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On the clinical treatment of cancer disease, a strategy has been used through the association of two or more anticancer compound in order to enhance anti-tumour effect using synergistic effect of drugs combination, reducing the effective dosage and side effects and tumour resistance.Nearly two thirds of the breast cancer cells have their positive estrogens receptor, and then tamoxifen, as an estrogen receptor modulator, can reverse the multidrug resistance (MDR) of these tumout cells.In this study, we investigate a novel strategy of combining an estrogen receptor modulator, tamoxifen citrate (TMX), along with an anticancer drug, docetaxel (DTX), in the form of liposomal co-delivery system.In MTT array, the ratio-dependent between these two drugs was evaluated by the median-effect analysis in an attempt to improve the therapeutic efficacy of this combination in vivo.Then the synergistic effect of drug combinations was verified in the breast cancer cell MCF-7 and MCF-7/ADR expressed MDR.Multidrug-loaded liposomes show the strong cytotoxicity in MCF-7cell and reversed multidrug resistance in MCF-7/ADR cell which expressed MDR.We explored in vitro cytotoxicity of different groups including free DTX, DTX liposomes, TMX liposomes and TMX+DTX liposomes on MCF-7 cells and MCF-7/ADR cells, respectively.(Fig 1, Fig2).Obviously, DTX+TMX liposomes have stronger vitro cytotoxicity of MCF-7 cells in lower concentration of DTX.Besides, TMX+DTX liposomes can reverse the multidrug resistance and lead to lowest cell viability (%) compared to other groups in the figure.