DESIGN AND EVALUATION OF MICROSPHERES LOADED WITH REBAMIPIDE

In this present research study, we sought to develop novel Rebamipide microspheres and explore the influence of various concentrations of sodium alginate (polymer) and calcium chloride (cross-linking agent) on particle size, entrapment efficiency, and drug release of the same. These microspheres were prepared by ionotropic gelation technique for oral delivery in the treatment of gastro duodenal ulcers. The formulated microspheres were evaluated regarding size, shape, % EE, % yield, drug release and characterization was studied using FTIR, DSC, SEM analysis. Among the total S14 formulations, S7 formulation was optimized at 2.2% of sodium alginate, 7% of calcium chloride maintained 500rpm, for 2h at room temperature. The in vitro dissolution showed sustained release of Rebamipide upto 96.12% by diffusion mechanism over 12h, which followed the zero order and Korsmeyer-Peppas model (R2 = 0.987, 0.993), respectively. The marketed product displayed the drug release of 95.15% within 1h. The optimized S7 formulation displayed the %EE 95.30, particle size 73.45±0.09 µm, % yield 96.30 and swelling index 95.26%. The optimized S7 formulation subjected to stability studies for 6months as per ICH guidelines, and concluded that significant difference was not observed for % yield, %EE, and drug release before and after stability studies, hence the formulation (S7) found stable. Finally, the prepared Rebamipide microspheres showed significant effect on gastritis in a controlled manner for prolonged period of time. Key words: Rebamipide, microspheres, ionotropic gelation method, DSC, sustained release.