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Considering the intrinsic complexity of cancer, the emergence of multifunctional nanocarriers provides more possibilities for cancer therapy. Herein, a novel multifunctional nanocarrier (g-CNQDs–PEG–RGD) is successfully developed by covalently grafting graphitic-C3N4 quantum dots (g-CNQDs) with arginine–glycine–aspartic acid (RGD) via diamine-terminated oligomeric polyethylene glycol (PEG). The functionalization of g-CNQDs with PEG and RGD imparts the nanocomposite with low cytotoxicity, excellent physiological stability and specific targeting ability toward cancer cells with the αvβ3 receptor. The widely used fluorescent antineoplastic anthracycline drug doxorubicin (DOX) is non-covalently loaded onto g-CNQDs–PEG–RGD. It is advantageous that the g-CNQDs–PEG–RGD–DOX nano-assembly exhibits enhanced cellular uptake by HepG2 cells, which overexpress integrin αvβ3 receptors. Thus, the enhanced targeting specificity and intracellular acid condition-triggered drug release promise excellent therapeutic effects. Meanwhile, the inherent stable fluorescence of g-CNQDs–PEG–RGD and DOX enables real-time monitoring of cellular uptake of the g-CNQDs–PEG–RGD–DOX nano-assembly, consequent release of DOX and the fate of the carrier. These findings demonstrate that g-CNQDs–PEG–RGD–DOX will be promising for high treatment efficacy with minimal side effects in future therapy. [ABSTRACT FROM AUTHOR]

• A drug delivery system based on fluorescent MoS 2 QDs is synthesized. • PEGylated MoS 2 QDs has good physiological stability and is suitable for carrier. • The drug delivery system is traceable and exhibits pH-responsive release property. Since low pH value is widely observed in most of solid tumors, pH-responsive drug delivery system (DDS) can provide a general strategy for tumor-targeting therapy. In this work, a traceable and pH-responsive DDS (MoS 2 -PEG-DOX) based on MoS 2 quantum dots (MoS 2 QDs) is successfully developed by covalently grafting MoS 2 QDs with diamine-terminated oligomeric polyethylene glycol (PEG) and then loading with a fluorescent antineoplastic anthracycline drug, doxorubicin (DOX). The functionalization of MoS 2 QDs with PEG imparts the nanocomposite with strong blue photoluminescence, low cytotoxicity, and excellent physiological stability. The MoS 2 -PEG-DOX nano-assembly can be effectively taken up by U251 cells, and an accelerated DOX release is then triggered by intracellular acid condition, which in turn diminishing unwanted side effects derived by the incorporation of DOX into healthy cells. Meanwhile, the cellular uptake of the MoS 2 -PEG-DOX nano-assembly, consequent DOX release and the localization of nanocarrier can be real-time monitored due to the inherent stable fluorescence of MoS 2 -PEG and DOX. These findings demonstrate that MoS 2 -PEG-DOX will be promising for high treatment efficacy with minimal side effects in future therapy. [ABSTRACT FROM AUTHOR]