Nanostructured lipid carriers for parenteral delivery of silybin: Biodistribution and pharmacokinetic studies
Nanostructured lipid carriers for parenteral delivery of silybin: Biodistribution and pharmacokinetic studies
复制标题
DOI：
10.1016/j.colsurfb.2010.06.008
复制
发表时间：
2010-10-15
影响因子：
5.8
通讯作者：
Zhang, Qiang
中科院分区：
文献类型：
--
作者：
Jia, Lejiao;Zhang, Dianrui;Zhang, Qiang
本研究的目的是探索纳米结构脂质载体（NLCs）静脉给药水飞蓟宾（一种水溶性较差的抗肝病药物）的潜力。采用乳化高温蒸发低温固化法制备水飞蓟宾- nlc。所得NLC的平均尺寸为232.1 nm， zeta电位为-20.7 mV。差示扫描量热法（DSC）分析表明，水飞蓟宾在NLC中不呈结晶态。水飞蓟宾- nlc的体外释放数据符合两阶段指数动力学模型。以新西兰兔和昆明小鼠为实验动物，研究水飞蓟宾- nlc静脉给药后的药代动力学和组织分布。平行研究了水飞蓟宾控制溶液。与水飞蓟宾溶液相比，水飞蓟宾- nlc具有更高的组织浓度-时间曲线下面积（AUC），且在血液中循环的时间更长。组织分布表明水飞蓟宾- nlc在RES器官，特别是肝脏中有较高的摄取。这些结果表明NLC是一种潜在的水飞蓟宾缓释靶向体系。(C) 2010 Elsevier B.V.版权所有
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.