Synthesis and evaluation of a water-soluble polymer to reduce Ac-225 daughter migration

被引:13
|
作者
Fitzsimmons, Jonathan [1 ]
Atcher, Robert [1 ]
机构
[1] Los Alamos Natl Lab, Biosci Div, Los Alamos, NM 87545 USA
来源
关键词
actinium; alpha therapy; polyethylenimine; bismuth; PEI; daughter retention;
D O I
10.1002/jlcr.1143
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The actinium decay chain has been promoted as an in vivo alpha generator for therapy, but migration of daughters from the primary conjugate has lead to increased toxicity away from the target organ. To reduce daughter migration, polyethylenimine (PEI) was used with a primary chelator and secondary chelators. The primary chelator, DOTA, was used to coordinate 225 Actinium and secondary chelators-acetate and DTPA, were added to the polymer for coordination of daughters formed by decay. The (225)Actinium polymer derivatives containing secondary chelators were found to retain radioactive daughters better than the 225 Actinium bond to the primary alone. The retention of (213)Bismuth and (209)Thallium had the following order from highest retained to lowest DOTA-PEI-DTPA approximate to DOTA-PEI-CH2OO- > DOTA-PEI. The data suggests this polymer approach could be used to reduce daughter migration and has potential for development of actinium labeled radiopharmaceuticals. Copyright (c) 2007 John Wiley & Sons, Ltd.
引用
收藏
页码:147 / 153
页数:7
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