In vitro and in vivo evaluation of a self-microemulsifying drug delivery system for silybin

Abstract

Abstract: To enhance the oral absorption of the poorly water-soluble drug silybin, a self-microemulsifying drug delivery system (SMEDDS) composed of ethyl linoleate, Cremophor EL and PEG 400 for oral administration of silybin was formulated, and its physicochemical properties and bioavailability of silybin were evaluated. The in vitro release of silybin from microemulsion and dispersion of silybin from SMEDDS were significantly faster than those from the commercial silybin hard capsule, respectively. The area under the drug concentration-time curve (AUC) and the mean maximum plasma level (Cmax) of the SMEDDS were remarkably greater than those of the hard capsule after oral administration to rats. The absorption of silybin formulated in SMEDDS exhibited a 2.3-fold increase in bioavailability as compared with the hard capsule. These results demonstrated that SMESDDS might be a useful drug delivery system for the oral delivery of the poorly water-soluble drug silybin.

Key words: Self-microemulsifying drug delivery system, Silybin, Microemulsion, Bioavailability

CLC Number:

R945

Supporting:

Xin-Ru Li, Yu-Sheng Pei, Yan-Qing Huang, Yan-Xia Zhou, Yu-Chen Zhang, Yan Liu^*. In vitro and in vivo evaluation of a self-microemulsifying drug delivery system for silybin[J]. .

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