Formulation, design and optimization of antidiabetic drug loaded microspheres

The present research aim is to develop the tablet formulation containing microspheres and encapsulating microsphere with antidiabetic drug specially Sitagliptin Phosphate Monohydrate and poly lactic co glycolic acid (PLGA) as a polymer. Preformulation study of the selected drug was carried out. Then, the microspheres were prepared by factorial design, i.e., Design-Expert 12 software (Stat-Ease Inc., USA) was used for designing of experiment, to study interaction between independent variables and dependent variables and deriving optimum formulation. Spray dryer was used for preparation of microspheres. The zeta potential, particle size, infrared spectral analysis, scanning electron microscopy, % drug content, encapsulation efficiency and % drug release were evaluated. Optimized batch F3 showed an average particle size 2500.6 nm. The in vitro drug release at 12th hour and % drug entrapment efficiency of optimized batch F3 was found to be 92.35% and the 34.00%, respectively. The final product has lowered particle size 2500.6 nm and it is focused for well acceptable and suitable due to significant drug release. The final tablet was prepared from optimized batch F3. The precompression parameters, i.e., flow properties of granules, were carried out, and then, post-compression parameters like weight variation, thickness, hardness, friability, % drug content and % drug release were evaluated. The stability study and in vitro antidiabetic study was carried out for tablet. The final product is well acceptable, suitable, palatable, easy for administration and elegant. [GRAPHICS] .