增强的渗透性和保留（EPR）效应：概念和方法的意义，以增强其应用,Journal of Personalized Medicine

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增强的渗透性和保留（EPR）效应：概念和方法的意义，以增强其应用
Journal of Personalized Medicine ( IF 4.433 ) Pub Date : 2021-08-06 , DOI: 10.3390/jpm11080771
Jun Wu ₁

Affiliation

临床实践中人类实体瘤的化疗远不能令人满意。尽管发现并合成了数十万种靶向癌细胞增殖和代谢中各种关键单元的抗癌化合物，但根本问题是缺乏将这些化合物选择性地靶向递送至实体瘤组织以在一定长度内维持有效浓度水平药物-肿瘤相互作用执行抗癌活性的时间。增强的通透性和滞留效应（EPR 效应）描述了一种普遍的病理生理现象和机制，其中超过一定大小（大于 40 kDa）的大分子化合物如白蛋白和其他聚合物偶联药物可以在肿瘤血管化区域逐渐积累，从而实现靶向将抗癌化合物递送和保留到实体瘤组织中。临床实践中通过 EPR 效应进行靶向治疗并不总是成功，因为 EPR 效应的强度取决于肿瘤的类型和位置、肿瘤中的血液灌注状态以及大分子抗癌药物的理化性质。

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The Enhanced Permeability and Retention (EPR) Effect: The Significance of the Concept and Methods to Enhance Its Application

Chemotherapy for human solid tumors in clinical practice is far from satisfactory. Despite the discovery and synthesis of hundreds of thousands of anticancer compounds targeting various crucial units in cancer cell proliferation and metabolism, the fundamental problem is the lack of targeting delivery of these compounds selectively into solid tumor tissue to maintain an effective concentration level for a certain length of time for drug-tumor interaction to execute anticancer activities. The enhanced permeability and retention effect (EPR effect) describes a universal pathophysiological phenomenon and mechanism in which macromolecular compounds such as albumin and other polymer-conjugated drugs beyond certain sizes (above 40 kDa) can progressively accumulate in the tumor vascularized area and thus achieve targeting delivery and retention of anticancer compounds into solid tumor tissue. Targeting therapy via the EPR effect in clinical practice is not always successful since the strength of the EPR effect varies depending on the type and location of tumors, status of blood perfusion in tumors, and the physical-chemical properties of macromolecular anticancer agents. This review highlights the significance of the concept and mechanism of the EPR effect and discusses methods for better utilizing the EPR effect in developing smarter macromolecular nanomedicine to achieve a satisfactory outcome in clinical applications.

更新日期：2021-08-07

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