Kobayashi Hisataka, Brechbiel Martin W
Center for Cancer Research, National Cancer Institute, National Institutes of Health, Building 10, Room 4N109, 10 Center Drive, Bethesda, MD 20892-1374, USA.
Mol Imaging. 2003 Jan;2(1):1-10. doi: 10.1162/15353500200303100.
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.
利用相对简单的化学方法制备的众多大分子磁共振成像(MRI)造影剂可能很容易获得,这些造影剂可为多种应用提供足够的增强效果。与CT成像中使用的碘的必要浓度相比,这些造影剂使用的钆离子浓度大约低100倍。在此,我们以我们最近报道的基于树枝状聚合物的造影剂家族为例,描述大分子MRI造影剂的一些一般潜在发展方向。分子大小的变化改变了排泄途径。分子量小于60 kDa的较小尺寸造影剂通过肾脏排泄,这使得这些造影剂有可能适合作为功能性肾造影剂。发现亲水性和较大尺寸的造影剂更适合用作血池造影剂。由聚丙基亚胺二氨基丁烷树枝状聚合物核形成的疏水性变体产生肝脏造影剂。较大的亲水性造影剂可用于淋巴成像。最后,与单克隆抗体或抗生物素蛋白偶联的造影剂能够作为肿瘤特异性造影剂发挥作用,它们也可能被用作钆中子俘获疗法或与放射免疫疗法联合使用的治疗药物。