精氨酸水溶液复溶的多西他赛聚合物胶束的体外药效学及体内分布

目的：考察精氨酸复溶的多西他赛胶束的体外药效及体内分布情况。方法：用CCK-8法考察多西他赛胶束和多西他赛注射液对肿瘤细胞的增殖抑制作用。以荧光染料DIR标记多西他赛聚合物胶束,通过活体成像系统比较精氨酸水溶液复溶组,生理盐水复溶组和多西他赛注射液组的荧光分布。结果：多西他赛胶束组IC₅₀值明显比多西他赛注射液组高。精氨酸复溶的多西他赛胶束组肿瘤部位荧光强度比生理盐水复溶组和多西他赛注射液组都强。结论：精氨酸复溶的多西他赛胶束肿瘤靶向性更强且在肿瘤部位的停留时间更长,但其体外抗肿瘤活性有待提高。

In vitro Cytotoxicity and in vivo Distribution of Arginine-dispersed Docetaxel Polymeric Micelles

Objective: To investigate the in vitro cytotoxicity and in vivo distribution of the arginine-dispersed docetaxel polymeric micelles(DTX-PMs). Methods: The CCK-8 method was used to compare the tumor cell growth inhibition of docetaxel micelles and docetaxel injection. The labeled micelles were prepared by a rotary evaporation method with the fluorescent dye DIR incorporated, and an in vivo imaging system was used to detect the in vivo distribution of arginine-dispersed micells. Results: The fluorescene intensity of arginine-dispersed DTX-PMs at the tumor site was stronger than those of both docetaxel injection and saline-dispersed micelles. However, the IC₅₀ value of DTX-PMs was two times higher than that of docetaxel injection. Conclusion: The arginine-dispersed DTX-PMs have a much better tumor-targeting effect and a longer time at tumor site, but the in vitro antitumor effect of DTX-PMs needs to be improved.