Dendritic polylysine based ανβ3 integrin targeted probe for near-infrared fluorescent imaging of glioma

The difficulty in identifying tumor tissues from healthy brain tissues is a major challenge for the accurate resection of glioma in clinical practice. Many efforts have been made to develop targeting probes to precisely visualize and resect glioma. However, most of these probes are hindered by non-degradation, intolerable toxicity, complicated and costly preparation procedures. In this work, we report an alpha nu beta 3 integrin-targeted near-infrared (NIR) fluorescent probe DP-RGD for detection of glioma. Considering its well-defined structure, good biodegradability, and biocompatibility, dendritic polylysine (DP) is selected as the carrier which is conjugated with a glioma-targeting ligand c(RGDyK) and NIR fluorescent dye IR783. The diameter of the targeted probe DPRGD can be well controlled in a range of 10-20 nm. Cytotoxicity and histological analysis demonstrated that the probe possesses good biocompatibility. NIR fluorescent imaging studies indicated that this probe possessed high tumor targeting efficiency and precisely visualized the glioma xenograft with a high tumor to normal tissue signal ratio. Above all, the alpha nu beta 3 integrin-targeted probe DP-RGD shows great promise for noninvasively and precisely visualizing glioma and holds the possibility for NIR fluorescent imaging-guided glioma resection.