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Enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo

Authors Yang G, Zhao YP, Zhang YT, Dang BL, Liu Y, Feng NP

Received 18 July 2015

Accepted for publication 20 September 2015

Published 22 October 2015 Volume 2015:10(1) Pages 6633—6644

DOI https://doi.org/10.2147/IJN.S92665

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Govarthanan Muthusamy

Peer reviewer comments 3

Editor who approved publication: Dr Lei Yang

Gang Yang,1 Yaping Zhao,2 Yongtai Zhang,1 Beilei Dang,1 Ying Liu,1 Nianping Feng1

1School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 2School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai, People’s Republic of China

Abstract: The aim of this investigation was to develop a procedure to improve the dissolution and bioavailability of silymarin (SM) by using bile salt-containing liposomes that were prepared by supercritical fluid technology (ie, solution-enhanced dispersion by supercritical fluids [SEDS]). The process for the preparation of SM-loaded liposomes containing a bile salt (SM-Lip-SEDS) was optimized using a central composite design of response surface methodology with the ratio of SM to phospholipids (w/w), flow rate of solution (mL/min), and pressure (MPa) as independent variables. Particle size, entrapment efficiency (EE), and drug loading (DL) were dependent variables for optimization of the process and formulation variables. The particle size, zeta potential, EE, and DL of the optimized SM-Lip-SEDS were 160.5 nm, -62.3 mV, 91.4%, and 4.73%, respectively. Two other methods to produce SM liposomes were compared to the SEDS method. The liposomes obtained by the SEDS method exhibited the highest EE and DL, smallest particle size, and best stability compared to liposomes produced by the thin-film dispersion and reversed-phase evaporation methods. Compared to the SM powder, SM-Lip-SEDS showed increased in vitro drug release. The in vivo AUC0-t of SM-Lip-SEDS was 4.8-fold higher than that of the SM powder. These results illustrate that liposomes containing a bile salt can be used to enhance the oral bioavailability of SM and that supercritical fluid technology is suitable for the preparation of liposomes.

Keywords: silymarin, solution-enhanced dispersion by supercritical fluids, liposomes, bile salt, bioavailability

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