Study of biodistribution and systemic toxicity of glucose functionalized SPIO/DOX micelles

AbstractThe present study examined the cytotoxicity and magnetic resonance imaging (MRI) distribution of cancer-targeted, MRI-visible polymeric micelles that encapsulate doxorubicin (DOX) and superparamagnetic iron oxide (SPIO) and are conjugated with glucose as a targeting ligand. In this study, the micelles were characterized by dynamic light scattering to determine particle size and zeta potential. Morphology and structure of the micelles were evaluated by transmission electron microscopy. To investigate the clinical potential of glucose-micelles, in vitro cytotoxicity assays of nonencapsulating or SPIO-and-DOX–coencapsulating micelles were performed on L929 mouse fibroblasts, and we found that glucose-micelles did not exert in vitro cytotoxic effects. Next, in vitro MRI detectability of glucose SPIO micelles was evaluated at the loaded SPIO content of 2.5% and 50%, and it was found that glucose-micelles can increase MRI relaxivity (R2*) at high SPIO loading. Furthermore, 50% SPIO micelles persisted in...