High relaxivity trimetallic nitride (Gd3N) metallofullerene MRI contrast agents with optimized functionality.
High relaxivity trimetallic nitride (Gd3N) metallofullerene MRI contrast agents with optimized functionality.
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DOI:
10.1021/bc900375n
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发表时间:
2010-04-21
影响因子:
4.7
通讯作者:
Dorn, Harry C.
中科院分区:
文献类型:
--
作者:
Zhang, Jianfei;Fatouros, Panos P.;Shu, Chunying;Reid, Jonathan;Owens, Lesley Shantell;Cai, Ting;Gibson, Harry W.;Long, Gary L.;Corwin, Frank D.;Chen, Zhi-Jian;Dorn, Harry C.
The water soluble poly(ethylene glycol) (PEG) functionalized and hydroxylated endohedral trimetallic nitride metallofullerene derivatives, Gd3N@C80[DiPEG(OH)x], have been synthesized and characterized. The 1H MRI relaxivities in aqueous solution were measured for the derivatives with four different molecular weights of PEG (350–5000 Da) at 0.35 T, 2.4 T and 9.4 T. The 350/750 Da PEGs derivatives were found to have the highest relaxivities values among the derivatives, 237/232 mM−1s−1 for r1 and 460/398 mM−1s−1 for r2 (79/77 mM−1s−1 and 153/133 mM−1s−1 based on Gd3+ ion) respectively, at a clinical-range magnetic field of 2.4 T. These represent some of the highest relaxivities reported in the literatures for any commercial or investigational MRI contrast agent. Dynamic light scattering results confirm a larger size distribution for 350/750 Da PEGs derivatives (95/96 nm) relative to longer chain length derivatives, 5000 Da PEG derivatives (37nm). Direct infusion of the optimized 350 Da PEG derivatives into live tumor-bearing rat brains demonstrated an initial uniform distribution and hence, the potential for effective brachytherapy applications when the encapsulated Gd3+ ions are replaced with radioactive 177Lu.
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