International Journal of PharmTech Research CODEN( USA): IJPRIF ISSN : 0974-4304 ol.1, No.2, pp 179-183 , April-June 2009 Formulation and Evaluation of Carvedilol loaded Eudragit e 100 Nanoparticles Selvakumar Kalimuthu, A. V. Yadav*, Biopharmaceutics Research Group,Department of Biopharmaceutics, Government College of Pharmacy, Karad - 415124, M.S., India. E- mail: [email protected]Abstract:The aim of this work was to prepare Eudragit E 100 Nanoparticles of Carvedilol and to characterize them. Nanoparticles of Carvedilol with Eudragit E 100 were prepared by the Nanoprecipitation method using Polymeric stabilizer Poloxamer 407. Nanoparticles of Carvedilol were obtained with high encapsulation efficiency. The particles were characterized for particle size by photon correlation spectroscopy and transmission electron microscopy. The in vitro release studies were carried out by USP Type II apparatus in SGF without enzyme (pH 1.2).The particle size of the prepared nanoparticles ranged from 190 nm – 270 nm. Nanoparicles of Carvedilol were obtained with high encapsulation efficiency (85-91%). The drug release from the carvedilol nanoparticles showed within 5 minutes. These studies suggest that the feasibility of formulating carvedilol – loaded Eudragit E 100 nanoparticles for the treatment of hypertension. Keywords:Carvedilol, Nanoparticles, Particle size, Zeta potential, TEM, in vitro release studies. Introduction: Carvedilol is a nonselective -adrenergic blocking agent with α 1 -blocking activity. Carvedilol is (2 RS)-1-(9H-Carbazol-4yloxy)-3-[[2-(2- methoxy phenoxy)ethyl]amino] propan-2-ol. (Fig.1). Figure .1 Chemical structure of Carvedilol It antagonizes the actions of catecholamine more potently at β receptors than at α receptors. It is β 1 and β 2 blocker; α 1 -blocker. It is a racemic mixture in which non cardio selective β-adrenergic receptor blocking activity is present in the S(-) enantiomer and selective α 1 -adrenergic receptor blocking activity is present in both R(+) and S(-) enantiomers at equal potency. In higher concentrations it blocks the entry of Ca ++ into the vascular smooth muscle. It also has antioxidant activity. The ratio of α 1 - to β adrenergic receptor antagonist potency for carvedilol is 1:10. Carvedilol is a lipid soluble compound, practically insoluble in water and poorly absorbed from the gastrointestinal tract. The slow absorption of Carvedilol was attributed to its poor water solubility. It has absolute bioavailability 25-35%. Therefore Nanotechnology can be used to improve the bioavailability of Carvedilol by improving the dissolution characteristics and other physico-chemical characterization. Nanoparticles are one of the multiparticulate delivery systems and are prepared to improve bioavailability or stability and to target drug to specific sites. Nanoparticles can also offer advantages like limiting fluctuation within therapeutic range, reducing side effects, decreasing dosing frequency, and improving patient compliance 1 . Haznder and Dortune reported controlled release Eudragit microspheres of acetazolamide 2 , whereas Dai et al studied Eudragit Nanoparticles as a carrier for enhancing oral bioavailability of cyclosporine 3 . Tzu-Hui Wu et al reported novel quercetin nanoparticles system prepared by a simple nanoprecipitation technology with Eudragit E (EE) and polyvinylalcohol as carriers 4 . Bingbing Jiang, Ling Hu, Changyou Gao et al. developed a co-precipitation method to fabricate nano-scale core- shell particles of ibuprofen stabilized by DEAE dextran 5 . O.Kayser, et al. were developed Formulation of amphotericin B as nanosuspension for oral
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International Journal of PharmTech Research CODEN( USA): IJPRIF ISSN : 0974-4304 ol.1, No.2, pp 179-183 , April-June 2009
Formulation and Evaluation of Carvedilol loaded
Eudragit e 100 Nanoparticles
Selvakumar Kalimuthu, A. V. Yadav*,
Biopharmaceutics Research Group,Department of Biopharmaceutics, Government