Department of Radiology, Innsbruck Medical University, 6020 Innsbruck, Austria.
Histochem Cell Biol. 2010 Aug;134(2):171-96. doi: 10.1007/s00418-010-0726-6. Epub 2010 Jul 14.
We are developing a nanoparticulate histochemical reagent designed for histochemistry in living animals (molecular imaging), which should finally be useful in clinical imaging applications. The iterative development procedure employed involves conceptual design of the reagent, synthesis and testing of the reagent, then redesign based on data from the testing; each cycle of testing and development generates a new generation of nanoparticles, and this report describes the synthesis and testing of the third generation. The nanoparticles are based on human serum albumin and the imaging modality selected is magnetic resonance imaging (MRI). Testing the second particle generation with newly introduced techniques revealed the presence of impurities in the final product, therefore we replaced dialysis with diafiltration. We introduced further testing methods including thin layer chromatography, arsenazo III as chromogenic assay for gadolinium, and several versions of polyacrylamide gel electrophoresis, for physicochemical characterisation of the nanoparticles and intermediate synthesis compounds. The high grade of chemical purity achieved by combined application of these methodologies allowed standardised particle sizes to be achieved (low dispersities), and accurate measurement of critical physicochemical parameters influencing particle size and imaging properties. Regression plots confirmed the high purity and standardisation. The good degree of quantitative physicochemical characterisation aided our understanding of the nanoparticles and allowed a conceptual model of them to be prepared. Toxicological screening demonstrated the extremely low toxicity of the particles. The high magnetic resonance relaxivities and enhanced mechanical stability of the particles make them an excellent platform for the further development of MRI molecular imaging.
我们正在开发一种用于活体动物组织化学(分子成像)的纳米颗粒组织化学试剂,该试剂最终将在临床成像应用中发挥作用。所采用的迭代开发过程涉及试剂的概念设计、试剂的合成和测试,然后根据测试数据进行重新设计;每个测试和开发周期都会生成新一代的纳米颗粒,本报告描述了第三代的合成和测试。这些纳米颗粒基于人血清白蛋白,所选的成像方式是磁共振成像(MRI)。使用新引入的技术测试第二代颗粒时,发现最终产品中存在杂质,因此我们用切向流过滤代替了透析。我们引入了进一步的测试方法,包括薄层层析、用于检测钆的偶氮 III 显色测定法,以及几种版本的聚丙烯酰胺凝胶电泳,用于纳米颗粒和中间合成化合物的物理化学特性分析。这些方法的综合应用达到了很高的化学纯度水平(低分散度),并能准确测量影响颗粒大小和成像性能的关键物理化学参数。回归图证实了高纯度和标准化。良好的定量物理化学特性分析有助于我们理解纳米颗粒,并为它们准备了一个概念模型。毒理学筛选证明了这些颗粒的极低毒性。这些颗粒具有高磁共振弛豫率和增强的机械稳定性,使它们成为进一步开发 MRI 分子成像的绝佳平台。