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微泡造影剂:靶向超声成像及超声辅助药物递送应用

Microbubble contrast agents: targeted ultrasound imaging and ultrasound-assisted drug-delivery applications.

作者信息

Klibanov Alexander L

机构信息

Department of Internal Medicine, Cardiovascular Division, University of Virginia, Charlottesville, Virginia 22908-0158, USA.

出版信息

Invest Radiol. 2006 Mar;41(3):354-62. doi: 10.1097/01.rli.0000199292.88189.0f.

Abstract

The use of microbubble contrast agents for general tissue delineation and perfusion enjoys steady interest in ultrasound imaging. Microbubbles as contrast materials require a small dosage and show excellent detection sensitivity. Targeting ligands on the surface of microbubbles permit the selective accumulation of these particles in the areas of interest, which show an up-regulated level of receptor molecules on vascular endothelium. Selective contrast imaging of inflammation, ischemia-reperfusion injury, angiogenesis, and thrombosis has been achieved in animal models. Ultrasound-assisted drug delivery and activation, performed by combining microbubble agent containing drug substances or coadministered with pharmaceutical agents (including plasmid DNA for transfection), has been achieved in multiple model systems in vitro and in vivo. Ultrasound and microbubbles-based targeted acceleration of the thrombolytic enzyme action already have reached clinical trials. Overall, microbubble targeting and ultrasound-assisted microbubble-based drug-delivery systems will offer a step toward the application of targeted personalized diagnostics and therapy.

摘要

将微泡造影剂用于一般组织的描绘和灌注在超声成像领域一直备受关注。作为造影剂的微泡所需剂量小,检测灵敏度高。微泡表面的靶向配体可使这些颗粒在感兴趣区域选择性积聚,这些区域的血管内皮上受体分子水平上调。在动物模型中已实现对炎症、缺血再灌注损伤、血管生成和血栓形成的选择性造影成像。通过将含有药物物质的微泡剂与药物制剂(包括用于转染的质粒DNA)联合使用或共同给药,在多个体外和体内模型系统中已实现超声辅助药物递送和激活。基于超声和微泡的溶栓酶作用靶向加速已进入临床试验阶段。总体而言,微泡靶向和基于超声辅助微泡的药物递送系统将朝着靶向个性化诊断和治疗的应用迈出一步。

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