Abstract

GLECAPREVIR SUSTAINED RELEASE MUCOADHESIVE MICROSPHERE FORMULATIONS: DEVELOPMENT AND PHARMACEUTICAL CHARACTERIZATION

*Ms. Sagrika Pandey, Dr. Lata Choudhary, Dr. Yogesh Pounikar

Abstract

Background: Conventional drug delivery systems often face limitations such as poor bioavailability and lack of site-specific action. To overcome these challenges, mucoadhesive microspheres have emerged as a promising approach for controlled and targeted drug delivery. The present study aims to develop and evaluate Glecaprevir-loaded mucoadhesive microspheres using spruce gum to enhance drug retention, bioavailability, and sustained release. Methods: Mucoadhesive microspheres were prepared using a cross-linking method with calcium chloride. Pre-formulation studies were conducted using FTIR, DSC, and XRD to assess drug-polymer compatibility. The formulations (F1-F4) were evaluated for production yield, drug loading, entrapment efficiency, particle size, swelling index, and mucoadhesion. Surface morphology was analyzed using SEM, and in vitro drug release studies were performed using a Franz diffusion cell. Results: The prepared microspheres showed a production yield of 40.26-55.93% and drug loading of 49.21-74.60%. Particle size ranged from 14.3-18.3 μm. Swelling (82-91%) and ucoadhesion (45.6-79.6%) increased with polymer concentration. The optimized formulation (F2) exhibited maximum drug release of 98.26% within 300 minutes. FTIR confirmed compatibility, while DSC and XRD indicated conversion of the drug into an amorphous form, enhancing solubility. Discussion: The study demonstrates that polymer concentration plays a crucial role in controlling drug release, swelling behavior, and mucoadhesion. The transformation of Glecaprevir from crystalline to amorphous form improved its dissolution characteristics. The optimized formulation (F2) showed a balanced profile of drug release and mucoadhesion, making it suitable for sustained drug delivery. Conclusion: Glecaprevir-loaded mucoadhesive microspheres were successfully formulated and evaluated. The optimized formulation exhibited desirable physicochemical properties, sustained drug release, and enhanced mucoadhesion. This system can serve as an effective approach for controlled drug delivery and improved therapeutic efficacy.

Keywords: Control Drug Delivery, Glecaprevir, Mucoadhesive Microsphere, Spruce Gum etc.