Dendrimer-based macromolecular MRI contrast agents: characteristics and application.

Dendrimer-based macromolecular MRI contrast agents: characteristics and application.
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DOI:
10.1162/153535003765276237
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发表时间:
2003-01-01
期刊:
影响因子:
2.8
通讯作者:
Brechbiel, Martin W
Brechbiel, Martin W
中科院分区:
医学4区
文献类型:
--
作者:
Kobayashi, Hisataka;Brechbiel, Martin W

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采用相对简单的化学方法制备的许多大分子MRI造影剂可能很容易获得,可以为多种应用提供充分的增强。与CT成像所需的碘浓度相比,这些试剂使用的钆离子浓度大约低100倍。在这里,我们以最近报道的树突基造影剂家族为例,描述了一些大分子MRI造影剂的一般潜在方向。分子大小的改变改变了排泄途径。分子量小于60 kDa的小尺寸造影剂通过肾脏排出,因此这些造影剂可能适合作为功能性肾脏造影剂。发现亲水和较大尺寸的造影剂更适合用作血池造影剂。由聚丙烯胺二氨基丁烷树突状核形成的疏水变体创造了肝脏造影剂。较大的亲水剂可用于淋巴显像。最后,与单克隆抗体或亲和素偶联的造影剂可以作为肿瘤特异性造影剂,也可以用作钆中子捕获治疗或与放射免疫治疗联合的治疗药物。
Numerous macromolecular MRI contrast agents prepared employing relatively simple chemistry may be readily available that can provide sufficient enhancement for multiple applications. These agents operate using a approximately 100-fold lower concentration of gadolinium ions in comparison to the necessary concentration of iodine employed in CT imaging. Herein, we describe some of the general potential directions of macromolecular MRI contrast agents using our recently reported families of dendrimer-based agents as examples. Changes in molecular size altered the route of excretion. Smaller-sized contrast agents less than 60 kDa molecular weight were excreted through the kidney resulting in these agents being potentially suitable as functional renal contrast agents. Hydrophilic and larger-sized contrast agents were found better suited for use as blood pool contrast agents. Hydrophobic variants formed with polypropylenimine diaminobutane dendrimer cores created liver contrast agents. Larger hydrophilic agents are useful for lymphatic imaging. Finally, contrast agents conjugated with either monoclonal antibodies or with avidin are able to function as tumor-specific contrast agents, which also might be employed as therapeutic drugs for either gadolinium neutron capture therapy or in conjunction with radioimmunotherapy.