Carbon dots (Cdots) are known as photosensitizers in which the nitrogen doping is able to improve the oxygen-photosensitization performance and singlet-oxygen generation. Herein, the characteristics of nanoconjugates of nitrogen-doped Cdots and doxorubicin were compared with the property of nitrogen-doped Cdots alone. The investigation was performed for the evaluation of pH-dependent zeta potential, quantum yield, photosensitization efficiency and singlet-oxygen generation, besides spectroscopy (UV-visible absorption and fluorescence spectra) and cytotoxicity on cancer model (HeLa cells). Encapsulation efficiency, drug loading, and drug release without and with light irradiation were also carried out. These investigations were always pursued under the comparison among different nitrogen amounts (ethylenediamine/citric acid = 1-5) in Cdots, and some characteristics strongly depended on nitrogen amounts in Cdots. For instance, surface charge, UV-visible absorbance, emission intensity, quantum yield, photosensitization efficiency and singlet-oxygen generation were most effective at ethylenediamine/citric acid = 4. Moreover, strong conjugation of DOX to Cdots via π-π stacking and electrostatic interactions resulted in a high carrier efficiency and an effective drug loading and release. The results suggested that nitrogen-doped Cdots can be considered promising candidates to be used in a combination therapy involving photodynamic and anticancer strategies under the mutual effect with DOX.
Keywords: drug delivery; nitrogen-doping carbon dot; oxygen photosensitization; photodynamic therapy; singlet-oxygen generation.