High drug-loading system of hollow carbon dots-doxorubicin: preparation, in vitro release and pH-targeted research

Hollow carbon dots (HCDs), as drug carriers, and doxorubicin (DOX), as a model drug, were selected to prepare a HCDs-DOX-loading system. First, HCDs were prepared by a hydrothermal method and characterized by transmission electron microscopy (TEM), powder X-ray diffraction (PXRD), and nuclear magnetic resonance (¹³C NMR), UV-vis absorption, Fourier-transform infrared (FT-IR) and X-ray photoelectron spectroscopies (XPS). The HCDs were then used to load DOX. The drug-loading system of HCDs-DOX was characterized by zeta potential measurements, and UV-vis absorption and fluorescence spectroscopies. We then studied the drug loading, formation mechanism, cytotoxicity, in vitro release and pH-targeted properties. HCDs-DOX was found to have a high drug (DOX)-loading ratio (∼42.9%) and better sustained pH targeted-release and lower cytotoxicity than those of DOX. In the HCDs-DOX system, interactions between the HCDs and DOX were electrostatic resulting in the formation of -N[double bond, length as m-dash]C-via the coupling of -NH₂ (on HCDs) and -C[double bond, length as m-dash]O (on DOX). In vitro release of HCDs-DOX conformed to the Weibull model and Fick diffusion, consistent with that of free DOX. We report, for the first time, that the: (i) functional groups on the HCD surfaces (not their hollow structure) play a key role in drug loading; (ii) the carrier (HCDs) did not change the in vitro release model or mechanism of DOX before and after loading by the HCDs.