Thermoresponsive, Hydrolytically Degradable Polymer Micelles Intended for Radionuclide Delivery
Thermoresponsive, Hydrolytically Degradable Polymer Micelles Intended for Radionuclide Delivery
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DOI：
10.1002/mabi.200900083
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发表时间：
2009-10-08
影响因子：
4.6
通讯作者：
Ulbrich, Karel
中科院分区：
文献类型：
--
作者：
Hruby, Martin;Konak, Cestmir;Ulbrich, Karel
通过在聚合物嵌段之间具有水解可降解的N-葡糖胺基团的自组装温敏性聚（N-异丙基丙烯酰胺）-接枝-聚[N-（2-羟丙基）甲基丙烯酰胺]共聚物制备的新型聚合物胶束被提出用于将诊断和治疗放射性核素递送到实体肿瘤中。胶束通过将共聚物的水溶液快速加热至37 ℃而形成。它们的流体动力学直径为128 nm（使用动态光散射测量），在pH = 7.4的水性缓冲液中孵育期间缓慢降解。用I-131和Y-90两者进行标记具有高产率（>85%）。未标记的聚合物对任何测试的鼠和人细胞系均无细胞毒性。
Novel polymer micelles, prepared by self-assembling thermoresponsive poly(N-isopropylacrylamide)-graft-poly[N-(2-hydroxypropyl)methacrylamide] copolymers with hydrolytically degradable N-glycosylamine groups between the polymer blocks are proposed for delivery of diagnostic and therapeutic radionuclides into solid tumors. The micelles are formed by fast heating of an aqueous solution of the copolymer to 37 degrees C. They have a hydrodynamic diameter of 128 nm (measured using dynamic light scattering) and slowly degrade during incubation in aqueous buffer at pH = 7.4. Labeling with both I-131 and Y-90 proceeds with high yields (>85%). The unlabeled polymers are not cytotoxic for any of the tested murine and human cell lines.