Targeted Delivery of Doxorubicin Using Transferrin-Conjugated Carbon Dots for Cancer Therapy.

A transferrin receptor (TfR)-targeted nanodrug [green fluorescence emission carbon dot (GCD)-polyethylene glycol (PEG)-transferrin (Tf)@doxorubicin (Dox)] for cancer therapy was developed by functionalizing GCDs with PEG, Tf, and Dox. GCDs were synthesized by the one-step hydrothermal method, followed by conjugating PEG and Tf by covalent bonds and loading Dox by electrostatic interactions. The nanodrug exhibits high stability under neutral conditions and effectively releases Dox at pH of 5.5. GCD-PEG-Tf@Dox can be selectively internalized by TfR-overexpressed tumor cells (MCF-7 and K150) via receptor-mediated endocytosis and further release Dox to the nuclei. As a result, GCD-PEG-Tf@Dox exhibits significant lethality to tumor cells (MCF-7 and K150) but greatly reduced toxicity to normal cells [Chinese hamster ovary cell line (CHO)] compared with free Dox. In vivo studies have confirmed that GCD-PEG-Tf@Dox can effectively inhibit tumor proliferation with negligible side effects.