Nanostructured lipid carriers for parenteral delivery of silybin: Biodistribution and pharmacokinetic studies

被引：145

作者：

Jia, Lejiao ^{[1
]}

Zhang, Dianrui ^{[1
]}

Li, Zhenyu ^{[2
]}

Duan, Cunxian ^{[1
]}

Wang, Yancai ^{[1
]}

Feng, Feifei ^{[1
]}

Wang, Feihu ^{[1
]}

Liu, Yue ^{[1
]}

Zhang, Qiang ^{[3
]}

机构：

[1] Shandong Univ, Coll Pharm, Dept Pharmaceut, Jinan 250012, Peoples R China

[2] Shandong Univ, Coll Pharm, Dept Med Chem, Jinan 250012, Peoples R China

[3] Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

来源：

COLLOIDS AND SURFACES B-BIOINTERFACES | 2010年 / 80卷 / 02期

关键词：

Silybin; Nanostructured lipid carriers; Pharmacokinetics; Tissue distribution; In vitro release; MILK THISTLE; ORAL BIOAVAILABILITY; BODY DISTRIBUTION; BINARY-MIXTURES; NANOPARTICLES; SILYMARIN; THERAPY; LIQUID; SYSTEM; BILE;

D O I：

10.1016/j.colsurfb.2010.06.008

中图分类号：

Q6 [生物物理学];

学科分类号：

071011 [生物物理学];

摘要：

The objective of the present study was to explore the potential of nanostructured lipid carriers (NLCs) for the intravenous delivery of silybin, a poorly water-soluble antihepatopathy agent. Silybin-NLC was prepared by the method of emulsion evaporation at a high temperature and solidification at a low temperature. The resultant NLC had a mean size 232.1 nm and a zeta potential of -20.7 mV. The differential scanning calorimetry (DSC) analysis indicated that silybin was not in crystalline state in the NLC. In vitro data for release of the drug from silybin-NLC was fitted to a two-stage exponential kinetic model. The pharmacokinetics and tissue distribution of silybin-NLC were studied after intravenous administration using New Zealand rabbits and Kunming mice as experimental animals. A silybin control solution was studied parallelly. Silybin-NLC showed higher AUC (area under tissue concentration-time curve) values and circulated in the blood stream for a longer time compared with silybin solution. The tissue distribution demonstrated a high uptake of silybin-NLC in RES organs particularly in liver. These results indicate that NLC is a potential sustained release and targeting system for silybin. (C) 2010 Elsevier B.V. All rights reserved.

引用

页码：213 / 218

页数：6

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