Design, Optimize and Evaluate Dapagliflozin Sustained Release Microspheres using Box-Behnken Design

This study aimed on optimizing dapagliflozin microspheres for sustained release to improve efficacy over the marketed product. Microspheres were formulated by a Solvent Evaporation method involving sodium alginate, ethyl cellulose and HPMC K 100. The process was optimized through Box- Behnken statistical experimental model, adjusting polymer concentration, surfactant amount and rotational speed. Seventeen formulations were formulated and the optimized formulation (F2) was investigated for its micromeritic characteristics, SEM, in-vitro release, kinetic modeling, and stability. FT-IR study showed no negative correlation among the drug and polymers. F2 exhibited maximum yield (81.78%), entrapment efficiency (82.21%) with optimum particle size (278.69 μm). Increased concentration of polymer improved yield and efficiency of drug entrapment while stirring rate decreased particle size. SEM analysis revealed rough, porous and spherical microspheres, and the release was sustained, with 98.02% of the drug released over 20 hours. The optimized microspheres showed prolonged drug release under gastrointestinal conditions, offering increased efficacy and potentially enhancing patient adherence by lowering dosing compared to the marketed product.