Uptake of cyclosporine A loaded colloidal drug carriers by mouse peritoneal macrophages in vitro  

小鼠腹腔巨噬细胞对环孢菌素A胶体型药物载体的体外摄取(英文)

作　　者：王杰[1] 张强[1] 

机构地区：[1]北京大学医学部药学院药剂教研室,北京中国100083

出　　处：《Acta Pharmacologica Sinica》2001年第1期59-63,共5页中国药理学报（英文版）

基　　金：National Natural Science Foundation of China, № 39870897

摘　　要：AIM: To investigate the uptake of cyclosporine A loaded colloidal drug carriers by mouse peritoneal macrophage (MPM) in vitro. METHODS: The [3H]cyclosporine A loaded colloidal particles: poly lactic acid nanospheres, polylactic acid nanocapsules, and microemulsions were prepared. The [3H]cyclosporine A loaded colloidal particles were incubated with MPM for 30 min at 37℃, then the cells were separated from the colloidal particles and the radioactivity was measured by a liquid scintillation counter. RESULTS: In comparison to the cyclosporine A solution, the binding to polylactic acid nanospheres produced a 20-fold increase in the uptake of cyclosporine A by MPM in 30 min incubation, whereas some obvious decrease in the uptake of cyclosporine A by MPM was observed in the binding of cyclosporine A with polylactic acid nanocapsules or microemulsions. The surfactant coating and plasma protein adsorption were found to have marked effects on the uptake of cyclosporine A loaded nanospheres by MPM. CONCLUSION: Our present study indicated that colloidal drug carriers might affect the targeting of cyclosporine A to mononuclear phagocyte system.目的:研究小鼠腹腔巨噬细胞体外对环孢菌素A胶体亚微粒的摄取。方法:制备[~3H]-环孢菌素A纳米球、纳米囊和微乳三种胶体亚微粒,以小鼠腹腔巨噬细胞为体外细胞模型,研究小鼠腹腔巨噬细胞体外对环孢菌素A胶体亚微粒的摄取。结果:纳米球可使巨噬细胞对环孢菌素A的摄取达对照溶液的20倍,而纳米囊和微乳则使巨噬细胞对环孢菌素A的摄取明显减少。在胶体亚微粒的表面进行表面活性剂修饰和血浆蛋白吸附对巨噬细胞的摄取有明显影响。结论:将环孢菌素A包封于胶体亚微粒中能改变其对巨噬细胞的靶向作用。

关 键 词：CYCLOSPORINS MICROSPHERES CAPSULES emulsions pentoneal macrophages 

分 类 号：R94[医药卫生—药剂学]