Highly sensitive and safe contrast agents (CAs) are essential for magnetic resonance imaging (MRI) to achieve accurate tumor detection and imaging. Dendrimer-based macromolecular MRI contrast agents are advantageous owing to their tumor-targeting ability, enhanced imaging contrast and enlarged imaging window. However, most of them have drawbacks of non-degradability and thereby long-term retention in body and toxicity. Herein, a tumor-targeting biodegradable dendritic CA (DCA) (FA-PEG-G2-DTPA-Gd) was prepared from a polyester dendrimer conjugated with gadolinium (Gd) chelates and PEG chains with distal folic acid. The DCA had a high longitudinal relaxivity up to 17.1mM(-1)s(-1), 4 times higher than the clinically used CA Magnevist. The MRI contrasted by FA-PEG-G2-DTPA-Gd outlined the inoculated tumor more clearly, and had much higher contrast enhancement for a much longer time than Magnevist. More importantly, the biodegradable FA-PEG-G2-DTPA-Gd gave much less Gd retentions in all the organs or tissues than non-degradable DCAs. Thus, the high efficiency in MRI contrast enhancement and low Gd retention merit it a promising CA for contrast enhanced tumor MRI.
Copyright © 2013 Elsevier B.V. All rights reserved.