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Pluronic L61 accelerates flip-flop and transbilayer doxorubicin permeation

机译:Pluronic L61加快了触发器和跨双层阿霉素的渗透

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It has recently been found that Pluronics (block copolymers of ethylene oxide, EO, and propylene oxide, PO) favor the permeability and accumulation of anthracycline antibiotics, for example doxorubicin (Dox), in tumor cells. In an effort to understand these results, the interaction of EO2/ PO32/EO2 (Pluronic L61) with unilamellar egg yolk vesicles (80-100 nm in diameter) was examined. A partition coefficient K-p = [Pl](membrane)/[Pl](water) = 45 was determined. This corresponds to adsorption of about 20 polymer molecules to the surface of each vesicle in a 20 mum polymer solution. Despite this rather weak adsorption, Pluronic has a substantial effect upon the transmembrane permeation rate of Dox and upon the phospholipid flip-flop rate within the bilayers. Thus, the Dox permeation rate increases threefold and the flip-flop rate increases sixfold in 20 mum Pluronic. The two rates increase linearly with the amount of adsorbed polymer. The obvious ability of Pluronics to increase the mobility of membrane components may have important biomedical consequences. [References: 28]
机译:最近发现,Pluronics(环氧乙烷,EO和环氧丙烷PO的嵌段共聚物)有利于蒽环类抗生素例如阿霉素(Dox)在肿瘤细胞中的渗透性和积累。为了理解这些结果,检查了EO2 / PO32 / EO2(Pluronic L61)与单层蛋黄囊泡(直径80-100 nm)的相互作用。确定分配系数K-p = [Pl](膜)/ [Pl](水)= 45。这相当于在20毫米聚合物溶液中约20个聚合物分子吸附到每个囊泡的表面。尽管这种吸附作用很弱,但Pluronic对Dox的跨膜渗透速率和双层内的磷脂翻转速率有很大影响。因此,在20毫米的Pluronic中,Dox的渗透率增加了三倍,触发器的速度增加了六倍。两种速率随聚合物吸附量线性增加。 Pluronics具有明显的增加膜组件迁移率的能力,可能会产生重要的生物医学后果。 [参考:28]

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