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Self-microemulsifying drug-delivery system for improved oral bioavailability of 20(S)-25-methoxyl-dammarane-3β, 12β, 20-triol: preparation and evaluation

Authors Cai S, Shi CH, Zhang XR, Tang XJ, Suo H, Yang L, Zhao YQ

Received 31 October 2013

Accepted for publication 12 December 2013

Published 12 February 2014 Volume 2014:9(1) Pages 913—920

DOI https://doi.org/10.2147/IJN.S56894

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Shuang Cai,1,* Cai-Hong Shi,2,* Xiangrong Zhang,2 Xiaojiao Tang,2 Hao Suo,2 Li Yang,2 Yuqing Zhao2

1Department of Pharmacy, The First Affiliated Hospital of China Medical University, 2Shenyang Pharmaceutical University, Shenyang, People's Republic of China

*These authors contributed equally to this work

Abstract: The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of the poorly water-soluble compound 20(S)-25-methoxydammarane-3β;12β;20-triol (25-OCH3-PPD). Optimized SMEDDS formulations for 25-OCH3-PPD contained Cremophor® EL (50%) as the surfactant, glycerin (20%) as the cosurfactant, and Labrafil® M1944 (30%) as the oil. The SMEDDS were characterized by morphological observation and mean droplet size. The pharmacokinetics and bioavailability of the 25-OCH3-PPD suspension and SMEDDS were evaluated and compared in rats. The plasma concentrations of 25-OCH3-PPD and its main metabolite, 25-OH-PPD, were determined by ultra performance liquid chromatography-tandem mass spectrometry. The relative bioavailability of SMEDDS was dramatically enhanced by an average of 9.8-fold compared with the suspension. Improved solubility and lymphatic transport may contribute to this enhanced bioavailability. Our studies highlight the promise of SMEDDS for the delivery of 25-OCH3-PPD via the oral route.

Keywords: 25-methoxydammarane-3β;12β;20-triol (25-OCH3-PPD), 25-OH-PPD, self-microemulsifying drug delivery system, bioavailability, pharmacokinetics

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