Evaluation of α v β 3 Integrin-Targeted Positron Emission Tomography Tracer 18 F-Galacto-RGD for Imaging of Vascular Inflammation in Atherosclerotic Mice

Abstract

Background— 18F-Galacto-RGD is a positron emission tomography (PET) tracer binding to αvβ3 integrin that is expressed by macrophages and endothelial cells in atherosclerotic lesions. Therefore, we evaluated 18F-galacto-RGD for imaging vascular inflammation by studying its uptake into atherosclerotic lesions of hypercholesterolemic mice in comparison to deoxyglucose. Methods and results— Hypercholesterolemic LDLR−/−ApoB100/100 mice on a Western diet and normally fed adult C57BL/6 control mice were injected with 18F-galacto-RGD and 3H-deoxyglucose followed by imaging with a small animal PET/CT scanner. The aorta was dissected 2 hours after tracer injection for biodistribution studies, autoradiography, and histology. Biodistribution of 18F-galacto-RGD was higher in the atherosclerotic than in the normal aorta. Autoradiography demonstrated focal 18F-galacto-RGD uptake in the atherosclerotic plaques when compared with the adjacent normal vessel wall or adventitia. Plaque-to-normal vessel wall ratios were compa...