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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Enhanced in vitro cellular uptake of P-gp substrate by poloxamer-modified liposomes (PMLs) in MDR cancer cells
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Enhanced in vitro cellular uptake of P-gp substrate by poloxamer-modified liposomes (PMLs) in MDR cancer cells

机译：泊洛沙姆修饰的脂质体（PML）在MDR癌细胞中增强了P-gp底物的体外细胞摄取

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摘要

Poloxamer-modified liposomes (PMLs) were prepared using poloxamers (P85 and F68) by the thin-film hydration method for overcoming the multidrug resistance and thereby enhancing the intracellular uptake of specific substrates of P-gp, rhodamine 123 (R123). The prepared liposomes, plain liposomes (PLs) and PMLs, were characterized by particle size, zeta potential and drug entrapment efficiency, and assessed by in vitro cellular uptake using KB and KBV20C (P-gp over-expression cell line) cells. The transmission electron microscopy study revealed the spherical shape of the prepared liposomes. No significant difference was observed between the PMLs and liposome without poloxamer (PLs) in the particle size (~160 nm) and zeta potential (~—5 mV). The in vitro cellular uptake study showed that P85-modified liposomes (PML-P85) significantly increased the internalization of R123 in MDR tumour cells. Our results showed that PML-P85 could be an effective carrier for anticancer drugs in MDR cancer therapy.
机译：泊洛沙姆修饰的脂质体（PML）使用泊洛沙姆（P85和F68）通过薄膜水化方法制备，以克服多药耐药性，从而增强了P-gp罗丹明123（R123）特定底物的细胞内摄取。制备的脂质体，普通脂质体（PLs）和PML的特征在于粒径，ζ电位和药物截留效率，并通过使用KB和KBV20C（P-gp过表达细胞系）细胞的体外细胞吸收来评估。透射电子显微镜研究揭示了所制备脂质体的球形。在PML和不含泊洛沙姆（PLs）的脂质体之间，在粒径（〜160 nm）和Zeta电位（〜-5 mV）之间未观察到显着差异。体外细胞摄取研究表明，P85修饰的脂质体（PML-P85）显着增加了MDR肿瘤细胞中R123的内在化。我们的结果表明，PML-P85可能是抗MDR癌症治疗中抗癌药物的有效载体。

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