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首页> 外文期刊>Chemistry and Physics of Lipids >Surface modification of paclitaxel-loaded liposomes using d-alpha-tocopheryl polyethylene glycol 1000 succinate: Enhanced cellular uptake and cytotoxicity in multidrug resistant breast cancer cells
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Surface modification of paclitaxel-loaded liposomes using d-alpha-tocopheryl polyethylene glycol 1000 succinate: Enhanced cellular uptake and cytotoxicity in multidrug resistant breast cancer cells

机译：使用D-α-生育基聚乙二醇1000琥珀酸酯的紫杉醇加载脂质体的表面改性：多药抗性乳腺癌细胞中增强的细胞吸收和细胞毒性

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摘要

Liposomes can achieve a controlled release and an improved bioavailability of water-insoluble drug with minimized side effects. Paclitaxel is an efficient anticancer drug for the treatment of various cancers. However, paclitaxel has a solubility of 0.5 mg/L in water and a low bioavailability of 6.5%. Moreover, paclitaxel is a substrate for p-glycoprotein, which shows a decreased accumulation of drug within the cancer cell expressed by a p-glycoprotein. Therefore, the purpose of this study is to prepare a paclitaxel-loaded liposome and evaluate the effect of d-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) as an inhibitor of p-glycoprotein on the paclitaxel-loaded liposome. The paclitaxel-loaded liposome and TPGS coated paclitaxel-loaded liposome had spherical vesicles, with mean particle size 184.9 18.45 nm with PDI 0.324 +/- 0.018 and 282.6 +/- 20.41 nm with PDI 0.269 +/- 0.013, respectively. Paclitaxel-loaded liposome and TPGS coated paclitaxel-loaded liposome showed a controlled and sustained release of PTX over 72 h. The cellular uptake of paclitaxel from TPGS coated paclitaxel-loaded liposome was a 3.56-fold increase for 2 h and 5.75-fold increase for 4 h compared to that from paclitaxel-loaded liposome in MCF-7/ADR cells, resulting in improved cytotoxicity against MCF-7/ADR cells. Western blot assay revealed the P-gp inhibitory effect of TPGS-coated PTX-liposome. In conclusion, TPGS coated liposome with a sustained releasing capability and the inhibitory effect of p-glycoprotein may be a promising carrier for future applications in cancer therapy.
机译：脂质体可以实现控制释放和具有最小化副作用的水不溶性药物的改善的生物利用度。紫杉醇是一种治疗各种癌症的有效抗癌药物。然而，紫杉醇在水中的溶解度为0.5mg / l，并​​且低生物利用度为6.5％。此外，紫杉醇是对p-糖蛋白的底物，其显示出在p-糖蛋白表达的癌细胞内的药物积聚降低。因此，本研究的目的是制备紫杉醇加载的脂质体，并评估D-α-生育基聚乙二醇1000琥珀酸酯（TPGs）作为紫杉醇负载脂质体上对糖蛋白的抑制剂的影响。紫杉醇装载的脂质体和TPGS涂覆紫杉醇负载的脂质体具有球形囊泡，平均粒度为184.9 18.45nm，PDI 0.324 +/- 0.018和282.6 +/- 20.41nm分别为PDI 0.269 +/- 0.013。紫杉醇负载脂质体和TPGS涂覆的紫杉醇加载的脂质体显示出72小时的PTX受控和持续释放。与来自MCF-7 / ADR细胞中的紫杉醇加载的脂质体相比，来自TPGS的紫杉醇的紫杉醇植入紫杉醇负载脂质体的穴位摄取为3.56倍，增加，5.75倍。 MCF-7 / ADR细胞。 Western印迹测定显示TPGS涂覆的PTX-脂质体的P-GP抑制作用。总之，具有持续释放能力的TPGS涂覆脂质体和P-糖蛋白的抑制作用可能是癌症治疗中未来应用的有望的载体。

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