FORMULATION AND OPTIMIZATION OF BACLOFEN FLOATING MICROSPHERES: A GASTRORETENTIVE DRUG DELIVERY APPROACH
The aim of the present study was to develop and evaluate Baclofen floating microspheres to prolong the gastric residence time of Baclofen, a drug with an absorption window in the upper gastrointestinal tract. The microspheres were prepared using the solvent evaporation technique. The dependent variables studied were particle size (Y1), percentage drug entrapment efficiency (Y2), percentage buoyancy (Y3), in-vitro drug release at 1 hour (Y4), and in-vitro drug release at 6 hours (Y5). A 3² full factorial design was employed to assess the combined effect of two independent variables Eudragit RL100 (X1) and Eudragit RS100 (X2), on the aforementioned responses. Multiple regression analysis revealed that increasing concentrations of Eudragit RL100 and Eudragit RS100 led to a reduction in in-vitro drug release, while enhancing particle size, drug entrapment efficiency, and buoyancy. The optimized formulation consisted of microspheres with an average particle size of 115.96 µm, drug entrapment efficiency of 90.06%, and buoyancy of 90.76%. In-vitro studies demonstrated sustained drug release for up to 24 hours. The floating microspheres were free-flowing, porous, and nearly spherical in shape. Drug release followed Fickian diffusion and best fitted the Higuchi model, as determined by drug release kinetics studies