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Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis

Authors Deng J, Wu Z, Zhao Z, Wu C, Yuan M, Su Z, Wang Y, Wang Z

Received 27 January 2020

Accepted for publication 22 April 2020

Published 3 June 2020 Volume 2020:15 Pages 3937—3951

DOI https://doi.org/10.2147/IJN.S247406

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Linlin Sun


Jianping Deng,1,2 Zicong Wu,1,2 Zhenling Zhao,2,3 Chaoxi Wu,2,3 Min Yuan,1 Zhengquan Su,1 Yifei Wang,2,3 Zhiping Wang1,2

1Guangdong Provincial Engineering Center of Topical Precise Drug Delivery System, Department of Pharmaceutics, Guangdong Engineering Research Center of Natural Products and New Drugs, Guangdong Provincial University Engineering Technology Research Center of Natural Products and Drugs, Guangdong Pharmaceutical University, Guangzhou 510000, People’s Republic of China; 2Guangzhou (Jinan) Biomedical Research and Development Center, Guangzhou 510000, People’s Republic of China; 3College of Life Science and Technology, Jinan University, Guangzhou 510000, People’s Republic of China

Correspondence: Yifei Wang; Zhiping Wang Email twang-yf@163.com; wzping-jshb@gdpu.edu.cn

Purpose: Berberine (BBR), a major ingredient extracted from Coptis chinensis, is a natural drug with limited oral bioavailability. We developed nanostructured lipid carriers (NLCs) as a delivery system for enhanced anti-inflammatory activity of BBR against ulcerative colitis (UC).
Methods: BBR-loaded nanostructured lipid carriers (BBR-NLCs) prepared via high-pressure homogenization were evaluated for particle size, zeta potential, drug entrapment efficiency, drug loading, drug release, toxicity, and cellular uptake. The anti-UC activities of free and encapsulated BBR were evaluated in a DSS-induced acute model of UC in mice.
Results: Spherical BBR-NLCs were prepared with a particle size of 63.96±  0.31 nm, a zeta potential of +3.16 ±  0.05 mV, an entrapment efficiency of 101.97± 6.34%, and a drug loading of 6.00± 0.09%. BBR-NLCs showed excellent biocompatibility in vivo. Cellular uptake experiments showed that BBR-NLCs improved uptake of BBR by RAW 264.7 cells and Caco-2 cells. Oral administration of BBR-NLCs significantly alleviated colitis symptoms (DAI, colon length, spleen swelling, MPO activity) through inhibition of NF-κB nuclear translocation, decreased expression of pro-inflammatory cytokines (IL-1β, IL-6, MMP-9, CX3CR1, COX-2, TERT), and increased expression of the tight junction protein ZO-1.
Conclusion: BBR-loaded NLCs improved colitis symptoms, which suggested that this may be a novel formulation for treatment of UC.

Keywords: berberine, nanostructured lipid carriers, anti-inflammatory, ulcerative colitis

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