Synthesis, biodistribution and excretion of radiolabeled poly(2-alkyl-2-oxazoline)s
Synthesis, biodistribution and excretion of radiolabeled poly(2-alkyl-2-oxazoline)s
复制标题
DOI：
10.1016/j.jconrel.2007.02.015
复制
发表时间：
2007-06-22
影响因子：
10.8
通讯作者：
Essler, Markus
中科院分区：
文献类型：
--
作者：
Gaertner, Florian C.;Luxenhofer, Robert;Essler, Markus
在这里，我们报告的制备定义明确的水溶性聚（2-甲基-2-恶唑啉）和聚（2-乙基-2-恶唑啉）末端配备有螯合剂（N，N '，N“，N”'-四氮杂十二烷-1，4，7，10-四乙酸（DOTA））的放射性核素标记。本文研究了In-111标记的聚（2-烷基-2-恶唑啉）在小鼠体内的组织分布和排泄。我们发现，亲水性聚合物不会在组织中积累，并迅速从血池中清除，主要是通过肾脏中的肾小球过滤。相反，只有一小部分通过肝胆道排泄。网状内皮系统（RES）仅吸收极少量的聚（2-烷基-2-恶唑啉）。闪烁成像研究表明In-111标记的聚（2-恶唑啉）在体内成像的可行性。由于用于靶向的另外的官能度可以容易地经由官能单体单元引入到聚（2-恶唑啉）中，因此这些化合物满足作为放射性核素治疗中的载体分子的应用的基本要求。(c)2007 Elsevier B. V.保留所有权利。
Here we report on the preparation of well defined water-soluble poly(2-methyl-2-oxazoline) and poly(2-ethyl-2-oxazoline) terminally equipped with a chelator (N,N',N '',N"'-tetraazacylododecane-1,4,7,10-tetraacetic acid (DOTA)) for radionuclide labeling. The tissue distribution and excretion of In-111-labeled poly(2-alkyl-2-oxazoline)s were studied in mice. We found that the hydrophilic polymers do not accumulate in tissues and are rapidly cleared from the blood pool, predominantly by glomerular filtration in the kidneys. In contrast only a small fraction is excreted via the hepatobiliary tract. Only minimal amounts of poly(2-alkyl-2-oxazoline)s are taken up by the reticuloendothelial system (RES). Scintigraphic studies revealed the feasibility of in vivo imaging of In-111-labeled poly(2-oxazoline)s. Since additional functionatities for targeting can readily be introduced into poly(2-oxazoline)s via functional monomer units, these compounds fulfill fundamental requirements for an application as carrier molecules in radionuclide therapy. (c) 2007 Elsevier B.V. All rights reserved.