Matsumura Yasuhiro, Kataoka Kazunori
Investigative Treatment Division, Research Center for Innovative Oncology, National Cancer Center Hospital East, 6-5-1 Kashiwanoha, Kashiwa 277-8577, Japan.
Cancer Sci. 2009 Apr;100(4):572-9. doi: 10.1111/j.1349-7006.2009.01103.x.
The size of anticancer agent-incorporating micelles can be controlled within the diameter range of 20-100 nm to ensure that they do not penetrate normal vessel walls. With this development, it is expected that the incidence of drug-induced side-effects may be decreased owing to the reduced drug distribution in normal tissue. Micelle systems can also evade non-specific capture by the reticuloendothelial system because the outer shell of a micelle is covered with polyethylene glycol. Consequently, a polymer micelle carrier can be delivered selectively to a tumor by utilizing the enhanced permeability and retention effect. Moreover, a water-insoluble drug can be incorporated into polymer micelles. Presently, several anticancer agent-incorporating micelle carrier systems are under preclinical and clinical evaluation. Furthermore, nucleic acid-incorporating micelle carrier systems are also being developed.
可将载有抗癌剂的胶束尺寸控制在20至100纳米的直径范围内,以确保它们不会穿透正常血管壁。随着这一进展,预计由于药物在正常组织中的分布减少,药物诱导的副作用发生率可能会降低。胶束系统还可以避免被网状内皮系统非特异性捕获,因为胶束的外壳覆盖有聚乙二醇。因此,利用增强的渗透和滞留效应,聚合物胶束载体可以选择性地递送至肿瘤。此外,水不溶性药物可以掺入聚合物胶束中。目前,几种载有抗癌剂的胶束载体系统正在进行临床前和临床评估。此外,载有核酸的胶束载体系统也在开发中。