目的:制备三氧化二砷(As2O3)白蛋白微球并鉴定其理化特性及抗肿瘤活性。方法:通过乳化热固化法制备(As2O3)白蛋白微球,应用电镜、微球稳定性实验及体外动力缓释实验等测定其理化特性和释放特性,并以MTT法测定缓释液对骨肉瘤细胞株U-2OS、人肺癌细胞株(SPC-A-1)增殖的抑制能力。结果:As2O3微球粒径集中在56.4~256.7μm。平均(156±3.56)μm。微球含量为(55.22±11.19)%。As2O3微球半数释放时间为23.34h。As2O3微球缓释液表现出对U-2OS及SPC-A-1较强的抑瘤活性。结论:经检测乳化热固化法制备出的As2O3白蛋白徽球,具有较好的理化、缓释特性及抑瘤能力。
Objective: To prepare arsenic trioxide (As2O3) albumin microspheres and to analyze their physicochemical properties and in vitro antitumor activities. Methods; As2O3 albumin microspheres were prepared by emulsification-heat solidification. Physicochemical and the slow-release properties of the microspheres were identified by the electron microscope, thermal stabilization analysis and dynamic dialysis system in vitro. MTT method was used to evaluate the inhibitory effect of the released fluid on human osteosarcoma cell line U-2 OS cells and human lung adenocarcinoma cell line SPC-A-1 cells. Results: The mean diameter of the m/crospheres was (156±3.56)μm ( ranging 56.4 - 256.7 /μm ), with the As2O3 content being (55.22±11.19)% and t1/2 of release time being 23.34 h. The slowly released fluid showed a significant inhibitory effect on U-2 0S and SPC-A-1 cells. Conclusion: As2O3 albumin microspheres prepared in the present study have satisfactory physicochemical, slow-releasing, and tumor-inhibition properties.