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首页> 外文期刊>Journal of drug targeting >Block copolymer micelles as delivery vehicles of hydrophobic drugs: Micelle-cell interactions
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Block copolymer micelles as delivery vehicles of hydrophobic drugs: Micelle-cell interactions

机译:嵌段共聚物胶束作为疏水性药物的传递载体:胶束-细胞相互作用

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摘要

One-thitd of drugs in development are water insoluble and one-half fail in trials because of poor pharmacokinetics, Block copolymer micelles are nanosized panicles that can solubilize hydrophobic drugs and alter their kinetics in vitro and in vivo. However, block copolymer micelles are not solely passive drug containers that simply solubilize hydrophobic drugs; cells internalize micelles To facilitate the development of advanced, controlled, micellar drug delivery vehicles, we have to understand the fate of micelles and micelle-incorporated drugs in cells and in vivo. With micelle-based drug formulations recently reaching clinical trials, the impetus for answers is ever so strong and detailed studies of interactions of micelles and cells are starting to emerge Most notably, the question arises: Is the internalization of block copolymer micelles carrying small molecular weight drugs an undesired side effect or a useful means of improving the effectiveness of the incorporated drugs?
机译:研发中的药物的三分之一是水不溶性的,并且由于不良的药物代谢动力学而在试验中失败了一半。嵌段共聚物胶束是纳米颗粒,可以溶解疏水性药物并在体外和体内改变其动力学。然而,嵌段共聚物胶束不只是简单地溶解疏水性药物的被动药物容器;反之亦然。细胞将胶束内部化为了促进先进,可控制的胶束药物传递载体的发展,我们必须了解胶束和掺入胶束的药物在细胞和体内的命运。随着基于胶束的药物制剂近来进入临床试验,对答案的推动力如此之强,关于胶束与细胞相互作用的详细研究开始兴起。最值得注意的是,出现了一个问题:嵌段共聚物胶束的内在化是否具有小分子量?药物有不良副作用或提高掺入药物有效性的有用方法?

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