Hruby Martin, Konak Cestmir, Kucka Jan, Vetrik Miroslav, Filippov Sergey K, Vetvicka David, Mackova Hana, Karlsson Goran, Edwards Katarina, Rihova Blanka, Ulbrich Karel
Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, 162 06 Prague 6, Czech Republic.
Macromol Biosci. 2009 Oct 8;9(10):1016-27. doi: 10.1002/mabi.200900083.
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 (131)I and (90)Y proceeds with high yields (>85%). The unlabeled polymers are not cytotoxic for any of the tested murine and human cell lines.
通过自组装热响应性聚（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来用于将诊断和治疗性放射性核素递送至实体瘤中，该共聚物在聚合物嵌段之间带有可水解降解的N-糖基胺基团。胶束通过将共聚物水溶液快速加热至37℃形成。它们的流体动力学直径为128nm（使用动态光散射测量），并且在pH = 7.4的水性缓冲液中孵育期间缓慢降解。用（131）I和（90）Y标记的产率都很高（> 85％）。未标记的聚合物对任何测试的小鼠和人类细胞系都没有细胞毒性。
