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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。
To study the effect of surface modification on phagocytosis and distribution of cyclosporin A nanoparticles in vitro. METHODS: Poly (L-lactic acid) nanoparticles with a mean diameter of 59 nm were prepared with 3H cyclosporin A and surface-modified with Brij 78, Myrj 5 3 and Myrj 5 93 surfactants respectively by physical adsorption . Mouse peritoneal macrophages in vitro cell model to a Kunming mice as an animal model of in vitro cell phagocytosis and in vivo tissue distribution experiments. Results: The intraperitoneal macrophages of mice could uptake the cyclosporin A by 20 times as much as the solution group, and the surface modification could significantly reduce the uptake of peritoneal macrophages in mice. In the nanoparticle group, the distribution of cyclosporin A in the liver and spleen of mice was significantly increased compared with the cyclosporine A solution group, and the surface modification could make the distribution of cyclosporin A in the liver and spleen of mice Different degrees of increase. CONCLUSIONS: Surface modification can significantly alter the cellular uptake of cyclosporin A polylactic acid nanoparticles in vitro and the tissue distribution in the reticuloendothelial system in vivo.