Design and Evaluation of Mesalamine-Loaded Nanospheres for SIte-Specific drug delivery in ulcerative colitis treatment

• Kirti Rathore

  Author

• Anirudh Singh Deora

  Author

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Colon-specific drug delivery systems (CSDDS) have gained significant attention due to their therapeutic advantages in treating local colonic diseases such as inflammatory bowel disease (IBD), ulcerative colitis (UC), Crohn's disease, and colorectal cancer. Conventional drug delivery systems fail to provide targeted release at the colon, leading to systemic side effects and reduced therapeutic efficacy. This study aimed to develop and evaluate colon-targeted nanosphere formulations of mesalamine (5-aminosalicylic acid) using Eudragit RS and Eudragit L polymers for site-specific delivery to the colon. Nanospheres were prepared by the nanoprecipitation method, characterized for particle size, zeta potential, drug entrapment efficiency, morphology, and in-vitro drug release. The nanospheres were subsequently compressed into tablets and coated with cellulose acetate phthalate. Preformulation studies, FTIR compatibility studies, DSC thermal analysis, and XRD were conducted. In-vivo evaluation was performed using DSS-induced colitis model in BALB/c mice. The optimized formulation F2 (Eudragit RS, 500 mg polymer) demonstrated 96% drug entrapment efficiency and released 96.24% drug within 15 hours under simulated colonic conditions. Tablet formulation F3 exhibited maximum drug release of 96.58% at 17 hours. Stability studies at accelerated conditions confirmed formulation stability over three months. In-vivo results showed significant reduction in disease activity index (DAI), CRP, ESR, and WBC levels, with histopathological studies confirming near-complete mucosal recovery. These findings suggest mesalamine nanosphere tablets as a promising colon-targeted drug delivery platform.

Copyright (c) 2026 Kirti Rathore, Anirudh Singh Deora (Author)

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