Abstract

Berberine hydrochloride (BBH) has a variety of pharmacological activities such as antitumor, antimicrobial, anti-inflammation, and reduce irritable bowel syndrome. However, poor stability and low oral bioavailability limited its usage. Herein, an oil-in-water nanoemulsion system of BBH was developed to improve its stability and oral bioavailability. The pseudoternary phase diagrams were constructed for the determination of composition of various nanoemulsions. The nanoemulsions of BBH composed of Labrafil M 1944 CS (oil phase), RH-40 (surfactant), glycerin (co-surfactant), and water (aqueous phase). The O/W nanoemulsion of BBH showed a relative bioavailability of 440.40% compared with unencapsulated BBH and was stable in our 6-month stability study. Further, there was a significant increase in intestinal permeability of BBH as assessed by Caco-2 cell monolayers and a significant reduction in efflux of BBH by the multidrug efflux pump P-glycoprotein. This study confirmed that the nanoemulsion formulation could be used as an alternative oral formulation of BBH to improve its stability, oral bioavailability and permeability.

Details

Title
Nanoemulsion-based delivery system for enhanced oral bioavailability and Caco-2 cell monolayers permeability of berberine hydrochloride
Author
Yong-Jiang, Li 1 ; Xiong-Bin Hu 1 ; Xiu-Ling Lu 1 ; De-Hua, Liao 2 ; Tian-Tian, Tang 3 ; Jun-Yong, Wu 1 ; Da-Xiong, Xiang 4 

 Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, Hunan, China;; Key Laboratory of Traditional Chinese Medicine Preparations of Hunan Province, the Second Xiangya Hospital, Central South University, Changsha, Hunan, China; 
 Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, Hunan, China;; Key Laboratory of Traditional Chinese Medicine Preparations of Hunan Province, the Second Xiangya Hospital, Central South University, Changsha, Hunan, China;; Hunan Cancer Hospital, Changsha, Hunan, China; 
 Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, Hunan, China;; Institute of Clinical Pharmacy, Central South University, Changsha, Hunan, China 
 Department of Pharmacy, The Second Xiangya Hospital, Central South University, Changsha, Hunan, China;; Key Laboratory of Traditional Chinese Medicine Preparations of Hunan Province, the Second Xiangya Hospital, Central South University, Changsha, Hunan, China;; Institute of Clinical Pharmacy, Central South University, Changsha, Hunan, China 
Pages
1868-1873
Publication year
2017
Publication date
Nov 2017
Publisher
Taylor & Francis Ltd.
ISSN
10717544
e-ISSN
15210464
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2195231964
Copyright
© 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This work is licensed under the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.