iRGD-decorated red shift emissive carbon nanodots for tumor targeting fluorescence imaging.

Carbon nanodots (CDs) have been exhibiting increasing applications owing to their luminescence properties and biocompatibility as imaging probes in diagnosis. However, poor tumor targeting and penetration of CDs is still the biggest challenge limiting their tumor imaging efficacy. To improve the tumor targeting and penetration efficiency of CDs, we developed an active tumor targeting imaging system by simply fabricating a tumor-homing penetration peptide iRGD (CRGDKGPDC) to red shift emissive CDs (iRGD-CDs) with a physical method. Particularly, iRGD-CDs showed a small size and red shift fluorescence signals as CDs, which made iRGD-CDs suitable for in vivo fluorescence imaging. iRGD-CDs showed higher cellular uptake in vitro, while presented higher penetration and accumulation in tumor tissue in vivo, leading to better tumor imaging efficacy. In conclusion, decoration with iRGD could significantly increase the permeability of CDs in tumor vessels and tumor tissue, generating more CDs leaking out from tumor vasculature, consequently improving the sensitivity of tumor imaging.