论文部分内容阅读
研究叶酸受体靶向多烯紫杉醇膜修饰脂质体(FA-PDCT-L)的体内外抗肿瘤活性。采用有机溶剂注入法制备FA-PDCT-L并利用透射电镜、粒径zeta电位测定仪考察其理化性质。采用CCK-8法检测多烯紫杉醇注射液(DCT-I)、未修饰DCT脂质体(DCT-L)和FA-PDCT-L在不同孵育时间对MCF-7及A549肿瘤细胞的生长抑制作用,并进行体外溶血性实验;将荷瘤小鼠随机分为DCT-I、DCT-L、FA-PDCT-L和对照组(生理盐水),10 mg.kg 1.d 1尾静脉注射给药,实验结束后测定各组小鼠体重、瘤重,并计算抑瘤率,进行生存分析。结果显示:FA-PDCT-L对MCF-7和A549的IC50值在各时间点均显著低于DCT-I组及DCT-L组,且在体外4 h内未见溶血现象。与对照组相比,DCT-I、DCT-L和FA-PDCT-L组小鼠瘤重均减少,其中FA-PDCT-L的作用最为显著,抑瘤率为79.03%(P<0.05);FA-PDCT-L生存曲线和中位生存时间显著高于DCT-I和DCT-L。该研究表明FA-PDCT-L具有良好的抗癌活性,有望成为肿瘤治疗中DCT的优良载体。
To study the antitumor activity of folic acid receptor targeting docetaxel membrane-modified liposomes (FA-PDCT-L) in vitro and in vivo. FA-PDCT-L was prepared by organic solvent injection method and its physical and chemical properties were investigated by transmission electron microscopy and particle size zeta potential meter. The inhibitory effects of DCT-I, DCT-L and FA-PDCT-L on the growth of MCF-7 and A549 tumor cells were detected by CCK-8 at different incubation time , And in vitro hemolytic experiments; the tumor-bearing mice were randomly divided into DCT-I, DCT-L, FA-PDCT-L and control group (saline), 10 mg.kg 1.d 1 intravenous injection At the end of the experiment, the body weight and tumor weight of each group were measured, and the tumor inhibition rate was calculated for survival analysis. The results showed that the IC50 values of FA-PDCT-L on MCF-7 and A549 at each time point were significantly lower than those in DCT-I and DCT-L groups, and no hemolysis in 4 hours in vitro. Compared with the control group, the tumor weight of DCT-I, DCT-L and FA-PDCT-L groups were all decreased, and the effect of FA-PDCT-L was the most significant, with the inhibition rate of 79.03% (P <0.05). FA-PDCT-L survival curve and median survival time were significantly higher than DCT-I and DCT-L. This study shows that FA-PDCT-L has good anticancer activity and is expected to be an excellent carrier of DCT in tumor therapy.