فهرست نشریات علمی دسترسی آزاد ایران

The current research sought to establish and evaluate a gastro-retentive drug delivery system of Remdesivir-loaded floating microspheres utilizing a 3² factorial design. Microspheres were formulated by the emulsion solvent diffusion method, employing Eudragit L 100 as the primary polymer. Among the nine formulations developed, the optimized batch (OREL) exhibited favourable physicochemical characteristics, including a mean particle size of 0.254 µm, high entrapment efficiency (76.32%), and sustained drug discharge of 81.12% over 12 hours. The microspheres demonstrated good stability with a polydispersity index of 0.245 and a zeta potential of -23.5 mV. Drug release kinetics followed both zero-order and Higuchi models, indicating a diffusion-controlled mechanism. FTIR and DSC analyses confirmed the absence of significant drug excipient interactions, ensuring chemical compatibility. In vivo radiographic studies using barium sulphate (BaSO₄) confirmed gastric retention for over 10 hours. Pharmacokinetic studies showed enhanced oral bioavailability and a prolonged half-life of Remdesivir compared to the unmodified drug. This is the first report on the successful development of floating microspheres for Remdesivir, offering a sustained-release profile and improved therapeutic potential. The system effectively reduces dosing frequency and may enhance patient compliance in antiviral therapy.