Analysis on the current status of targeted drug delivery to tumors.

Analysis on the current status of targeted drug delivery to tumors.
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DOI:
10.1016/j.jconrel.2012.07.010
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发表时间:
2012-12-10
期刊:
Journal of controlled release : official journal of the Controlled Release Society
影响因子:
--
通讯作者:
Park K
Park K
中科院分区:
其他
文献类型:
--
作者:
Kwon IK;Lee SC;Han B;Park K

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肿瘤靶向给药是给药的最终目标之一。纳米粒子工程的最新进展确实改善了药物靶向,但结果并不像预期的那样好。这在很大程度上是因为纳米颗粒,无论它们有多先进,都能像传统的药物输送系统一样,通过血液循环找到目标。目前,基于纳米颗粒的药物递送到靶肿瘤组织是基于错误的假设,即大多数纳米颗粒(无论是否聚乙二醇化)通过增强的渗透和保留(EPR)效应到达靶点。研究表明,所谓的靶向部分,即,抗体或配体在纳米颗粒表面上并不能真正改善对靶肿瘤的递送。肿瘤靶向给药涉及到高度复杂的生物学、机械学、化学和转运现象,这些现象的特征在时空上是变化的。然而,大部分的努力都集中在设计和表面操作的药物携带的纳米粒子与其他方面的关注相对较少。本文探讨了目前的误解和靶向给药的主要困难。
Targeted drug delivery to tumor sites is one of the ultimate goals in drug delivery. Recent progress in nanoparticle engineering has certainly improved drug targeting, but the results are not as good as expected. This is largely due to the fact that nanoparticles, regardless of how advanced they are, find the target as a result of blood circulation, like the conventional drug delivery systems do. Currently, the nanoparticle-based drug delivery to the target tumor tissues is based on wrong assumptions that most of the nanoparticles, either PEGylated or not, reach the target by the enhanced permeation and retention (EPR) effect. Studies have shown that so-called targeting moieties, i.e., antibodies or ligands, on the nanoparticle surface do not really improve delivery to target tumors. Targeted drug delivery to tumor sites is associated with highly complex biological, mechanical, chemical and transport phenomena, of which characteristics vary spatiotemporally. Yet, most of the efforts have been focused on design and surface manipulation of the drug carrying nanoparticles with relatively little attention to other aspects. This article examines the current misunderstandings and the main difficulties in targeted drug delivery.
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