Synergistic Effect of Human Serum Albumin and Fullerene on Gd-DO3A for Tumor-Targeting Imaging

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• 作者：Ying Zhang ; Toujun Zou ; Mirong Guan ; Mingming Zhen ; Daiqin Chen ; Xiangping Guan ; Hongbin Han ; Chunru Wang ; Chunying Shu
• 刊名：ACS Applied Materials & Interfaces
• 出版年：2016
• 出版时间：May 11, 2016
• 年：2016
• 卷：8
• 期：18
• 页码：11246-11254
• 全文大小：613K
• 年卷期：0
• ISSN：1944-8252

文摘

A macromolecular magnetic resonance imaging (MRI) contrast agent was successfully synthesized by conjugating the gadolinium/1,4,7,10-tetraazacyclododecane-1,4,7-tetracetic acid complex (Gd-DO3A) with 6,6-phenyl-C₆₁ butyric acid (PC₆₁BA) and upon further modification with human serum albumin (HSA). The final product, PC₆₁BA-(Gd-DO3A)/HSA, has a high stability and exhibits a much higher relaxivity (r₁ = 89.1 mM^–1 s^–1 at 0.5 T, 300 K) than Gd-DO3A (r₁ = 4.7 mM^–1 s^–1) does under the same condition, producing the synergistic positive effect of HSA and C₆₀ on the relaxivity of Gd-DO3A. The in vivo MR images of PC₆₁BA-(Gd-DO3A)/HSA-treated tumor-bearing mice show strong signal enhancement for the tumor area due to the enhanced permeability and retention effect. The maximum accumulation of PC₆₁BA-(Gd-DO3A)/HSA at the tumor site was achieved at 4 h postinjection, which may guide surgery. The results from the hematology and histological observations indicate that PC₆₁BA-(Gd-DO3A)/HSA has no obvious toxicity in vivo. These unique properties of PC₆₁BA-(Gd-DO3A)/HSA enable them to be highly efficient for tumor-targeting MRI in vivo, possibly providing a good solution for tumor diagnosis.