Abstract: 【Abstract】ObjectiveTo modified doxorubicin liposome with transferrin（TF）, and to investigate its inhibition efficacy on the proliferation of human breast cancer cells. MethodsThe liposome was prepared by thin film ultrasonic, and doxorubicin liposomal was prepared by sulfuric acid gradient. The TFdoxorubicin liposome was prepared by the post insertion method. The uptake of TFliposomal doxorubicin on breast cancer cells MCF7 and MDAMB231 were detected by confocal microscopy. The killing ability of TFdoxorubicin liposomal targeting for MCF7 and MDAMB231 were detected by MTT assay. Inhibitory effect of TFdoxorubicin liposome on the growth of MCF7 and MDAMB231 were detected by soft agar colony assay. ResultsConfocal microscopy result showed that the uptake of TFliposomal doxorubicin on MCF7 and MDAMB231 were significantly higher than doxorubicin liposomal. Cellkilling ability on MCF7 and MDAMB231 showed that the IC50 in TFliposomal doxorubicin ［MCF7 cells:（20.8±3.2）μmol/L; MDAMB231 cells:（20.1±3.0）μmol/L）］ were significantly lower than the liposomal ［（158.6±24.6）μmol/L; （160.1±25.1）μmol/L）］ and free doxorubicin ［（161.7±26.2）μmol/L;（166.9±27.0）μmol/L）］, with significant differences（F=116.03，P<0.001; F=75.29， P<0.001）. Soft agar colony assay showed that the inhibition of TFdoxorubicin liposome on colony growth were significantly higher than doxorubicin liposome, free doxorubicin and control ［diameter of MDAMB231 cells:（60.5±10.4）μm, （94.3±16.8）μm, （131.8±22.6）μm, （162.8±30.3）μm; diameter of MCF7 cells:（31.8±5.5）μm, （62.1±11.1）μm, （108.6±18.6）μm, 157.4±29.3）μm］ , with significant differences (F=87.17， P＜0.000 1；  F=178.23， P＜0.000 1). ConclusionTFdoxorubicin liposome has a significant inhibitory effect on the proliferation of breast cancer cells in vitro, and can effectively and specifically kill the breast cancer cells, which provides theoretical basis for the treatment of breast cancer in vivo.

Key words: Transferrin, Doxorubicin, Liposomes, Breast neoplasms