DEVELOPMENT AND CHARACTERIZATION OF MICROBALLONS BASED DRUG DELIVERY SYSTEM OF MESALAMINE HYDROCHLORIDE

Abstract

Objective: An objective of the present investigation was to prepare Eudragit S-100: Eudragit RS-100 microballons of mesalamine hydrochloride and evaluate for their anti-inflammatory activity. Material method: Microballons were prepared by quasi solvent diffusion and evaporation method using different ratios of Eudragit S-100: Eudragit RS-100 (1:1 to 1:4 % w/w), mesalamine hydrochloride (40 to 100% w/w), PVA concentration (0.5 to 1.25 %), stirring speeds (300-500 rpm) and temperature (25^°C, 37 ^°C and 45 ^°C). The yield of preparation and encapsulation efficiency was high for all hollow microballons formulation. Results and Discussion: Microballons prepared by using Eudragit S-100: Eudragit RS-100 ratio 1:2 %w/w, 80:100% w/w) drug concentration, 0.75 % w/v concentration of surfactant (PVA), stirring speed 400 rpm, and temperature 37^°C were selected as an optimized. The optimized microballons formulation were evaluated for their surface morphology, particle size and size distribution, percentage drug entrapment and in vitro mesalamine release in SGF (pH 1.2), and PBS (pH 7.4). The % Cumulative released was found 91.2±3.5% in SGF (pH 1.2) and 89.2±3.5 in PBS (pH 7.4) up to 24 hrs. The data of drug released revealed that the microballons formulation follows a diffusion controlled drug release mechanism. In vivo evaluation of the optimized microballons formulation were carried out in healthy male albino rats by measuring  anti inflammatory activity produced after oral administration of optimized microballons formulation at a dose of (equivalent to 50 mg/kg of mesalamine hydrochloride). The progressive reduction in paw volume was observed till the end of study and maximum upto 0.4 ml after 2 hr. Conclusion : It is concluded from the present investigation that Eudragit S-100: Eudragit RS-100 microballons bearing mesalamine are promising controlled release vector for effective treatment of inflammation.

Keywords: microballons, hollow microspheres, anti-inflammatory activity, mesalamine hydrochloride, solvent diffusion evaporation method.