrophilic nature ofPEG enhance the solubility ofhydrophobic drug or carrierswhen conjugated with them. It enhances the physical andchemical stability of drug andprevents aggregation of thedrugs in vivo as well as duringstorage. PEG helps in reducing theaggregation of red blood cell andalsoimprovethebloodcompatibility of PEG copolymersthatareimplantedascardiovascular devices such asstents. It is mainly used in storage cally cross linked hydrogels have been formed fromPEG.Some linear polymers used in pharmaceuticalsRepeating monomer unitPolyolefin-(-CH2—CH-) CH3-(-CH2—CH-) s and polyvinylidenics-(-CH2—CHCl-)-(-CH 2—CH-) 2-)-2353Chemical lybutadienepolyethylenePBPE(HDPE &LDPE)Poly(vinyl chloride)PVPPoly(vinyl acetate)PVAcPoly (vinyl alcohol)Poly(vinylidene national Journal of Pharma And Chemical Research I Volume 2 I Issue 4 I Oct – Dec I 2016

ISSN 2395-3411Available online at www.ijpacr.comPhysical properties that contribute to therate of biodegradation of polymer Water permeability and water solubilityA reflection of the free volume of the polymerand its hydrophilicity will determine the rate ofhydrolysis and whether bulk or surfacehydrolytic degradation occurs. Crystallinity of the polymerOnly the amorphous phase of the polymer isaccessible to permeates (i.e. water drug) andto enzymatic attack. Glass-transition temperatureThe glassy or rubbery nature of the polymerwill be reflected in its permeability andmolecular chain mobility. The chain mobilityappears to be an important factor indetermining the susceptibility to enzymaticattack. Physical dimensions(E.g. size and surface-to-volume ratio) theseappear to become significant in the advancedstages on biodegradation, when phagocytosismay come into play.2Need of biodegradable polymers Non-biodegradable polymers are costly,invasive because require surgical removalafter completion of drug release and maycause tissue toxicity if retained for longertime. While diffusion controlled release is anexcellent means of achieving controlleddrug delivery, it is limited by the polymerpermeability and the characteristics of adrug increase, its diffusion coefficientdecreases. Biodegradable polymers do not need asecond surgery for removal of polymer asit undergoes auto-biodegradation.2363Characterization of polymer In general, polymers for biomedical andpharmaceuticalapplicationsarecharacterized in order to determine theirmolecular weight, composition andthermal properties. All of thesecharacteristics may influence theproperties of the final device ormedicine. Characterization technique is mostlyused to determine molecular mass,molecular structure, morphology andmechanical properties. The molecular weight of polymers canvary from a few hundred to severalmillion gram per mole, while cross linkedpolymers have infinite molecular weight. Polymers obtained from chemicalsynthesisformafamilyofmacromolecular species characterizedby a mean molecular weight with �. This effects adds heterogeneity tochemically synthesized copolymers, andthe only way to appreciate this effect isto analyze the composition of thepolymers at low conversion degreeduring polymer synthesis.6Characteristics of an ideal polymer It should be inert and compatible withthe environment. It should be non- toxic andphysiologically inert. It should be easily administrable. It should be easy to fabricate and mustbe inexpensive. It should have good mechanicalstrength. It must have compatibility with most ofthe drugs. It must not adversely affect the rate ofrelease of the drug. It must not have tendency to retain intissue and must be a goodbiodegradable material.Characterization technique used to study polymer ameterType of polymerGPCMolecular weightPDLADSCThermal changesPLGATGAThermal changesPDLAIRChanges inconcentration ofterminal tcomeMolecular weight decreaseas the degradationproceeds.Tg decreases asdegradation proceeds.Above Tg, polymerdegradation fasterHydrolytic degration rateconstant determined by acidcatalysis reaction.International Journal of Pharma And Chemical Research I Volume 2 I Issue 4 I Oct – Dec I 2016

ISSN 2395-3411Available online at www.ijpacr.comFT-IRAbsorbance peakPolyesterSEMSurfacecharacterizationCopolymer of sebacic acidand carboxy phenoxypropaneNMRMolar fraction ofmonomer and degreein ion ofmonomer releaseChemicalcomposition,molecular weightSurface molecularweight and endgroup.1PDLAPDLA AND PLGACopolymer oflactide/caprolactonePLLA237Degradation rate increaseswith increasingpolydispersity.Crystalline region is moreresistant to erosion thanamorphous.Base catalyzed hydrolysisPDLA was by a randomscisson mechanism; whileacid catalyzed is fasterchain scisson.GA degrade faster than LAHydrolytic degradation wasmonitored. Crystallanityincreased with time.Good linearity obtained inthe kinetics study of PLLAdegradation at the surface.Mechanism of drug release from polymer1) Erosion of the polymer surface withconcomitant release of physicallyentrapped drug When glassy (a dry) polymer comesinto contact with water or any othermedium which is thermodynamicallycompatible, it get swallowed anddiffusion takes place.3) Diffusion controlled release of thephysically entrapped drug, with bioabsorption of the polymer delayeduntil after drug deletion. The third approach avoid anyirreproducibility of the bio erosion rateand the difficulty of trying tosynchronize the diffusion and bioerosion process to achieve a specifieddelivery rate. A polymer that is to be used inbiodegradable delivery system must betailored to meet a number ofrequirements, the most important ofwhicharepermeability,biodegradability, and tensile strength. These properties are interdependent tosome degree and modifications of apolymer to optimize one property willhave an effect on the other three. A number of potentially biodegradablepolymer system are used based on theknown Susceptibilityoftheirmonomeranalogues to undergo cleavage undermild hydrolytic conditionsFig. 2FUTURE PROSPECTSo The most exciting opportunities inpolymer drug delivery lie in the arena ofresponsive delivery system, with which itwill be possible to deliver drugs throughimplantable devices in response to ameasured blood level to deliver a drugprecisely to a targeted site.o Much of the development novel materialsin controlled drug delivery is focusing onthe preparation and use of theseresponsive polymers with specificallydesigned microscopic and microscopicstructural and chemical features. suchsystem includes:2) Cleavage of covalent bonds betweenthe polymer and drug, occurring in thepolymer bulk or at the surface,followed by drug diffusion. In these mechanism disruption ofcovalent bond between polymer anddrug. It occurs either in polymer bulk or atthe surface which may lead to drugdiffusion.2International Journal of Pharma And Chemical Research I Volume 2 I Issue 4 I Oct – Dec I 2016

ISSN 2395-3411 Available online at ydrophobic interaction.Block or graft polymerComplexation networks responding viahydrogen or ionic bonding.Dendritesorstarpolymersasnanoparticles for immobilization ofenzymes,drugs,peptidesorotherbiological ingredients.New biodegradable polymers.New blends of hydrocolloids andcarbohydrates –based polymer.Dendrimers provides a platform for theattachement of drug or gene and theirrelease through several mechanism.In any case, the purpose behindcontrolling the drug delivery is to achievemore effective in both under and overdosing therapies.CONCLUSION This review has covered the majorconcern about the natural and syntheticpolymers, their classification, mechanismand various applications. Nowadays, there are few ally. Biodegradable polymers have beenresearched, but polymer based onrenewable sources (especially on starch)are most desirable. Thedrawbackassociatedwithconventional dosage form have beenovercomebyutilizingpolymerssynthesized specifically to solve theproblems. The use of novel polymers not only offersbut also can prove to be harmful becauseof the toxicity and other incompatibilitiesassociated with them. 238Care should be taken to properly selectpolymers while designing a deliverysystem.The ultimate goal is to introduce costeffective, biocompatible, multifunctional,less toxic polymers so that the deliverysystem pass through the various phasesof clinical trials and benefit to the society.It is believed that the advances inpolymer science will revolutionize thedesign, development and performance ofpolymer based drug delivery system.Biodegradable polymers have proventheir potential for the development ofnew, advances and efficient drug deliverysystem.ACKNOWLEDGEMENTI am thankful to Principal Mr. PatrekarP.V. for their support and guidance.REFERENCES1. Jay J and Ronak P. Role ofbiodegradable polymers in drug al research. 2012; 4(4).2. Ankita R, Anil B and Brijesh K. Polymersin a Drug Delivery System-A review.International Journal of PharmaceuticalResearch and Development. 2002; 2(8).3. Denis L, Gilles P and Christin V.Biomedical and Pharmaceutical Polymer.published by Pharmaceutical press.2011: 1-148.4. Omanthanu P and Ramesh P. Polymer inDrug Delivery System. current opinion inchemical biology. 2001: 447-451.5. Denis L, Gilles P and Christin V.Biomedical and Pharmaceutical Polymerpublished by Pharmaceutical press.2011: 1-148.6. www.PHARMATUTOR.ORG.ART-1509.International Journal of Pharma And Chemical Research I Volume 2 I Issue 4 I Oct – Dec I 2016

Polymers Used in Pharmaceuticals: A Brief Review Pawar Dipali Sanjay*, Patrekar Prasad Vasantrao, Dhanawade Pooja Pandit, Dongare Sujata Dattaprasad and Mali Savita Shivaji . The review provides the overview of the mechanism of polymer, properties, characterization of polymer and future of polymer technology which should be considered are .

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