Preparation of sorafenib self-microemulsifying drug delivery system and its relative bioavailability in rats

doi:10.5246/jcps.2011.02.021

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Preparation of sorafenib self-microemulsifying drug delivery system and its relative bioavailability in rats

Ya-Ou Liu, Jie-Ming Fan, Xue-Qing Wang^*, Qiang Zhang

1. Department of Pharmacy, the First Hospital of Peking University, Beijing 100034, China
2. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Center, Beijing 100191, China

Received:2010-12-06 Revised:2011-02-10 Online:2011-03-15 Published:2011-03-15
Contact: Xue-Qing Wang*

Abstract

Abstract:

Sorafenib is a novel antitumor drug, which is poorly absorbed in the gastrointestinal tract due to its low solubility in water. To improve the bioavailability of sorafenib, a self-microemulsifying drug delivery system (SMEDDS) formulation of sorafenib was prepared and its relative bioavailability in rats was evaluated. The blank SMEDDS was prepared from a mixture of ethyl oleate (oil phase, 20%, w/w), Cremophol EL (surfactant, 48%, w/w), PEG-400 (co-surfactant, 16%, w/w) and ethanol (co-surfactant, 16%, w/w). Sorafenib was subsequently dissolved in the blank SMEDDS to obtain a sorafenib SMEDDS formulation with a final sorafenib concentration at 20 mg/mL. The particle size of the emulsified sorafenib SMEDDS was about 20-25 nm. Compared with sorafenib suspension, the prepared SMEDDS formulation exhibited no effect on the Tmax, significantly increased the AUC, Cmax and MRT and decreased the drug clearance. Most importantly, the oral bioavailability based on AUC0-72 h increased about 25 times after formulating sorafenib in SMEDDS. We concluded that SMEDDS could be a promising vesicle for the oral delivery of the poorly soluble antitumor drug sorafenib.

Key words: Sorafenib, SMEDDS, Relative bioavailability

CLC Number:

R969.1

Supporting:

Ya-Ou Liu, Jie-Ming Fan, Xue-Qing Wang^*, Qiang Zhang. Preparation of sorafenib self-microemulsifying drug delivery system and its relative bioavailability in rats [J]. , DOI: 10.5246/jcps.2011.02.021.

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Preparation of sorafenib self-microemulsifying drug delivery system and its relative bioavailability in rats

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