多西他赛他莫昔芬复方脂质体逆转乳腺癌细胞耐药性的研究  

Study of Overcoming Multidrug Resistance in Breast Cancer Cell with Docetaxel-Tamoxifen Liposomes in Vitro

作　　者：李亚男[1] 田琳[1] 罗文基[1] 徐月红[2] LI Ya-nan;TIAN Lin;LUO Wen-ji;XU Yue-hong(Department of Pharmacy,The Fifth Affiliated Hospital of Sun Yat-sen University,Zhuhai 519000,China;School of Pharmaceutical Sciences,Sun Yat-sen University,Guangzhou 510006,China)

机构地区：[1]中山大学附属第五医院药学部,广东珠海519000 [2]中山大学药学院,广东广州510006

出　　处：《海峡药学》2022年第11期1-5,共5页Strait Pharmaceutical Journal

摘　　要：目的 在体外考察多西他赛(Docetaxel, DTX)他莫昔芬(Tamoxifen, TMX)复方脂质体对乳腺癌细胞耐药性的逆转作用。方法 在体外,利用乳腺肿瘤细胞MCF-7和耐药乳腺肿瘤细胞MCF-7/ADR,通过MTU实验和中效原理评价多西他赛和他莫昔芬不同浓度时的协同作用。通过薄膜分散法制备具有协同作用的多西他赛他莫昔芬复方脂质体。在体外通过MTT实验考察复方脂质体细胞毒性和逆转肿瘤耐药作用。结果 在MCF-7细胞和MCF-7/ADR细胞,TMX-DUX混合物(M∶M=7∶1)的中效原理联合指数值都小于1,具有协同作用。对MCF-7细胞,游离药物DTX在浓度0.001 nM到50 nM有细胞毒性,游离TMX没有细胞毒性,DTX-TMX复方脂质体具有细胞毒性。对耐药MCF-7/ADR细胞,游离药物DTX在浓度0.001 nM到50 nM没有细胞毒性,游离TMX没有细胞毒性,DTX-TMX复方脂质体具有细胞毒性,并且细胞毒性强度大于对MCF-7细胞。结论 DTX-TMX复方脂质体能够逆转肿瘤耐药性。OBJECTIVE To investigate docetaxel(DTX) tamoxifen(TMX) compound liposomes to reverse the drug resistance of breast cancer cells in vitro.METHODS On breast tumor cells MCF-7 and MCF-7/ADR,the synergistic effect of docetaxel and tamoxifen at different concentrations was evaluated by MTT experiment and the principle of intermediate effect in vitro.The certain proportion of docetaxel and tamoxifen with synergistic effect liposomes were used to prepare by film dispersion method.In vitro MTT experiments were conducted to investigate the compound liposome cytotoxicity and reverse tumor drug resistance.RESULTS On the MCF-7 and MCF-7/ADR cells, the joint index value of the TMX-DTX mixture(M∶M=7∶1) was less than 1 with synergistic effect.In MCF-7 cells, the free drug DTX had cytotoxicity at concentrations of 0.001 nM to 50 nM,free TMX had no cytotoxicity, and compound liposomes had cytotoxicity.In drug-resistant MCF-7/ADR cells, the free drug DTX had no cytotoxicity at concentrations of 0.001 nM to 50 nM,free TMX had no cytotoxicity, compound liposomes had cytotoxicity that was greater than in MCF-7 cells.CONCLUSION The synergistic effect of docetaxel-tamoxifen liposomes can enhance the antitumor efficacy, reduce the dose of drugs, and can reverse the resistance of tumors.

关 键 词：多西他赛 他莫昔芬 脂质体 逆转肿瘤耐药性 乳腺癌细胞 

分 类 号：R94[医药卫生—药剂学]