FORMULATION AND EVALUATION OF ENTACAPONE MICROSPHERES BY IONOTROPIC GELATION TECHNIQUE

Abstract: In this present research study, an attempt was made to develop novel Entacapone microspheres and consider the influence of various concentrations of sodium alginate and calcium chloride 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 "wearing-off" symptoms of Parkinson's disease. The formulated microspheres were evaluated regarding entrapment efficiency, percentage yield, drug release and characterization was studied using FTIR, DSC, SEM analysis. Among the total S14 formulations, S13 formulation was optimized at 2% of sodium alginate, 10% of calcium chloride with pectin. The in vitro dissolution showed sustained release of Entacapone up to 97.89±5.05 by diffusion mechanism over 12h, which followed the zero order and Higuchi model (R2 = 0.982, 0.979) respectively, the drug release from microspheres was anomalous Non fickian diffusion. The marketed product displayed the drug release of 95.12±5.01within 1 hr. From these results it was concluded that, optimized formulation is stable and retained their original properties with minor differences. Entacapone alginate microspheres is an effective drug delivery system that offers more predictable and extensive drug release with enhanced shelf-life in the treatment of acute Parkinsonism. Key Words: Entacapone, Microspheres, Parkinson's disease, Cross-linking agent.