首页> 美国卫生研究院文献>Oncology Letters >Solid lipid nanoparticles with TPGS and Brij 78: A co-delivery vehicle of curcumin and piperine for reversing P-glycoprotein-mediated multidrug resistance in vitro
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Solid lipid nanoparticles with TPGS and Brij 78: A co-delivery vehicle of curcumin and piperine for reversing P-glycoprotein-mediated multidrug resistance in vitro

机译:具有TPGS和Brij 78的固体脂质纳米颗粒:姜黄素和胡椒碱的共同递送载体可在体外逆转P糖蛋白介导的多药耐药性

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摘要

Multidrug resistance (MDR) is a main clinical hurdle for chemotherapy of cancer, and overexpression of P-glycoprotein (P-gp) is a key factor. In the present study, a new co-delivery system for reversing MDR was designed and developed. The system was composed of curcumin (Cur) and piperine (Pip) encapsulated in solid lipid nanoparticles (SLNs) with tocopheryl polyethylene glycol succinate (TPGS) and Brij 78 [(Cur+Pip)-SLNs]. TPGS and Brij 78 could sensitize MDR tumors by inhibiting the P-gp drug efflux system. The combination of Cur and Pip, when administered in SLNs formulations, resulted in a significant enhancement in cytotoxicity and allowed efficient intracellular delivery of the drugs in drug-resistant A2780/Taxol cells. This dual inhibitory strategy may have significant potential in the clinical management of MDR in cancer.
机译:多药耐药性(MDR)是癌症化疗的主要临床障碍,P-糖蛋白(P-gp)的过表达是关键因素。在本研究中,设计和开发了一种新的用于逆转MDR的共同投放系统。该系统由姜黄素(Cur)和胡椒碱(Pip)包裹在固体脂质纳米颗粒(SLNs)中,生育酚聚乙二醇琥珀酸酯(TPGS)和Brij 78 [(Cur + Pip)-SLNs]。 TPGS和Brij 78可以通过抑制P-gp药物外排系统来使MDR肿瘤敏感。当以SLNs制剂给药时,Cur和Pip的组合可显着增强细胞毒性,并允许药物在耐药A2780 / Taxol细胞中有效地细胞内递送。这种双重抑制策略可能在癌症的MDR的临床管理中具有巨大的潜力。

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