PREPARATION AND CHARACTERIZATION OF NITRENDIPINE LOADED GRAFTED COPOLYMER MICROSPHERES: A PRELIMINARY STUDY
DOI:
https://doi.org/10.22159/ajpcr.2018.v11i9.23733Keywords:
Nitrendipine, Chitosan, Microspheres, Graft copolymerizationAbstract
Objectives: Developing countries like India suffers mostly from cardiovascular problems and kidney failure. An antihypertensive drug is mainly used to avoid the cardiovascular problems and kidney failure. Nitrendipine is a calcium antagonist widely used in the treatment of hypertension. The bioavailability of drug, when administered orally, is low. Sustained drug delivery systems are using microspheres emerging as an effective method to increase the bioavailability of the drug. The current work involves the encapsulation of nitrendipine - acrylamide grafted chitosan which helps to overcome poor solubility and hydrophobic nature of the nitrendipine. This will enhance the drug dissolution and reduce the side effects of the antihypertensive drug.
Methods: By emulsion cross-linking method, grafted copolymers were prepared. The physicochemical interactions between the drug and grafted copolymer were analyzed by scanning electron microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC).
Results: Encapsulated drug and grafted copolymer were characterized by FTIR to understand the chemical interactions and to identify the functional groups present. Morphology and particle size of the grafted copolymer with drug and without drug were assessed by SEM. DSC was used to identify the melting endotherms of a drug, copolymer cross-linked microspheres, and drug encapsulated microspheres.
Conclusion: Thus, the drug encapsulated grafted copolymer increases the hydrophilic character and thereby making the polymers feasible for functioning as drug carriers for sustained drug delivery system.
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Jarari N, Rao N, Peela JR, Ellafi KA, Shakila S, Said AR, et al. A review on prescribing patterns of antihypertensive drugs. Clin Hypertens 2015;22:7.
Law MR, Morris JK, Wald NJ. Use of blood pressure lowering drugs in the prevention of cardiovascular disease: Meta-analysis of 147 randomised trials in the context of expectations from prospective epidemiological studies. BMJ 2009;338:b1665-b1665.
Wald DS, Law M, Morris JK, Bestwick JP, Wald NJ. Combination therapy versus monotherapy in reducing blood pressure: Meta-analysis on 11,000 participants from 42 trials. Am J Med 2009;122:290-300.
Reddy LC, Reddy RS, Rao KK, Subha MC, Rao CK. Development of polymeric blend microspheres from chitosan-hydroxypropylmethyl cellulose for controlled release of an anti-cancer drug. J Korean Chem Soc 2013;57:439-46.
Siddiqui MA, Plosker GL. Fixed-dose combination enalapril/ nitrendipine a review of its use in mild-to-moderate hypertension. Drugs 2004;64:1135-48.
Banker GS, Rhodes CT. Modern Pharmaceutics. 3rd ed. New York: M. Dekker Publishers; 1996.
Sreekumaran AN, Vidhya KM, Saranya TR, Sreelakshmy KR, Nair SC. Mucoadhesive buccal patch of Cefixime trihydrate using biodegradable natural polymer. Int J Pharm Pharm Sci 2014;6:366-71.
Nair SC, Anoop KR. Local antimicrobial delivery of satranidazole loaded cross linked periodontal chips using bio degradable polymers. Int J Pharm Pharm Sci 2013;5:839-47.
Soppimath KS, Kulkarni AR, Aminabhavi TM. Chemically modified polyacrylamide-g-guar gum-based crosslinked anionic microgels as pH-sensitive drug delivery systems: Preparation and characterization. J Control Release 2001;75:331-45.
Agnihotri SA, Mallikarjuna NN, Aminabhavi TM. Recent advances on chitosan-based micro- and nanoparticles in drug delivery. J Control Release 2004;100:5-28.
Li K, Wang Y, Huang M, Yan H, Yang H, Xiao S, et al. Preparation of chitosan-graft-polyacrylamide magnetic composite microspheres for enhanced selective removal of mercury ions from water. J Colloid Interface Scic 2015;455:261-70.
Pathania D, Gupta D, Agarwal S, Asif M, Gupta VK. Fabrication of chitosan-g-poly(acrylamide)/CuS nanocomposite for controlled drug delivery and antibacterial activity. Mater Sci Eng C 2016;64:428-35.
Phadke KV, Manjeshwar LS, Aminabhavi TM. Novel pH-sensitive blend microspheres for controlled release of nifedipine - An antihypertensive drug. Int J Biol Macromol 2015;75:505-14.
Ramesh K, Krishnapriya M, Paul A, Nair SC. Preparation and evaluation of chitosan sodium alginate carbamazepine microspheres. Asian J Pharm Clin Res 2017;10:5-10.
Basu SK, Adhiyaman R. Preparation and characterization of nitrendipine-loaded eudragit RL 100 microspheres prepared by an emulsion-solvent evaporation method. Trop J Pharm Res 2008;7:1033 41.
Yang MS, De CF, You BG, Fan YL, Wang L, Yue P, et al. Preparation of sustained-release nitrendipine microspheres with eudragit RS and aerosil using quasi-emulsion solvent diffusion method. Int J Pharm 2003;259:103-13.
Yang M, Cui F, You B, You J, Wang L, Zhang L, et al. A novel pH-dependent gradient-release delivery system for nitrendipine: I. Manufacturing, evaluation in vitro and bioavailability in healthy dogs. J Control Release 2004;98:219-29.
Angadi SC, Manjeshwar LS, Aminabhavi TM. Interpenetrating polymer network blend microspheres of chitosan and hydroxyethyl cellulose for controlled release of isoniazid. Int J Biol Macromol 2010;47:171-9.
Rokhade AP, Shelke NB, Patil SA, Aminabhavi TM. Novel interpenetrating polymer network microspheres of chitosan and methylcellulose for controlled release of theophylline. Carbohydr Polym 2007;69:678-87.
Fude C, Mingshi Y, Yanyan J, Dongmei C, Wenhui L, Yuling F, et al. Design of sustained-release nitrendipine microspheres having solid dispersion structure by quasi-emulsion solvent diffusion method. J Control Release 2003;91:375-84.
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