Development and Evaluation of an Eudragit-Coated Colon-Targeted Delivery System for Myrica esculenta in Ulcerative Colitis
Monika Joshi, Manju Pandey, Prem Shankar Gupta, Akash Ved, Ravi ShankarBackground:
Ulcerative colitis is a chronic inflammatory disorder of the colon that significantly impacts patients' quality of life. Current therapies often show limited efficacy and cause systemic side effects. Myrica esculenta, with its potent anti-inflammatory and antioxidant properties, presents a promising alternative for targeted treatment.
Objective:
This study aimed to design and evaluate colon-targeted tablets for Myrica esculenta using Eudragit E100 and Eudragit S100, and to assess various pharmaceutical parameters to enhance therapeutic outcomes while minimizing systemic exposure.
Methods:
Myrica esculenta extract was prepared via Soxhlet extraction and characterized using FTIR spectroscopy. CODESTM-based tablets were formulated with Eudragit E100 and E100 for pH-sensitive release, and the formulations were optimized using a central composite design (CCD). In vitro dissolution and in vivo roentgenography studies assessed drug release and colonic targeting.
Results:
The extraction yield of Myrica esculenta was 21.11%, and FTIR confirmed the presence of key bioactive compounds. The drug content across all formulations ranged from 91.59 ± 0.79% to 98.85%. Further in vitro release studies of 13 formulations (D1-D13) showed that the optimized formulation (D5) achieved 96.34% cumulative drug release, with 10% or less drug release in gastric and intestinal conditions. In vivo roentgenography confirmed that the CODESTM-based tablets remained intact through the small intestine and dissolved and released the active at colonic pH, validating the Eudragit-coated delivery system's efficacy.
Discussion:
The optimized CODESTM-based tablet not only achieved controlled release but also demonstrated high drug content uniformity, indicating the feasibility of reproducible manufacturing. In vivo roentgenography further validated the in vitro findings, confirming the integrity of tablets up to the small intestine and their disintegration in the colon. These results establish the suitability of Eudragit E100 and Eudragit S100 as functional polymers for pH-triggered colonic release.
Conclusion:
The developed colon-targeted system for Myrica esculenta effectively addresses the challenge of reaching the colon intact and achieving targeted release in the colonic fluid.