镓/镓-68与N-乙烯基吡咯烷酮、N-乙烯基甲酰胺和N-乙烯基亚氨基二乙酸共聚物的金属-聚合物配合物：水溶性合成柔性链大分子放射性标记的线索

Metal-Polymer Complexes of Gallium/Gallium-68 with Copolymers of N-Vinylpyrrolidonewith N-Vinylformamideand N-Vinyliminodiacetic Acid: A Hint for Radiolabeling of Water-Soluble Synthetic Flexible Chain Macromolecules.

作者信息

Gorshkov N I, Murko А Yu, Gavrilova I I, Bezrukova М А, Kipper А I, Shatik S V, Tokarev А V, Krasikov V D, Panarin Е F

机构信息

Federal State Budgetary Institution of Science Institute of Macromolecular Compounds, Russian Academy of Sciences (IMC RAS), Russian Federation, V.O. Bolshoy pr. 31, 199004 Saint Petersburg, Russia.

Federal State Budgetary Institution "Russian Research Center for Radiology and Surgical Technologies" of the Ministry of Health of the Russian Federation, Russian Federation, p. Pesochny, ul. Leningradskaya, 70, 197758 Saint Petersburg, Russia.

出版信息

Polymers (Basel). 2020 Dec 2;12(12):2889. doi: 10.3390/polym12122889.

DOI:10.3390/polym12122889

PMID:33276572

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7761557/

Abstract

Copolymer of N-vinylpyrrolidone (VP) with vinylformamide (VFA) and N-vinyliminodiacetic acid (VIDA) was synthesized; its metal-polymer complexes (MPCs) with gallium were obtained. The complexes were characterized by size exclusion chromatography, hydrodynamic and optical methods, scanning electron microscopy, and spectral methods (UV, IR, Н NMR spectroscopy). It was demonstrated that in going from polymer to complex, hydrodynamic parameters of macromolecules change only slightly, although the polymer contains intramolecular Ga(VIDA) fragments in its structure. A new method for preparation of MPCs with gallium and gallium-68 radionuclide was suggested. The obtained metal-polymer complex is stable over a wide range of pH values as well as in the histidine challenge reaction. In vivo distribution experiments in intact animals showed high primary accumulation of thegallium-68 MPC in blood with subsequent excretion via urinary tract.

摘要

合成了N-乙烯基吡咯烷酮（VP）与乙烯基甲酰胺（VFA）和N-乙烯基亚氨基二乙酸（VIDA）的共聚物；获得了其与镓的金属-聚合物配合物（MPC）。通过尺寸排阻色谱法、流体动力学和光学方法、扫描电子显微镜以及光谱方法（紫外、红外、核磁共振光谱）对配合物进行了表征。结果表明，尽管聚合物结构中含有分子内Ga(VIDA)片段，但从聚合物到配合物的过程中，大分子的流体动力学参数变化很小。提出了一种制备含镓和镓-68放射性核素的MPC的新方法。所获得的金属-聚合物配合物在很宽的pH值范围内以及在组氨酸激发反应中都很稳定。在完整动物体内的分布实验表明，镓-68 MPC在血液中具有较高的初始蓄积，随后通过泌尿系统排泄。