Polyoxazoline thermoresponsive micelles as radionuclide delivery systems.
Thermoresponsive polymer micelles are promising drug and radionuclide carriers with a strong passive targeting effect into solid tumors. We have synthesized ABA triblock copolymers poly[2-methyl-2-oxazoline-block-(2-isopropyl-2-oxazoline-co-2-butyl-2-oxazoline)-block-2-methyl-2-oxazoline]. These polymers are molecularly dissolved in aqueous millieu below the cloud point temperature (CPT) of the thermoresponsive central block and above CPT form polymer micelles at CMC 5-10 × 10(-5) g · mL(-1) with diameter ≈200 nm. The phenolic moiety introduced into the copolymer allowed radionuclide labeling with iodine-125 ongoing in good yield with sufficient in vitro stability under model conditions.
Hruby
Martin
M
Institute of Macromolecular Chemistry, v.v.i., Academy of Sciences of the Czech Republic, Heyrovsky Sq. 2, 162 06 Prague 6, Czech Republic. mhruby@centrum.cz
Filippov
Sergey K
SK
Panek
Jiri
J
Novakova
Michaela
M
Mackova
Hana
H
Kucka
Jan
J
Vetvicka
David
D
Ulbrich
Karel
K
D006461:Hemolysis; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D008970:Molecular Weight; D010080:Oxazoles / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D011868:Radioisotopes / Q000008:administration & dosage*; D013696:Temperature
D008823:Micelles; D010080:Oxazoles; D011108:Polymers; D011868:Radioisotopes; C555801:poly(2-methyl-2-oxazoline-block-(2-isopropyl-2-oxazoline-co-2-butyl-2-oxazoline)-block-2-methyl-2-oxazoline)