Oral pectin/oligochitosan microspheres for colon-specific controlled release of quercetin to treat inflammatory bowel disease.

Shisuo Jing, Huayuan Chen, Ergang Liu, Meng Zhang, Feng Zeng, Huan Shen, Yuefei Fang, Bahtiyor Muhitdinov, Yongzhuo Huang

Carbohydrate polymers 2023 Sep 15

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Inflammatory bowel disease (IBD) is a chronic, life quality-reducing disease with no cures available yet. To develop an effective medication suitable for long-term use is an urgent but unmet need. Quercetin (QT) is a natural dietary flavonoid with good safety and multifaceted pharmacological activities against inflammation. However, orally administrated quercetin yields unproductive outcomes for IBD treatment because of its poor solubility and extensive metabolism in the gastrointestinal tract. In this work, a colon-targeted QT delivery system (termed COS-CaP-QT) was developed, of which the pectin (PEC)/Ca2+ microspheres were prepared and then crosslinked by oligochitosan (COS). The drug release profile of COS-CaP-QT was pH-dependent and colon microenvironment-responsive, and COS-CaP-QT showed preferential distribution in the colon. The mechanism study showed that QT triggered the Notch pathway to regulate the proliferation of T helper 2 (Th2) cells and group 3 innate lymphoid cells (ILC3s) and the inflammatory microenvironment was remodeled. The in vivo therapeutic results revealed that COS-CaP-QT could relieve the colitis symptoms and maintain the colon length and intestinal barrier integrity. Copyright © 2023. Published by Elsevier Ltd.

Citation

Shisuo Jing, Huayuan Chen, Ergang Liu, Meng Zhang, Feng Zeng, Huan Shen, Yuefei Fang, Bahtiyor Muhitdinov, Yongzhuo Huang. Oral pectin/oligochitosan microspheres for colon-specific controlled release of quercetin to treat inflammatory bowel disease. Carbohydrate polymers. 2023 Sep 15;316:121025