Formulation and Evaluation of Mesalamine Microspheres for Colon Targeted Drug Delivery System
Journal Title: Journal of Pharmacy Research - Year 2011, Vol 4, Issue 6
Abstract
Mesalamine (5-ASA) is an anti-inflammatory drug used in treatment of Crohn’sdisease and ulcerative-colitis. As Mesalamine is rapidly absorbed from the small intestine and it is necessary to develop a colon-specific delivery system for it. In the long-term management of ulcerative colitis patients, repeat dosing maybe required. Since Mesalamine (5-ASA) is largely absorbed from the upper intestine, selective delivery of drugs into the colon may be regarded as a better method of drug delivery with fewer side effects and a higher efficacy. An objective of the present investigation is to prepare and evaluate Mesalamine microspheres for colon targeting. These microspheres were prepared by emulsion solvent evaporation method using different ratios of Mesalamine, Hydroxy propyl methyl cellulose (HPMC) and Ethylcellulose (EC), stirring speed (1000rpm) and emulsifier concentration(0.5%W/ V).Cellulose coated Mesalamine microspheres were evaluated for surface morphology, particle size analysis, percentage drug entrapment, percentage yield and in vitro drug release studies. Drug release studies carried out in acidic medium (0.1NHCl) for 2hr and in phosphate buffer pH 7.4 up to 12hrs. In acidic medium, the release rate was much slower; however, the drug was released quickly at phosphate buffer pH 7.4. Microspheres prepared by using drug: polymer ratio 1:2.5 stirring speed 1000 rpm, and 0.5% wt/vol concentration of tween 80 (emulsifier) were selected as an optimized formulation. It is concluded from the present investigation that Mesalamine microspheres are promising controlled release carriers for colon-targeted drug delivery.
Authors and Affiliations
A. Swapna*1 , Abdul Bari Mohd2 , Vinay Wamorkar3 , P. Swathimutyam
Keywords
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