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目的:制备可生物降解高分子材料作载体的多西紫杉醇载药纳米微球(Doc-np),检测其各项特征,并考察其体内外抗肿瘤效果。方法:采用溶剂分散法制备Doc-np。用原子力显微镜和透射电子显微镜观察Doc-np的形态,并用动态光散射仪测定纳米微球的粒径。通过紫外分光光度法测定并计算得出Doc-np的载药量和包封率,再测定该微球的体外释放曲线。在体外及体内考察Doc-np对人卵巢肿瘤SKOV3细胞系的杀伤效果。结果:Doc-np为不规则的圆形,表面光滑,其包封率在90%以上。体外释放曲线显示了Doc-np良好的缓释特性,由细胞实验结果看出Doc-np在体外的抑瘤效果更强。体内实验显示通过肿瘤局部的针对性给药,Doc-np与Doc相比明显延缓肿瘤的生长,显示出优于裸药的抗肿瘤效果。结论:Doc-np与Doc相比可以明显抑制人卵巢肿瘤的生长。肿瘤局部给药增强了Doc-np的抗肿瘤效果,作为一种更为有效的给药途径值得进一步研究。
OBJECTIVE: To prepare docetaxel-loaded nanospheres (Doc-np), a biodegradable macromolecule material, to detect its characteristics and investigate its anti-tumor effect in vitro and in vivo. Methods: Doc-np was prepared by solvent dispersion method. The morphology of Doc-np was observed with atomic force microscope and transmission electron microscope, and the particle size of nanospheres was measured with a dynamic light scattering instrument. The drug loading and entrapment efficiency of Doc-np were determined and calculated by ultraviolet spectrophotometry, and then the in vitro release curve of the microspheres was determined. The killing effect of Doc-np on human ovarian tumor SKOV3 cell line was investigated in vitro and in vivo. Results: Doc-np was irregular round, smooth surface, the encapsulation efficiency of more than 90%. In vitro release curve shows good sustained-release characteristics of Doc-np, the results of the cell experiments showed that Doc-np in vitro antitumor effect is stronger. In vivo experiments showed that by local targeted administration of the tumor, Doc-np significantly delayed the growth of the tumor compared with Doc and showed an antitumor effect superior to that of the naked drug. Conclusion: Doc-np can significantly inhibit the growth of human ovarian tumors compared with Doc. Topical administration of tumor enhances the anti-tumor effect of Doc-np and warrants further study as a more effective route of administration.