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Thermoresponsive,Hydrolytically Degradable Polymer Micelles Intended for Radionuclide Delivery |
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| Authors: | Martin Hruby Cestmir Konak Jan Kucka Miroslav Vetrik Sergey K Filippov David Vetvicka Hana Mackova Goran Karlsson Katarina Edwards Blanka Rihova Karel Ulbrich |
| Institution: | 1. Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, Heyrovsky Sq. 2, 162 06 Prague 6, Czech Republic;2. Nuclear Physics Institute, Academy of Sciences of the Czech Republic, 250 68 Rez, Czech Republic;3. Institute of Microbiology, Academy of Sciences of the Czech Republic, Videnska 1083, 142 20 Prague 4, Czech Republic;4. Department of Physical and Analytical Chemistry, Box 579, Uppsala University, SE‐75123, Uppsala, Sweden |
| Abstract: | Novel polymer micelles, prepared by self‐assembling thermoresponsive poly(N‐isopropylacrylamide)‐graft‐polyN‐(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 °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 131I and 90Y proceeds with high yields (>85%). The unlabeled polymers are not cytotoxic for any of the tested murine and human cell lines.  |
| Keywords: | drug‐delivery systems micelles radioisotopes thermoresponsive polymers |