An enhanced bioactive chitosan-modified microemulsion for mucosal healing of ulcerative colitis.

Int J Biol Macromol

School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; State Key Laboratory of Systems Medicine for Cancer, Shanghai Cancer Inst

Published: January 2025


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Article Abstract

The intestinal mucus layer plays a crucial role in the systemic absorption of drugs. While penetration through this layer traditionally constitutes a pivotal phase in drug absorption, the approach for treating ulcerative colitis (UC) shifts towards facilitating the direct delivery of drugs to the colon. In this study, we engineered a chitosan-modified microemulsion encapsulated nobiletin (NOB-CS-ME) characterized by small particle dimensions and positive charge specifically, designed to enable targeted delivery. In vitro experiments demonstrated that this NOB-CS-ME effectively became less into the intestinal mucus layer, thus achieving successful escape of the intestinal mucus barrier absorption. After circumventing this barrier, NOB-CS-ME exhibited heightened cellular uptake by colonic epithelial cells, displaying an approximately 1.3-fold increase compared to the unmodified microemulsion. Collectively, these observations imply enhanced drug bioavailability, potentially resulting in more efficacious mucosal healing, providing a promising avenue for natural small-molecule drug delivery in UC treatment.

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http://dx.doi.org/10.1016/j.ijbiomac.2024.137847DOI Listing

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