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引用本文:张楠,单伟光,王文喜.TPGS修饰脂质体对阿霉素抗肿瘤活性的增敏作用[J].中国现代应用药学,2012,29(4):298-302.
ZHANG Nan, SHAN Weiguang, WANG Wenxi.TPGS-modified Doxorubicin Liposomes Sensitize Tumor Cells to Doxorubicin[J].Chin J Mod Appl Pharm(中国现代应用药学),2012,29(4):298-302.
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TPGS修饰脂质体对阿霉素抗肿瘤活性的增敏作用
张楠,单伟光,王文喜
浙江工业大学药学院,杭州 310014
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。
关键词:  阿霉素  脂质体  耐药  TPGS  细胞摄取
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TPGS-modified Doxorubicin Liposomes Sensitize Tumor Cells to Doxorubicin
ZHANG Nan, SHAN Weiguang, WANG Wenxi
School of Pharmacy, Zhejiang University of Technology, Hangzhou 310014, China
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.
Key words:  doxorubicin  liposomes  drug resistance  TPGS  cellular uptake
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