Zhejiang Key Laboratory of Smart Biomaterials and Key Laboratory of Biomass Chemical Engineering of Ministry of Education, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027, China.
Zhejiang Key Laboratory of Smart Biomaterials and Key Laboratory of Biomass Chemical Engineering of Ministry of Education, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027, China; ZJU-Hangzhou Global Scientific and Technological Innovation Center, Hangzhou 311215, China.
Adv Drug Deliv Rev. 2022 Dec;191:114614. doi: 10.1016/j.addr.2022.114614. Epub 2022 Nov 5.
Over the past three decades, the enhanced permeability and retention (EPR) effect has been considered the basis of tumor-targeted drug delivery. Various cancer nanomedicines, including macromolecular drugs, have been designed to utilize this mechanism for preferential extravasation and accumulation in solid tumors. However, such nanomedicines have not yet achieved convincing therapeutic benefits in clinics. Increasing evidence suggests that the EPR effect is over-represented in human tumors, especially in metastatic tumors. This review covers the evolution of the concept, the heterogeneity and limitation of the EPR effect in clinical realities, and prospects for alternative strategies independent of the EPR effect.
在过去的三十年中，增强的通透性和保留（EPR）效应被认为是肿瘤靶向药物输送的基础。各种癌症纳米药物，包括大分子药物，被设计利用这种机制优先在实体瘤中渗出和积累。然而，这些纳米药物在临床上尚未取得令人信服的治疗效果。越来越多的证据表明，EPR 效应在人类肿瘤中过度表达，特别是在转移性肿瘤中。本综述涵盖了这一概念的演变，EPR 效应在临床现实中的异质性和局限性，以及独立于 EPR 效应的替代策略的前景。
