Magnetic iron oxide particles coated with carboxydextran for parenteral administration and liver contrasting - Pre-clinical profile of SH U555A
Magnetic iron oxide particles coated with carboxydextran for parenteral administration and liver contrasting - Pre-clinical profile of SH U555A
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DOI：
10.1080/02841859709174391
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发表时间：
1997-07-01
期刊：
影响因子：
1.3
通讯作者：
Weinmann, HJ
中科院分区：
文献类型：
--
作者：
Lawaczeck, R;Bauer, H;Weinmann, HJ
理由和目标：为了评估SH U 555 A的物理和药理学特性，SH U 555 A是一种磁性氧化铁颗粒悬浮液，旨在增强肝脏肿瘤和转移灶的可视化。材料和方法：采用化学和物理方法来表征这些磁性氧化铁颗粒在水溶液中的大小和结构。在小鼠、大鼠和狗中研究了颗粒的生物分布和药代动力学。结果：SH U 555 A颗粒由低分子量羧葡聚糖包被的铁氧化物组成，主要是γ-Fe_2O_3形式，流体动力学直径为57-59 nm，T_2弛豫率为164升·mmol（-1）·s（-1）（水，0.47 T）。在大鼠中，20 μ mol Fe/kg剂量下，颗粒在肝脏中的剂量依赖性半衰期为2 - 3天，较低剂量下的半衰期较短。在大鼠肿瘤模型中，静脉注射SH U 555 A后，肿瘤与肝脏的对比度明显改善。在14 μ mol Fe/kg剂量下，即使在非优化的T1加权自旋回波图像中也能获得半最大对比度效应。SH U 555 A是一种用于静脉给药的超顺磁性MR造影剂，具有很大的肝肿瘤划界潜力。
Rationale and objectives: To evaluate the physical and pharmacological profiles of SH U555A, a suspension of magnetic iron oxide particles that is designed to enhance the visualization of liver tumors and metastases.Material and Methods: Chemical and physical methods were used to characterize the-size and structure of these magnetic iron oxide particles in aqueous solution. The biodistribution and pharmacokinetics of the particles were studied in mice, rats and dogs. The imaging efficacy of the particles was demonstrated by MR imaging in rat liver tumors.Results: The SH U555A particles consist of low-molecular-weight carboxydextrancoated iron oxides predominantly of the gamma-Fe2O3 form with a hydrodynamic diameter ranging from 57-59 nm and strong T2 relaxivity of 164 liters.mmol(-1).s(-1) (water, 0.47 T). In rats the particles exhibited a dose-dependent half-life of between 2 and 3 days in the liver at a dose of 20 mu mol Fe/kg and a shorter half-life at lower doses. No major side effects were found. In a rat tumor model the rumor-to-liver contrast was markedly improved after i.v. administration of SH U555A, At a dose of 14 mu mol Fe/kg the half-maximal contrast-effect was obtained even in nonoptimized T1-weighted spin-echo images.Conclusion: SH U555A is a superparamagnetic MR contrast agent for i.v. administration and has substantial potential for the demarcation of liver tumors.