DESIGN, DEVELOPMENT AND EVALUATION OF VILDAGLIPTIN LOADED CROSSLINKED SODIUM ALGINATE AND MORINGA GUM MICROSPHERES BY IONOTROPIC GELATION METHOD AND IN SILICO STUDY USING PK-SIM SOFTWARE

Objective: Vildagliptin, a widely used antidiabetic agent, requires multiple daily doses, which can compromise patient adherence. This study aimed to design, optimize, and evaluate sustained-release microspheres of Vildagliptin using sodium alginate and Moringa gum prepared by ionotropic gelation, with a focus on improving entrapment efficiency, swelling behavior, and controlled drug release. In addition, physiologically based pharmacokinetic (PBPK) modeling was performed to predict in vivo performance. Methods: Microspheres were formulated using varying ratios of sodium alginate and Moringa gum. The polymers were dissolved in water at 50°C, followed by the incorporation of 100 mg of Vildagliptin. The mixture was dropped into barium chloride solutions of different concentrations to induce cross-linking, producing nine formulations. Formed microspheres were cured for 15 min, washed, and air-dried. All batches were evaluated for particle size, entrapment efficiency, swelling index, and in vitro drug-release behavior. Drug-release kinetics were analyzed using mathematical models, and PBPK simulations were conducted to assess predicted pharmacokinetic performance. Results: Among the nine formulations, F7 exhibited the most desirable characteristics with the highest entrapment efficiency (31.39%), a swelling index of 88, and controlled drug release reaching 95% within 4 h. Kinetic studies showed that most batches followed the Korsmeyer-Peppas model, indicating diffusion-controlled sustained release. PBPK modeling further demonstrated that F7 provided prolonged therapeutic plasma levels compared to immediate-release patterns. Conclusion: The study successfully developed sustained-release Vildagliptin microspheres using Moringa gum and barium chloride. Formulation F7 showed optimized entrapment, swelling capacity, and sustained-release performance, suggesting its potential to reduce dosing frequency and enhance patient compliance in diabetes management.