小鼠腹腔巨噬细胞对载环孢菌素A胶体亚微粒的摄取

The uptake of cyclosporine A loaded colloidal particles by mouse peritneal macrophage in vitro

目的:研究巨噬细胞对载环孢菌素A胶体亚微粒的摄取,探讨环孢菌素A的作用机理及筛选适宜的制剂。方法:用3H环孢菌素A制备了纳米球、纳米囊、微乳三种胶体亚微粒,以小鼠腹腔巨噬细胞为细胞模型,将各胶体亚微粒与巨噬细胞在37℃条件下培养30min,分离胶体亚微粒与巨噬细胞,用液闪的方法测定细胞中cpm值作为摄取值。结果:纳米球可使小鼠腹腔巨噬细胞的cpm值达环孢菌素A溶液对照组的20倍,而纳米囊和微乳则使小鼠腹腔巨噬细胞的cpm值相对于环孢菌素A溶液对照组有明显降低。表面活性剂包裹及蛋白吸附对小鼠腹腔巨噬细胞的cpm值均有明显影响。结论:将环孢菌素A包埋于胶体亚微闰中可以改变其对巨噬细胞的靶向性。

OBJECTIVE:To investigate the uptake of cyclosporine A loaded colloidal particles by mouse peritoneal macrophage in vitro .METHODS: 3H labelled cyclosporine A (CyA) loaded colloidal particles:polylactic acid nanospheres,polylactic acid nanocapsulse and microemulsions were prepared.The 3H labelled cyclosporine A loaded colloidal praticles were incubated with mouse peritoneal macrophage (MPM) for 30 min at 37℃,then the cells were seperated from the colloidal particlae and the radioactivity (cpm) of 3H in the cells were measured by a liquid scintillation counter.RESULTS:Comparing with the solution of CyA,about 20 times increase of cpm value in MPM were observed when binding CyA with polylactic acid nanospheres while some obvious decrease was observed by binding CyA with polylactic acid nanocapsules or microemulsions.The surfactant coating and plasma protein adsorption were found to have some effect on the uptake of microemulsions or nanoparticles by MPM respectively.CONCLUSION:Colloidal drug carriers may affect the targeting of CyA to mononuclear phagocyte system.