CROSSLINKED MICELLES WITH TRANSIENTLY LINKED DRUGS - A VERSATILE DRUG DELIVERY SYSTEM
CROSSLINKED MICELLES WITH TRANSIENTLY LINKED DRUGS - A VERSATILE DRUG DELIVERY SYSTEM
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DOI：
10.1515/ejnm.2010.3.1.19
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发表时间：
2010-05-01
期刊：
影响因子：
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通讯作者：
Hennink, Wim E.
中科院分区：
文献类型：
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作者：
Rijcken, Cristianne J. F.;Talelli, Marina;Hennink, Wim E.
治疗各种疾病的终极目标是将高剂量的具有高特异性的生物活性化合物输送到其靶部位，以获得最大的治疗效果，同时将对正常器官的副作用降到最低。纳米载体可以在实体肿瘤肿块、炎症和感染部位广泛积累，因为它们的大小取决于血管的渗透性和滞留性（EPR）的增强。迄今为止，各种具有纳米尺度的（宏观）分子组件，如脂质体、聚合物聚集体、碳纳米管和聚合物胶束，已经或正在被评估为药物输送系统。然而，传统的聚合物胶束迄今尚未在临床中显示出其真正的潜在益处。主要原因是（载药）胶束结构在血流动态环境中的不稳定性。近年来，我们的实验室开发了一种新型胶束平台技术，该技术基于一种创新的、高度可调的聚合物，旨在提高各种治疗药物的风险收益比。良好的血液循环，完全控制的药物释放，良好的肿瘤积累和良好的生物相容性是被证明的特点。由于这是一个定制的系统，我们拥有所有可用的工具来开发这种广泛适用的药物输送技术，以实际的医疗产品，在疾病管理领域具有明显的附加价值。
The holy grail in the treatment of various diseases is to deliver high doses of bioactive compounds with a high specificity to their target sites for maximum treatment efficacy, while minimising side effects to normal organs. Nanocarriers can accumulate extensively in solid tumour masses, inflammatory and infectious sites because of their size by virtue of the enhanced permeability and retention (EPR) effect of the vasculature. To date, various (macro) molecular assemblies with nanoscale dimensions such as liposomes, polymer-aggregates, carbon nanotubes and polymeric micelles have been or are currently evaluated as drug delivery systems. However, traditional polymeric micelles have thus far not shown their real potential benefits in the clinic. The dominant origin is the instability of a (drug-loaded) micellar structure in the dynamic environment of the blood stream. In recent years, a novel micellar platform technology has been developed in our laboratories and is based on an innovative, highly tuneable class of polymers designed to improve the risk-benefit ratio of a broad range of therapeutic agents. The superior blood circulation, fully controlled drug release profile, good tumour accumulation and excellent biocompatibility are proven features. Since it is a custommade system, we have all tools available to develop this broadly applicable drug delivery technology towards actual medicinal products with an evident added value in the field of disease management.