Preparation of baicalin colon-targeted granules and its intervention effect on ulcerative colitis in rats--颗粒学报PARTICUOLOGY

Huang, Y., Zhou, Y., Shen, Y., Wang, J., Zhou, L., & Chen, Z. (2024). Preparation of baicalin colon-targeted granules and its intervention effect on ulcerative colitis in rats. Particuology, 85, 13-21. https://doi.org/10.1016/j.partic.2023.03.017

Preparation of baicalin colon-targeted granules and its intervention effect on ulcerative colitis in rats

Yongqing Huang, Yuxin Zhou, Yao Shen, Jin Wang, Liangliang Zhou ^*, Zhenhua Chen ^*

Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang, 330013, China

10.1016/j.partic.2023.03.017

Volume 85, February 2024, Pages 13-21

Received 15 November 2022, Revised 7 March 2023, Accepted 22 March 2023, Available online 5 April 2023, Version of Record 17 April 2023.

E-mail: zhoulliang@163.com; zhenhuachen@jxstnu.edu.cn

Highlights

• Preparation of multiunit colon-targeted granules using plasticizer dry powder coating technology.

• In vivo imaging for assessing the targeting of plasticizer dry powder-coated granules.

• Improving the therapeutic effect of baicalin on ulcerative colitis in rats.

Abstract

Baicalin (BA) is a flavonoid extracted from the dried root of Scutellaria baicalensis Georgi with excellent antioxidant and anti-inflammatory biological activities. In this study, Eudragit S100 was used as the colonic target material to prepare BA colonic targeting granules (EBCGs) based on plasticizer dry powder coating technology to improve the targeting transportation performance of BA. In vitro studies showed that EBCGs with pH-sensitive properties were successfully prepared by plasticizer dry powder coating, and in vivo animal imaging studies showed that EBCGs could deliver BA to the colon and inhibit the release of BA in the upper gastrointestinal tract (GIT). In vivo studies showed that EBCGs had good therapeutic effects in colitis, which reduced expression levels of tumor necrosis factor alpha (TNF-α) and interleukin-1β (IL-1β) and increased superoxide dismutase (SOD) activities in the colonic tissues of rats with colitis. In conclusion, Eudragit S100 could be used for the preparation of multi-unit oral colon-targeted formulations by plasticizer dry powder coating technology, and our prepared EBCGs had good colon-targeting properties, which could improve the therapeutic effect and provide a potential application for ulcerative colitis (UC).

Graphical abstract

Keywords

Plasticizer dry powder coating; Colon-targeted granules; In vivo imaging; Ulcerative colitis

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