TPGS修饰脂质体对阿霉素抗肿瘤活性的增敏作用

TPGS-modified Doxorubicin Liposomes Sensitize Tumor Cells to Doxorubicin

摘要: 目的制备聚乙二醇1000维生素E琥珀酸酯(TPGS)修饰的阿霉素脂质体并考察其对阿霉素抗肿瘤活性的增敏作用。方法用阳离子树脂吸附法测定阿霉素脂质体的包封率；MTT法测定对MCF-7和MCF-7/ADR的毒性；用荧光显微镜观察阿霉素的细胞摄取，并用HPLC测定细胞内的阿霉素含量。结果 TPGS修饰的阿霉素脂质体增加了MCF-7/ADR对阿霉素的摄取，并增强了对MCF-7和MCF-7/ADR细胞的毒性。结论 TPGS修饰脂质体能显著增强MCF-7和MCF-7/ADR对阿霉素的敏感性。

Abstract: OBJECTIVE To prepare doxorubicin liposomes modified with TPGS, and investigate its sensitization effect of tumor cells to doxorubicin. METHODS The encapsulation efficiency of doxorubicin was determined via cationic resin absorption; the cytotoxicity to MCF-7 and MCF-7/ADR cell was determined by MTT assay; cellular uptake of doxorubicin was detected by fluorescence microscopy; the intracellular doxorubicin were determined by HPLC. RESULTS Doxorubicin liposomes modified with TPGS enhanced the cellular uptake of doxorubicin in MCF-7/ADR cells and enhance cytotoxicity both to MCF-7 and MCF-7/ADR cells. CONCLUSION TPGS-modified doxorubicin liposomes can evidently sensitize both MCF-7 and MCF-7/ADR cells to doxorubicin.