A dual-targeted Gd-based contrast agent for magnetic resonance imaging in tumor diagnosis

Enhanced magnetic resonance imaging (MRI) has important clinical value in the diagnosis of tumors. Much effort has been made to improve the relaxivity and specificity of contrast agents (CAs) in tumor diagnosis over the past few decades. However, there is still a lack of CAs which not only enhance the signal intensity of tumors rather than surrounding tissues in MRI but also maintain a high signal intensity prolonged for a long time. Herein, we synthesized a dual-targeted CA, RGD-(DOTA-Gd)-TPP (RDP), in which RGD is used to target the alpha v beta 3 integrin receptor overexpressed in tumor cells and TPP is used to bind to a mitochondrion further. The structure of RDP was characterized and its properties, such as relaxivity and biosafety, were measured and in vitro and in vivo MRI assays were carried out. It has been proven that RDP has higher relaxivity of aqueous solution than Magnevist used in clinics. Moreover, RDP achieved higher signal intensity and a longer signal duration in tumor imaging. Therefore, RDP can be applied as the potential dual-targeted MRI CA for clinical tumor diagnosis. A dual-targeted contrast agent, RGD-(DOTA-Gd)-TPP (RDP), was synthesized, in which RGD is used to target the alpha v beta 3 integrin receptor overexpressed in tumor cells and TPP is used to bind to a mitochondrion further.