Back to Journals » International Journal of Nanomedicine » Volume 5

Preparation, characterization and relative bioavailability of oral elemene o/w microemulsion

Authors Zeng Z, Zhou G, Wang X, Huang EZ, Zhan X, Liu J, Wang S, Wang A, Li H, Pei X, Xie T

Published 10 August 2010 Volume 2010:5 Pages 567—572

DOI https://doi.org/10.2147/IJN.S12485

Review by Single-blind

Peer reviewer comments 5


Zhaowu Zeng1, Guanglin Zhou1, Xiaoli Wang2, Eric Zhijian Huang1, Xiaori Zhan1, Jun Liu1, Shuling Wang1, Anming Wang1, Haifeng Li1, Xiaolin Pei1, Tian Xie1

1Research Center for Biomedicine and Health, Hangzhou Normal University, Hangzhou, Zhejiang, China; 2Yichun University of Jiangxi Province, Yichun, Jiangxi, China

Abstract: The objective was to develop an elemene oil/water (o/w) microemulsion and evaluate its characteristics and oral relative bioavailability in rats. Elemene was used as the oil phase and drug, polysorbate 80 as a surfactant along with ethanol, propylene glycol, and glycerol as the cosurfactants. The microemulsion was prepared by mixing method, or ultrasonication method in an ultrasonic bath. Its three-dimensional response surface diagram was drawn by Mathcad software. The microemulsion was characterized by visual observation, cross-polarized microscopy, size, zeta potential, acidity, viscosity, and surface tension measurement. The drug content and entrapment efficiency were determined by ultra fast liquid chromatography (UFLC) and liquid surface method. Blood was drawn from rats at different time points after oral administration of an elemene microemulsion or a commercial elemene emulsion for measurement of the drug in plasma by UFLC to establish the pharmacokinetic parameters and relative bioavailability. The elemene microemulsion as a clarified and isotropic system containing 1% elemene (w/v), 5% ethanol (v/v), 15% propylene glycol (v/v), 15% glycerol (v/v), and 5% polysorbate 80 (w/v), was characterized as (57.7 ± 2.8) nm in size, 0.485 ± 0.032 in polydispersity index, (3.2 ± 0.4) mv in zeta potential, (5.19 ± 0.08) in pH, 6 mpa•s in viscosity, (31.8 ± 0.3) mN•m-1 in surface tension, (8.273 ± 0.018) mg•mL-1 in content of ß-elemene, and (99.81 ± 0.24)% in average entrapment efficiency. The area under the concentration-time curves from 0 h to 24 h (AUC0→24h) of the elemene microemulsion and commercial elemene emulsion were integrated to be 3.092 mg•h•L-1 and 1.896 mg•h•L-1 respectively, yielding a relative bioavailability of 163.1%. The present study demonstrates the elemene microemulsion as a new formulation with ease of preparation, high entrapment efficiency, excellent clarity, good stability, and improved bioavailability.

Keywords: elemene, microemulsion, relative bioavailability

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]