Journal
REACTIVE & FUNCTIONAL POLYMERS
Volume 71, Issue 12, Pages 1155-1159Publisher
ELSEVIER
DOI: 10.1016/j.reactfunctpolym.2011.09.003
Keywords
Macroporous chelating beads; Radioembolization; Quinoline-8-ol; 8-Hydroxyquinoline-5-sulfonic acid; Liver cancer
Funding
- Grant Agency of the Czech Republic [P207/10/P054]
- Ministry of Education, Youth and Sports of the Czech Republic [1M4635608802]
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We describe the synthesis, characterization and radiochemical studies on macroporous chelating polymer beads as carriers of beta-emitters lutetium-177 and iodine-131 intended for radioembolization of liver tumors. The starting poly(glycidyl methacrylate-co-ethylene dimethacrylate) (bead size 20-40 mu) was reacted with ammonia or methylamine to introduce primary and secondary amino groups, respectively. The primary amino groups containing polymer was used for the attachment of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) moieties, while quinoline-8-ol or 8-hydroxyquinoline-5-sulfonic acid moieties, respectively, were introduced onto the secondary amino groups containing polymer. All the polymers were labeled quantitatively by lutetium-177 in ammonium acetate buffer. DOTA containing beads however required heating to 80 degrees C while the quinoline-8-ol or 8-hydroxyquinoline-5-sulfonic acid moieties containing polymers were quantitatively radiolabeled within 1 h at room temperature. The quinoline-8-ol groups containing polymer was radioiodinated in 95% yield by a chloramine method. Both lutetium-177 and iodine-131 radiolabels were stable in an in vitro study in rat blood plasma. Quinoline-8-ol or 8-hydroxyquinoline-5-sulfonic acid moieties are thus more suitable for the radiolabeling of macroporous beads with lutetium-177 for radioembolization purposes than well-established DOTA moieties and in addition, quinoline-8-ol also allows radiolabeling with iodine-131. (C) 2011 Elsevier Ltd. All rights reserved.
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