【摘要】 研究表面修饰对载环孢菌素A纳米粒体外细胞吞噬和体内组织分布的影响。方法 :用3H 环孢菌素A制备了平均粒径为 5 9nm的聚乳酸纳米粒 ,采用物理吸附的方法分别用Brij 78、Myrj 5 3和Myrj 5 93种表面活性剂对其进行了表面修饰。以小鼠腹腔巨噬细胞为体外细胞模型 ,以一级昆明种小鼠为动物模型 ,分别做体外细胞吞噬实验和体内组织分布实验。结果 :纳米粒组可使小鼠腹腔巨噬细胞对环孢菌素A的摄取值达溶液组的2 0倍 ,表面修饰可使小鼠腹腔巨噬细胞的摄取值明显减小。纳米粒组可使环孢菌素A在小鼠肝、脾的组织分布相对于环孢菌素A溶液组明显增加 ,表面修饰可使环孢菌素A在小鼠肝、脾的组织分布有不同程度的增加。结论 :表面修饰可以显著改变载环孢菌素A聚乳酸纳米粒的体外细胞摄取和体内在网状内皮系统的组织分布。更多还原

【Abstract】 Objective: To investigate the effect of surface modification on the uptake of cyclosporine A loaded nanoparticles by cells in vitro and on the body distribution in vivo . Methods: The polylactic acid nanoparticles with a mean diameter of 59 nm were prepared with 3H labelled cyclosporine A and then three surfactants: Brij 78, Myrj 53 and Myrj 59 were used to modify the surface of the nanoparticles by physical adsorption. The mouse peritoneal macrophages and 35 mice were used to investigate the uptake of nanoparticles by cells in vitro and body distribution in vivo respectively. Results: In in vitro experiment, a 20 fold increase of cpm value in mouse peritoneal macrophages was observed in cyclosporine A nanoparticles compared with that in the cyclosporine A solution. Surface modification was found to reduce the uptake of nanoparticles. In in vivo body distribution, a noticeable increase of cpm value in reticuloendothelial system (RES) was observed. Conclusion: Surface modification effectively altered the uptake of cyclosporine A loaded polylactic acid nanoparticles by cells in vitro and the body distribution in vivo .更多还原