School of Material Science and Engineering, Wuhan Institute of Technology, Wuhan 430074, China.
Pharm Res. 2010 Sep;27(9):1884-92. doi: 10.1007/s11095-010-0187-6. Epub 2010 Jun 18.
The aim was to investigate three dextran gadolinium complexes Dextran-DTPA-Gd as the potential MRI contrast agents in lymphatic system.
Three dextran gadolinium complexes Dextran-DTPA-Gd containing differing amounts of Gd-DTPA were synthesized by the incorporation of Gd-DTPA to the hydroxyl groups of dextran. These dextran ligands and gadolinium complexes were characterized, and their properties in vitro and in vivo were also evaluated.
Dextran-DTPA-Gd demonstrated obviously higher relaxation effectiveness than that of Gd-DTPA. The result of in vitro cytotoxicity assay showed that these macromolecular ligands and their corresponding gadolinium complexes had low cytotoxicity to HeLa cells. Dextran-DTPA-Gd greatly enhanced the contrast of MR images of normal politeal lymph nodes and reactive hyperplasia of politeal lymph nodes in rabbits and provided prolonged duration in lymphatic system with lower injection doses than that of Gd-DTPA. However, Dextran-DTPA-Gd displayed low signal enhancements in MR images of politeal lymph nodes with VX2 carcinoma in rabbits during the detection time.
These dextran gadolinium complexes Dextran-DTPA-Gd can be taken up selectively by lymphatic system and showed the potential as MRI contrast agents in lymphatic system.
研究三种葡聚糖钆配合物 Dextran-DTPA-Gd 作为潜在的磁共振成像(MRI)淋巴系统造影剂。
通过将 Gd-DTPA 掺入葡聚糖的羟基,合成了三种含有不同量 Gd-DTPA 的葡聚糖钆配合物 Dextran-DTPA-Gd。对这些葡聚糖配体和钆配合物进行了表征,并评估了它们的体外和体内性能。
Dextran-DTPA-Gd 表现出明显更高的弛豫效能,比 Gd-DTPA 更高。体外细胞毒性试验结果表明,这些高分子配体及其相应的钆配合物对 HeLa 细胞的细胞毒性较低。Dextran-DTPA-Gd 极大地增强了正常兔膝关节淋巴结和膝关节淋巴结反应性增生的 MRI 图像对比度,并以较低的注射剂量在淋巴系统中提供了更长的持续时间,比 Gd-DTPA 更长。然而,在检测时间内,Dextran-DTPA-Gd 在兔膝关节淋巴结 VX2 癌中显示出 MRI 图像的低信号增强。
这些葡聚糖钆配合物 Dextran-DTPA-Gd 可以被淋巴系统选择性摄取,并显示出作为淋巴系统 MRI 造影剂的潜力。