Hirsjärvi Samuli, Passirani Catherine, Benoit Jean-Pierre
LUNAM Université, Ingénierie de la Vectorisation Particulaire, Angers, France.
Curr Drug Discov Technol. 2011 Sep;8(3):188-96. doi: 10.2174/157016311796798991.
Nanocarriers can penetrate the tumour vasculature through its leaky endothelium and, in this way, accumulate in several solid tumours. This is called the enhanced permeation and retention (EPR) effect. Together with nanocarriers whose surface is tailored for prolonged blood circulation times, the concept is referred to as passive targeting. Targeting ligands, which bind to specific receptors on the tumour cells and endothelium, can be attached on the nanocarrier surface. This active targeting increases the selectivity of the delivery of drugs. Passive and active drug targeting with nanocarriers to tumours reduce toxic side-effects, increase efficacy, and enhance delivery of poorly soluble or sensitive therapeutic molecules. In this review, currently studied and used passive and active targeting strategies in cancer therapy are presented.
纳米载体可以通过肿瘤血管渗漏的内皮细胞穿透肿瘤脉管系统,从而在多种实体瘤中蓄积。这被称为增强渗透与滞留(EPR)效应。与表面经过修饰以延长血液循环时间的纳米载体一起,这一概念被称为被动靶向。可以将与肿瘤细胞和内皮细胞上特定受体结合的靶向配体附着在纳米载体表面。这种主动靶向提高了药物递送的选择性。纳米载体对肿瘤的被动和主动药物靶向可减少毒副作用、提高疗效,并增强难溶性或敏感治疗分子的递送。在本综述中,介绍了目前在癌症治疗中研究和使用的被动和主动靶向策略。