Development and Characterization of Floating Microspheres based Drug Delivery System for Effective Management of Peptic Ulcer

Abstract

Objective: The purpose of present study to develop Gastro-retentive drug delivery formulation for enhancing GRT including the physiological and formulation variables affecting gastric retention. It is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly . Method: Floating microspheres were prepared by Solvent evaporation (oil-in water emulsion) technique. In this 225mg polymethyl methacrylate (PMMA) were dissolved in a mixture of dimethyl formamide and dichloromethane (1:1) at room temperature. And 75mg Nizatidine hydrochloride was added in the above mixture. This was poured into 250 ml water containing 0.02% tween 80, maintained at a temperature 30-40oC and subsequent stirred at ranging agitation speed for 20 minute to allow the volatile solvent to evaporate. The microspheres formed were filtered, washed with water and dried in vaccum. newlineResult: The prepared Floating microspheres were characterized in different way like size distribution 131.4and#61617;1.6and#956;m and 89.5and#61617;1.4% entrapment efficiency was found, Invitro floating test of optimized floating microspheres formulation was studied in SGF (pH 1.2). The percent Cumulative amount of drug release was found 87.2and#61617;2.6% in SGF (pH 1.2), 90.2and#61617;3.5% in SIF (pH 6.8) and 93.2and#61617;3.5 % in PBS (pH 7.4) upto 24 hrs. The ulcer protection of the microspheres formulation were 79.84% as compared to the Nizatidine pure drug (66.05%) in ulcer induced rats. The C-max value of Nizatidine as obtained from the graph was 575.14±55.43 ng/ml with T-max value 2h and for formulation was 206.58 ± 7.71 ng/ml. newlineConclusion: Floating microspheres drug delivery system provides the possibility of enhancing the bioavailability and control the release of formulation exhibiting absorption window by prolonging the gastric emptying time of the dosage form ensuring availability of drug at the absorption site for the desired period of time. newlineKeywords: Floating drug delivery systems, Gastric residence time, in vitro and in vivo.