体内评价水飞蓟宾纳米混悬液靶向肝脏。

In vivo evaluation of silybin nanosuspensions targeting liver.

机构信息

School of Chemistry and Pharmaceutical Engineering, Shandong Polytechnic University, Jinan 250353, China.

出版信息

J Biomed Nanotechnol. 2012 Oct;8(5):760-9. doi: 10.1166/jbn.2012.1444.

DOI:10.1166/jbn.2012.1444

Abstract

The present study investigated the production, in vivo biodistribution and hepatoprotective of two formulated silybin nanosuspensions with different particle size. The physicochemical properties of the two formulated silybin nanosuspensions were investigated by TEM, AFM and SEM. A kinetic study was conducted to evaluate the influence of particle size on the in vivo tissue distribution following intravenous administration in the mice. The in vivo hepatoprotective studies were conducted on beagle dogs with optimized setting. A clear physicochemical difference was observed among the silybin solution, larger particles and the small particles. The formulation of larger particle size was preferentially targeted at liver and spleen. The silybin nanosuspensions, administrated either intravenously or orally, presented significant (P < or = 0.05) hepatoprotective effect by reducing the serum marker enzymes such as AST, ALT, ALP, TBIL and GGT. Histopathological study further confirmed the hepatoprotective activity of the two silybin nanosuspensions formulations when compared with the CCl4 treated control group. These results indicate that the nanosuspensions approaches could be used to improve the drug target delivery and therapeutic efficacy of the silybin.

摘要

本研究考察了两种不同粒径的水飞蓟宾纳米混悬剂的制备、体内分布和肝保护作用。通过 TEM、AFM 和 SEM 研究了两种水飞蓟宾纳米混悬剂的理化性质。进行了一项动力学研究，以评估静脉给药后粒径对体内组织分布的影响。在优化条件下，以比格犬进行了体内肝保护研究。水飞蓟宾溶液、较大颗粒和较小颗粒之间存在明显的理化差异。较大粒径的制剂优先靶向肝脏和脾脏。静脉注射或口服水飞蓟宾纳米混悬剂均可显著降低血清标志物酶（如 AST、ALT、ALP、TBIL 和 GGT），具有显著的肝保护作用（P<或=0.05）。与 CCl4 处理的对照组相比，组织病理学研究进一步证实了两种水飞蓟宾纳米混悬剂制剂的肝保护活性。这些结果表明，纳米混悬剂方法可用于提高水飞蓟宾的药物靶向递送和治疗效果。