Thermoresponsive, hydrolytically degradable polymer micelles intended for radionuclide delivery.
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.
Hruby
Martin
M
Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, 162 06 Prague 6, Czech Republic. mhruby@centrum.cz
Konak
Cestmir
C
Kucka
Jan
J
Vetrik
Miroslav
M
Filippov
Sergey K
SK
Vetvicka
David
D
Mackova
Hana
H
Karlsson
Goran
G
Edwards
Katarina
K
Rihova
Blanka
B
Ulbrich
Karel
K
D000178:Acrylamides / Q000737:chemistry / Q000378:metabolism; D000180:Acrylic Resins; D001672:Biocompatible Materials / Q000737:chemistry / Q000378:metabolism; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D016503:Drug Delivery Systems; D006801:Humans; D006868:Hydrolysis; D008422:Materials Testing; D008823:Micelles; D015394:Molecular Structure; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D011868:Radioisotopes / Q000737:chemistry / Q000378:metabolism*; D013696:Temperature
D000178:Acrylamides; D000180:Acrylic Resins; D001672:Biocompatible Materials; D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D011868:Radioisotopes; C052970:poly-N-isopropylacrylamide; C032976:N-(2-hydroxypropyl)methacrylamide