Berberine-Loaded Carboxylmethyl Chitosan Nanoparticles Ameliorate DSS-Induced Colitis and Remodel Gut Microbiota in Mice.

Abstract

Inflammatory bowel disease (IBD) is a refractory disorder characterized by chronic and recurrent inflammation. The progression and pathogenesis of IBD is closely related to oxidative stress and irregularly high concentrations of reactive oxygen species (ROS). A new oxidation-responsive nano prodrug was constructed from a phenylboronic esters-modified carboxylmethyl chitosan (OC-B) conjugated with berberine (BBR) that degrades selectively in response to ROS. The optimized micelles exhibited well-controlled physiochemical properties and stability in a physiological environment. OC-B-BBR micelles could effectively encapsulate the anti-inflammatory drug berberine and exhibit ideal H2O2-triggered release behavior as confirmed by in vitro drug loading and release studies. The in vivo anti-inflammatory effect and regulation of gut microbiota caused by it were explored in mice with colitis induced by dextran sodium sulfate (DSS). The results showed that OC-B-BBR significantly ameliorated colitis symptoms and colon damage by regulating the expression levels of IL-6 and remodeling gut microbiota. In summary, this study exhibited a novel BBR-loaded Carboxylmethyl Chitosan nano delivery system which may represent a promising approach for improving IBD treatment.

• Authors: Luqing Zhao, Xueying Du, Jiaxin Tian, Xiuhong Kang, Yuxin Li, Wenlin Dai, Danyan Li, Shengsheng Zhang, Chao Li
• Journal: Frontiers in pharmacology (Front Pharmacol) Vol. 12 Pg. 644387 ( 2021) ISSN: 1663-9812 [Print] Switzerland
• PMID: 33959013 (Publication Type: Journal Article)
• Copyright: Copyright © 2021 Zhao, Du, Tian, Kang, Li, Dai, Li, Zhang and Li.