UM  > 中華醫藥研究院
Dual-functional Brij-S20-modified nanocrystal formulation enhances the intestinal transport and oral bioavailability of berberine
Xiong, Wei1; Sang, Wei1; Linghu, Ke Gang1; Zhong, Zhang Feng1; Cheang, Wai San1; Li, Juan2; Hu, Yuan Jia1; Yu, Hua1,3,4; Wang, Yi Tao1
2018
Source PublicationINTERNATIONAL JOURNAL OF NANOMEDICINE
ISSN1178-2013
Volume13Pages:3781-3793
Abstract

Introduction: Berberine (BBR) is a plant-derived benzylisoquinoline alkaloid and has been demonstrated to be a potential treatment for various chronic diseases. The poor water solubility and P-glycoprotein (Pgp)-mediated drug efflux are the main challenges for its further application in a clinical setting.
Materials and methods: In this study, a Brij-S20 (BS20)-modified nanocrystal formulation (BBR-BS20-NCs) has been developed and investigated with the purpose of improving the intestinal absorption of BBR. The physicochemical properties of the developed BBR-BS20-NCs were characterized and the enhancement of the BBR-BS20-NCs on BBR absorption were investigated both in vitro and in vivo.
Results: The results indicated that BS20 could significantly enhance the intracellular uptake of BBR in MDCK-MDR1 cells via a short-term and reversible modulation on the Pgp function, accompanied by a marked increase in Pgp mRNA expression but without significant influence on the Pgp protein expression. Moreover, the morphology of the prepared BBR-BS20-NCs was observed to be prism-like, with a smooth surface and an average diameter of 148.0 ± 3.2 nm. Compared to raw BBR and physical mixture, BBR-BS20-NCs facilitated the dissolution rate and extent of release of BBR in aqueous solution, and further increased the absorption of BBR in MDCK-MDR1 monolayer by overcoming the Pgp-mediated secretory transport (Papp[BL-AP] values of 2.85 ± 0.04 × 10-6 cm/s, 2.21 ± 0.14 × 10-6 cm/s, and 2.00 ± 0.07 × 10-6 cm/s for pure BBR, physical mixture, and BBR-BS20-NCs, respectively). Significant improvements in the maximum concentration observed (Cmax) and area under drug concentration-time curve (AUC0–t) of BBR-BS20-NCs were obtained in pharmacokinetic studies compared to pure BBR, and the relative bioavailability of BBR-BS20-NCs to pure BBR was 404.1%.
Conclusion: The developed BBR-BS20-NCs combine the advantages of nanocrystal formulation and functional excipient. The novel pharmaceutical design provides a new strategy to improve the oral bioavailability of those drugs with both poor water solubility and Pgp-mediated efflux.

KeywordBerberine Poor Water Solubility Pgp-mediated Drug Efflux Brij Nanocrystals
DOIhttp://doi.org/10.2147/IJN.S163763
URLView the original
Indexed BySCI
Language英语
WOS Research AreaScience & Technology - Other Topics ; Pharmacology & Pharmacy
WOS SubjectNanoscience & Nanotechnology ; Pharmacology & Pharmacy
WOS IDWOS:000437158800003
PublisherDOVE MEDICAL PRESS LTD
The Source to ArticleWOS
Fulltext Access
Citation statistics
Cited Times [WOS]:2   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Institute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Macao SAR, China
2.Department of Pharmaceutics, China Pharmaceutical University, Nanjing, Jiangsu, China
3.Hong Kong Baptist University Shenzhen Research Center, Shenzhen, Guangdong, China
4.School of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Hong Kong SAR, China
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Xiong, Wei,Sang, Wei,Linghu, Ke Gang,et al. Dual-functional Brij-S20-modified nanocrystal formulation enhances the intestinal transport and oral bioavailability of berberine[J]. INTERNATIONAL JOURNAL OF NANOMEDICINE,2018,13:3781-3793.
APA Xiong, Wei.,Sang, Wei.,Linghu, Ke Gang.,Zhong, Zhang Feng.,Cheang, Wai San.,...&Wang, Yi Tao.(2018).Dual-functional Brij-S20-modified nanocrystal formulation enhances the intestinal transport and oral bioavailability of berberine.INTERNATIONAL JOURNAL OF NANOMEDICINE,13,3781-3793.
MLA Xiong, Wei,et al."Dual-functional Brij-S20-modified nanocrystal formulation enhances the intestinal transport and oral bioavailability of berberine".INTERNATIONAL JOURNAL OF NANOMEDICINE 13(2018):3781-3793.
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[Xiong, Wei]'s Articles
[Sang, Wei]'s Articles
[Linghu, Ke Gang]'s Articles
Baidu academic
Similar articles in Baidu academic
[Xiong, Wei]'s Articles
[Sang, Wei]'s Articles
[Linghu, Ke Gang]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[Xiong, Wei]'s Articles
[Sang, Wei]'s Articles
[Linghu, Ke Gang]'s Articles
Terms of Use
No data!
Social Bookmark/Share
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.