DEVELOPMENT AND IN VITRO CHARACTERIZATION OF THE EUDRAGIT S100 COATED MICROSPONGE OF BERBERINE HCLFOR TREATMENT OF ULCERATIVE COLITIS

Abstract

Ulcerative colitis (UC) is a chronic, relapsing inflammatory bowel disease affecting the mucosal lining of the colon and rectum, often leading to symptoms such as abdominal pain, diarrhea, and rectal bleeding. Existing pharmacological therapies are associated with limitations including systemic side effects, poor site-specific action, and reduced patient compliance. In recent years, herbal therapies have gained interest due to their safety profile and therapeutic potential. In this study, we developed a colon-targeted drug delivery system utilizing a microsponge-based approach for the effective delivery of Berberine, a natural alkaloid known for its potent anti-inflammatory and antioxidant properties, aimed at improving treatment outcomes in UC. The microsponges were prepared using the quasi-emulsion solvent diffusion method and subsequently coated with Eudragit  S-100, a pH-sensitive polymer, to facilitate site-specific release in the colonic region. The prepared formulations were extensively characterized for particle size, surface morphology, entrapment efficiency, swelling behavior, and in vitro drug release profile under simulated gastrointestinal conditions. Scanning electron microscopy revealed spherical porous microstructures with uniform distribution. The encapsulation efficiency was found to be optimal, and the drug release studies indicated minimal release in the acidic environment (pH 1.2 and 6.8) with a marked increase at pH 7.4, mimicking the colonic environment.

The developed system ensured protection of the drug in the upper gastrointestinal tract and enabled controlled release at the site of inflammation, thereby enhancing therapeutic efficacy while minimizing systemic exposure. This microsponge-based, Eudragit -coated delivery system offers a promising and innovative platform for targeted herbal therapy in ulcerative colitis and may serve as a potential alternative to conventional therapies, improving patient adherence and overall clinical outcomes.