Approaches to Improve Macromolecule and Nanoparticle Accumulation in the Tumor Microenvironment by the Enhanced Permeability and Retention Effect.
Approaches to Improve Macromolecule and Nanoparticle Accumulation in the Tumor Microenvironment by the Enhanced Permeability and Retention Effect.
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被动靶向是纳米载体和载药大分子选择性地将其有效载荷递送至实体肿瘤的最重要机制。被动靶向的一个重要驱动因素是增强的渗透性和保留（EPR）效应，这是大多数基于载体的肿瘤靶向药物递送努力的基石。尽管有大量的出版物展示了临床前动物模型的成功，但转化到临床的效果一直很差，目前只有少数纳米药物用于治疗癌症。已经列举了几个障碍和因素，导致对实体瘤的低递送效率和较差的临床转化，包括纳米载体和大分子的特性、血管和生理障碍、影响纳米载体在肿瘤内均匀分布的肿瘤血液供应的异质性、以及大分子和纳米颗粒在肿瘤基质中的转运和穿透深度。为了解决与人类肿瘤靶向和治疗效果差相关的挑战，需要克服影响大分子治疗剂和纳米颗粒递送系统的增强的渗透性和保留（EPR）效应的效率的已确定的障碍。在这篇综述中，方法，以促进改善EPR交付的结果和临床翻译的新的大分子治疗和纳米颗粒药物输送系统进行了讨论。
Passive targeting is the foremost mechanism by which nanocarriers and drug-bearing macromolecules deliver their payload selectively to solid tumors. An important driver of passive targeting is the enhanced permeability and retention (EPR) effect, which is the cornerstone of most carrier-based tumor-targeted drug delivery efforts. Despite the huge number of publications showcasing successes in preclinical animal models, translation to the clinic has been poor, with only a few nano-based drugs currently being used for the treatment of cancers. Several barriers and factors have been adduced for the low delivery efficiency to solid tumors and poor clinical translation, including the characteristics of the nanocarriers and macromolecules, vascular and physiological barriers, the heterogeneity of tumor blood supply which affects the homogenous distribution of nanocarriers within tumors, and the transport and penetration depth of macromolecules and nanoparticles in the tumor matrix. To address the challenges associated with poor tumor targeting and therapeutic efficacy in humans, the identified barriers that affect the efficiency of the enhanced permeability and retention (EPR) effect for macromolecular therapeutics and nanoparticle delivery systems need to be overcome. In this review, approaches to facilitate improved EPR delivery outcomes and the clinical translation of novel macromolecular therapeutics and nanoparticle drug delivery systems are discussed.
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影响因子：
4.9
作者：
Alexis F;Pridgen E;Molnar LK;Farokhzad OC
通讯作者：
Farokhzad OC
影响因子：
4.7
作者：
Baronzio G;Parmar G;Baronzio M
通讯作者：
Baronzio M
低强度聚焦超声触发相变纳米液滴的药物释放
影响因子：
12.4
作者：
Cao Y;Chen Y;Yu T;Guo Y;Liu F;Yao Y;Li P;Wang D;Wang Z;Chen Y;Ran H
通讯作者：
Ran H
影响因子：
17.1
作者：
Anselmo, Aaron C.;Zhang, Mengwen;Mitragotri, Samir
通讯作者：
Mitragotri, Samir
影响因子：
5.8
作者：
Andrés, D;Sánchez-Reus, I;Cascales, M
通讯作者：
Cascales, M