LI Xiang, ZHANG Jing, WANG Dong-kai, PAN Wei-san. Anti-tumor activity of folate receptor targeting docetaxel-loaded membrane-modified liposomesJ. 药学学报, 2013,48(7): 1142-1147.
Citation: LI Xiang, ZHANG Jing, WANG Dong-kai, PAN Wei-san. Anti-tumor activity of folate receptor targeting docetaxel-loaded membrane-modified liposomesJ. 药学学报, 2013,48(7): 1142-1147.

Anti-tumor activity of folate receptor targeting docetaxel-loaded membrane-modified liposomes

  • The anti-tumor activity of folate receptor targeting docetaxel-loaded membrane-modified liposomes (FA-PDCT-L) was investigated in vitro and in vivo.  FA-PDCT-L was prepared by organic solvent injection method.  Transmission electron microscope, dynamic light scattering and electrophoretic light scattering were employed to study the physicochemical parameters of FA-PDCT-L.  The inhibitory effects of docetaxel injection (DCT-I), non-modified DCT liposomes (DCT-L) and FA-PDCT-L on the growth of MCF-7 and A-549 cells at different incubation times were detected by CCK-8 assay; and the hemolytic test was employed in vitro.  Tumor mice were randomized into 4 groups: DCT-I, DCT-L, FA-PDCT-L and control group (normal saline), and given drugs at 10 mg·kg−1·d−1 through tail vein.  The tumor volume, mice weight, inhibition rate of tumor and life span were measured at the end of experiments.  The IC50 of the FA-PDCT-L for MCF-7 and A549 cell lines were significantly lower than that of DCT-I and DCT-L, without hemolysis reaction observed.  Compared with control group, the weights of tumor in DCT-I, DCT-L and FA-PDCT-L were decreased, especially for FA-PDCT-L, with inhibitory rates at 79.03 % (P < 0.05).  The life span and median survival time of FA-PDCT-L treated mice were significantly higher than that of DCT-I and DCT-L.  In conclusion, FA-PDCT-L shows a good anti-tumor activity, indicating that it is potential carriers for DCT in the treatment of tumor.

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