Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin

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 g...

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Veröffentlicht in:Journal of biomaterials applications 2014-02, Vol.28 (6), p.887-896
Hauptverfasser: Shangguan, Mingzhu, Lu, Yi, Qi, Jianping, Han, Jin, Tian, Zhiqiang, Xie, Yunchang, Hu, Fuqiang, Yuan, Hailong, Wu, Wei
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container_end_page 896
container_issue 6
container_start_page 887
container_title Journal of biomaterials applications
container_volume 28
creator Shangguan, Mingzhu
Lu, Yi
Qi, Jianping
Han, Jin
Tian, Zhiqiang
Xie, Yunchang
Hu, Fuqiang
Yuan, Hailong
Wu, Wei
description 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.
doi_str_mv 10.1177/0885328213485141
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subjects Administration, Oral
Animals
Bioavailability
Biological Availability
Carriers
Dogs
Drug delivery systems
Homogenizing
In vitro testing
Lecithin
Lipids
Lipids - chemistry
Lipolysis
Microscopy, Electron, Transmission
Nanostructure
Nanostructures
Particle Size
Silymarin - administration & dosage
Silymarin - blood
Silymarin - pharmacokinetics
title Binary lipids-based nanostructured lipid carriers for improved oral bioavailability of silymarin
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