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

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 Dr...

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Autores principales:	Deng J, Wu Z, Zhao Z, Wu C, Yuan M, Su Z, Wang Y, Wang Z
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2020
Materias:	berberine nanostructured lipid carriers anti-inflammatory ulcerative colitis Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/264d823f4e6e4cdcac9d360515019f00
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spelling	oai:doaj.org-article:264d823f4e6e4cdcac9d360515019f002021-12-02T10:33:25ZBerberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis1178-2013https://doaj.org/article/264d823f4e6e4cdcac9d360515019f002020-06-01T00:00:00Zhttps://www.dovepress.com/berberine-loaded-nanostructured-lipid-carriers-enhance-the-treatment-o-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Jianping 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 ChinaCorrespondence: Yifei Wang; Zhiping Wang Email twang-yf@163.com; wzping-jshb@gdpu.edu.cnPurpose: 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 colitisDeng JWu ZZhao ZWu CYuan MSu ZWang YWang ZDove Medical Pressarticleberberinenanostructured lipid carriersanti-inflammatoryulcerative colitisMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 3937-3951 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	berberine nanostructured lipid carriers anti-inflammatory ulcerative colitis Medicine (General) R5-920
spellingShingle	berberine nanostructured lipid carriers anti-inflammatory ulcerative colitis Medicine (General) R5-920 Deng J Wu Z Zhao Z Wu C Yuan M Su Z Wang Y Wang Z Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis
description	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 ChinaCorrespondence: Yifei Wang; Zhiping Wang Email twang-yf@163.com; wzping-jshb@gdpu.edu.cnPurpose: 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
format	article
author	Deng J Wu Z Zhao Z Wu C Yuan M Su Z Wang Y Wang Z
author_facet	Deng J Wu Z Zhao Z Wu C Yuan M Su Z Wang Y Wang Z
author_sort	Deng J
title	Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis
title_short	Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis
title_full	Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis
title_fullStr	Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis
title_full_unstemmed	Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis
title_sort	berberine-loaded nanostructured lipid carriers enhance the treatment of ulcerative colitis
publisher	Dove Medical Press
publishDate	2020
url	https://doaj.org/article/264d823f4e6e4cdcac9d360515019f00
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Berberine-Loaded Nanostructured Lipid Carriers Enhance the Treatment of Ulcerative Colitis

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