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Biocompatible nanoemulsions based on hemp oil and less surfactants for oral delivery of baicalein with enhanced bioavailability

Authors Yin J, Xiang C, Wang P, Yin Y, Hou Y

Received 27 December 2016

Accepted for publication 1 March 2017

Published 10 April 2017 Volume 2017:12 Pages 2923—2931


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Linlin Sun

Juntao Yin,1,* Cuiyu Xiang,1,* Peiqing Wang,1 Yuyun Yin,2 Yantao Hou3

1Department of Pharmaceutics, Huaihe Hospital Affiliated to Henan University, Kaifeng, 2Department of Physiochemical Analysis, Henan Provincial Institute for Food and Drug Control, Zhengzhou, 3Department of Pharmaceutical Engineering, Henan Vocational College of Applied Technology, Kaifeng, People’s Republic of China

*These authors contributed equally to this work

Abstract: Baicalein (BCL) possesses high pharmacological activities but low solubility and stability in the intestinal tract. This study aimed to probe the potential of nanoemulsions (NEs) consisting of hemp oil and less surfactants in ameliorating the oral bioavailability of BCL. BCL-loaded NEs (BCL-NEs) were prepared by high-pressure homogenization technique to reduce the amount of surfactants. BCL-NEs were characterized by particle size, entrapment efficiency (EE), in vitro drug release, and morphology. Bioavailability was studied in Sprague-Dawley rats following oral administration of BCL suspensions, BCL conventional emulsions, and BCL-NEs. The obtained NEs were ~90 nm in particle size with an EE of 99.31%. BCL-NEs significantly enhanced the oral bioavailability of BCL, up to 524.7% and 242.1% relative to the suspensions and conventional emulsions, respectively. BCL-NEs exhibited excellent intestinal permeability and transcellular transport ability. The cytotoxicity of BCL-NEs was documented to be low and acceptable for oral purpose. Our findings suggest that such novel NEs and preparative process provide a promising alternative to current formulation technologies and suitable for oral delivery of drugs with bioavailability issues.

Keywords: baicalein, nanoemulsions, biocompatibility, high-pressure homogenization, hemp oil, bioavailability

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