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Radioiodinated Portable Albumin Binder as a Versatile Agent for in Vivo Imaging with Single-Photon Emission Computed Tomography
Molecular Pharmaceutics ( IF 4.9 ) Pub Date : 2019-01-03 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b01116
Xuejun Wen 1 , Changrong Shi 1 , Duo Xu 1 , Pu Zhang 1 , Zizhen Li 2 , Jindian Li 1 , Xinhui Su 3 , Rongqiang Zhuang 1 , Ting Liu 1 , Zhide Guo 1 , Xianzhong Zhang 1
Affiliation  

In this study, radioiodinated 4-(p-iodophenyl)butyric acid ([131I]IBA) was synthesized and evaluated as a portable albumin-binder for potential applications in single photon emission computed tomography imaging of blood pool, tumor, and lymph node with significantly improved pharmacokinetic properties. The [131I]IBA was prepared under the catalyst of Cu2O/1,10-phenanthroline. After that, the albumin-binding capability of [131I]IBA was tested in vitro, ex vivo, and in vivo, respectively. [131I]IBA was obtained with very high radiolabeling yield (>99%) and good radiochemical purity (>98%) within 10 min. It binds to albumin effectively with high affinity (IC50= 46.5 μM) and has good stability. The results of biodistribution indicated that the [131I]IBA was mainly accumulated in blood with good retention (10.51 ± 2.58%ID/g at 30 min p.i. and 4.63 ± 0.17%ID/g at 4 h p.i.). In the SPECT imaging of mice models with [131I]IBA, blood pool, lymph node, and tumors could be imaged clearly with high target-to-background ratio. Overall, the radioiodinated albumin binder of [131I]IBA with long blood half-life and excellent stability could be used to decorate diversified albumin-binding radioligands and developed as a versatile theranostic agent.

中文翻译:

放射性碘化的便携式白蛋白结合剂,是一种具有单光子发射计算机断层扫描技术的体内成像多功能试剂

在这项研究中,合成了放射性碘化的4-(碘苯基)丁酸([ 131 I] IBA),并作为便携式白蛋白结合剂进行了评估,有望在血池,肿瘤和淋巴结的单光子发射计算机断层成像中应用具有显着改善的药代动力学特性。[ 131 I] IBA是在Cu 2 O / 1,10-菲咯啉的催化剂下制备的。之后,分别在体外离体体内测试了[ 131 I] IBA的白蛋白结合能力。[ 131I] IBA在10分钟内具有很高的放射标记产率(> 99%)和良好的放射化学纯度(> 98%)。它以高亲和力有效结合白蛋白(IC 50 = 46.5μM),并具有良好的稳定性。生物分布结果表明,[ 131 I] IBA主要在血液中富集并具有良好的保留(在pi 30分钟时为10.51±2.58%ID / g,在pi 4 h时为4.63±0.17%ID / g)。在具有[ 131 I] IBA的小鼠模型的SPECT成像中,可以以高的目标背景比清楚地成像血池,淋巴结和肿瘤。总体而言,[ 131I] IBA具有长的血液半衰期和出色的稳定性,可用于装饰多种与白蛋白结合的放射性配体,并已发展成为一种多功能的治疗剂。
更新日期:2019-01-03
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