<i>In Vivo</i> Platelet Detection Using a Glycoprotein IIb/IIIa-Targeted Near-Infrared Fluorescence Imaging Probe

Abstract

Platelets play a prominent role in multiple diseases, in particular arterial and venous thrombosis and also in atherosclerosis and cancer. To advance the <i>in vivo</i> study of the biological activity of this cell type from a basic experimental focus to a clinical focus, new translatable platelet-specific molecular imaging agents are required. Herein, we report the development of a near-infrared fluorescence probe based upon tirofiban, a clinically approved small-molecule glycoprotein IIb/IIIa inhibitor (GPIIb/IIIa). Through <i>in vitro</i> experiments with human platelets and <i>in vivo</i> ones in a murine model of deep-vein thrombosis, we demonstrate the avidity of the generated probe for activated platelets, with the added benefit of a short blood half-life, thereby enabling rapid <i>in vivo</i> visualization within the vasculature.