AUTHOR=Zhao Luqing , Du Xueying , Tian Jiaxin , Kang Xiuhong , Li Yuxin , Dai Wenlin , Li Danyan , Zhang Shengsheng , Li Chao 

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

JOURNAL=Frontiers in Pharmacology

VOLUME=Volume 12 - 2021

YEAR=2021

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2021.644387

DOI=10.3389/fphar.2021.644387

ISSN=1663-9812

ABSTRACT=Inflammatory bowel disease (IBD) is a refractory disorders characterized by chronic and relapsing inflammatory. Oxidative stress and abnormally high levels of reactive oxygen species (ROS) play an important role in the pathogenesis and progression of IBD. 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 physiological environment. In vitro drug loading and release studies confirmed that the OC-B-BBR micelles could effectively encapsulate the model anti-inflammatory drug berberine and exhibit desirable H2O2-triggered release behaviors. In vivo anti-inflammatory effect and regulation of gut microbiota by it were evaluated in a dextran sulfate sodium (DSS)-induced colitis model in mice. 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.