title: Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin.
abstract: The main purpose of this study was to prepare binary lipids-based nanostructured lipid carriers to improve the oral bioavailability of silymarin, a poorly water-soluble liver protectant. Silymarin-loaded nanostructured lipid carriers were prepared by the method of high-pressure homogenization with glycerol distearates (Precirol ATO-5) and oleic acid as the solid and liquid lipids, respectively, and lecithin (Lipoid E 100) and Tween-80 as the emulsifiers. The silymarin-nanostructured lipid carrier prepared under optimum conditions was spherical in shape with mean particle size of ∼78.87 nm, entrapment efficiency of 87.55%, loading capacity of 8.32%, and zeta potential of -65.3 mV, respectively. In vitro release of silymarin-nanostructured lipid carriers was very limited even after 12 h, while in vitro lipolysis showed fast digestion of nanostructured lipid carriers within 1 h. Relative oral bioavailability of silymarin-nanostructured lipid carriers in Beagle dogs was 2.54- and 3.10-fold that of marketed Legalon® and silymarin solid dispersion pellets, respectively. It was concluded that nanostructured lipid carriers were potential drug delivery systems to improve the bioavailability of silymarin. Other than improved dissolution, alternative mechanisms such as facilitated absorption as well as lymphatic transport may contribute to bioavailability enhancement.
authors.affiliation: 1Key Laboratory of Smart Drug Delivery of Ministry of Education and PLA, School of Pharmacy, Fudan University, Shanghai, PR China.
authors.forename: Mingzhu
authors.initials: M
authors.lastname: Shangguan
authors.forename: Yi
authors.initials: Y
authors.lastname: Lu
authors.forename: Jianping
authors.initials: J
authors.lastname: Qi
authors.forename: Jin
authors.initials: J
authors.lastname: Han
authors.forename: Zhiqiang
authors.initials: Z
authors.lastname: Tian
authors.forename: Yunchang
authors.initials: Y
authors.lastname: Xie
authors.forename: Fuqiang
authors.initials: F
authors.lastname: Hu
authors.forename: Hailong
authors.initials: H
authors.lastname: Yuan
authors.forename: Wei
authors.initials: W
authors.lastname: Wu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004285:Dogs; D008055:Lipids / Q000737:chemistry*; D008066:Lipolysis; D046529:Microscopy, Electron, Transmission; D049329:Nanostructures; D010316:Particle Size; D012838:Silymarin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
chemical_list: D008055:Lipids; D012838:Silymarin
keywords: Nanostructured lipid carrier; glycerol distearate; oleic acid; oral bioavailability; silymarin