Polymeric micelles in anticancer therapy: targeting, imaging and triggered release.

Polymeric micelles in anticancer therapy: targeting, imaging and triggered release.
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DOI:
10.1007/s11095-010-0233-4
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发表时间:
2010-12
影响因子:
3.7
通讯作者:
Hennink WE
Hennink WE
中科院分区:
医学3区
文献类型:
--
作者:
Oerlemans C;Bult W;Bos M;Storm G;Nijsen JF;Hennink WE

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胶束是粒径约为5-100 nm的胶体颗粒,目前正在研究作为抗癌治疗中疏水药物的载体。目前,五种用于抗癌治疗的胶束制剂正在进行临床评价,其中Genexol-PM已被FDA批准用于乳腺癌患者。然而,基于胶束的药物递送可以以不同的方式改进。靶向配体可以连接到胶束上,其特异性识别并结合肿瘤细胞中过表达的受体,并且螯合或掺入成像部分使得能够在体内追踪胶束用于生物分布研究。此外,pH-、热-、超声-或光敏嵌段共聚物允许受控的胶束解离和触发的药物释放。这些方法的结合将进一步提高基于胶束的药物递送的特异性和有效性,并使“魔术子弹”的发展向前迈出了一大步。
Micelles are colloidal particles with a size around 5–100 nm which are currently under investigation as carriers for hydrophobic drugs in anticancer therapy. Currently, five micellar formulations for anticancer therapy are under clinical evaluation, of which Genexol-PM has been FDA approved for use in patients with breast cancer. Micelle-based drug delivery, however, can be improved in different ways. Targeting ligands can be attached to the micelles which specifically recognize and bind to receptors overexpressed in tumor cells, and chelation or incorporation of imaging moieties enables tracking micelles in vivo for biodistribution studies. Moreover, pH-, thermo-, ultrasound-, or light-sensitive block copolymers allow for controlled micelle dissociation and triggered drug release. The combination of these approaches will further improve specificity and efficacy of micelle-based drug delivery and brings the development of a ‘magic bullet’ a major step forward.
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