L-glutamine conjugate of meselamine: a novel approach for targeted delivery to colon

The objective of the present work was to investigate the targeting potential of L-glutamine utilizing concept-based mutual prodrug design for the delivery of meselamine to colon. Meselamine was linked with L-glutamine through azo linkage and was subjected to in vitro stability studies in aqueous buffers of varied pH range and rat fecal matter. 84.7% release of meselamine was achieved in rat fecal matter with a half-life of 153.5 min, following first order kinetics. Experimental colitis was induced in rats by TNBS to evaluate the therapeutic efficacy of the carrier system and mitigating effect of the conjugate on the colonic inflammation. The results for quantifying parameters like clinical activity score rate, colon to body weight ratio, myeloperoxidase activity and histopathological studies suggest that L-glutamine could be developed as a promising carrier for targeting meselamine to colon for the management of inflammatory bowel disease.