提高 EPR 效应的策略：一种机制观点和临床转化。
Strategies to improve the EPR effect: A mechanistic perspective and clinical translation.
机构信息
John A. Paulson School of Engineering & Applied Sciences, Harvard University, Cambridge, MA 02138, USA; Wyss Institute for Biologically Inspired Engineering, Cambridge, MA 20138, USA.
John A. Paulson School of Engineering & Applied Sciences, Harvard University, Cambridge, MA 02138, USA; Wyss Institute for Biologically Inspired Engineering, Cambridge, MA 20138, USA; Harvard-MIT Division of Health Sciences and Technology, Massachusetts Institute of Technology, Cambridge, MA 02139, USA.
出版信息
J Control Release. 2022 May;345:512-536. doi: 10.1016/j.jconrel.2022.03.043. Epub 2022 Mar 23.
Many efforts have been made to achieve targeted delivery of anticancer drugs to enhance their efficacy and to reduce their adverse effects. These efforts include the development of nanomedicines as they can selectively penetrate through tumor blood vessels through the enhanced permeability and retention (EPR) effect. The EPR effect was first proposed by Maeda and co-workers in 1986, and since then various types of nanoparticles have been developed to take advantage of the phenomenon with regards to drug delivery. However, the EPR effect has been found to be highly variable and thus unreliable due to the complex tumor microenvironment. Various physical and pharmacological strategies have been explored to overcome this challenge. Here, we review key advances and emerging concepts of such EPR-enhancing strategies. Furthermore, we analyze 723 clinical trials of nanoparticles with EPR enhancers and discuss their clinical translation.
为了提高抗癌药物的疗效并降低其不良反应，人们已经做出了许多努力来实现其靶向递送。这些努力包括开发纳米药物，因为它们可以通过增强的通透性和保留（EPR）效应选择性地穿透肿瘤血管。EPR 效应最初是由 Maeda 等人于 1986 年提出的，此后，为了利用这一现象进行药物递送，已经开发了各种类型的纳米颗粒。然而，由于肿瘤微环境复杂，EPR 效应被发现具有高度的可变性，因此不可靠。已经探索了各种物理和药理学策略来克服这一挑战。在这里，我们回顾了这种 EPR 增强策略的关键进展和新兴概念。此外，我们分析了 723 项具有 EPR 增强剂的纳米颗粒的临床试验，并讨论了它们的临床转化。
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