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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 study the macrophage uptake of cyclosporin A-containing colloidal submicrospheres and explore the mechanism of action of cyclosporin A and to screen suitable preparation. METHODS: Three kinds of colloidal submicrospheres of nanospheres, nanocapsules and microemulsions were prepared by 3H cyclosporin A. The mouse peritoneal macrophages were used as the cell model. The colloidal submicron and macrophages were incubated at 37 ℃ Culture 30min, colloidal sub-particles and macrophages separated, measured by liquid scintillation cpm value as a value. Results: The nanosphere could make the cpm value of mouse peritoneal macrophages reach 20 times of the cyclosporin A solution control group, while the nanocapsules and microemulsions made cpm value of mice peritoneal macrophages relative to that of cyclosporine A solution of control group was significantly lower. Surfactant encapsulation and protein adsorption on cpm of mouse peritoneal macrophages have a significant impact. Conclusion: Embedding cyclosporin A in colloidal submicroscopic leukoplakia can change the targeting of macrophages.