Herein, a pH and redox dual-responsive drug delivery system (CDs-Pt(iv)-PEG) was developed based on fluorescence carbon dots (CDs). In this system, cisplatin(iv) prodrug (Pt(iv)) was selected as a model drug to reduce toxic side effects. The aldehyde-functionalized monomethoxy polyethylene glycol (mPEG-CHO) was conjugated to CDs-Pt(iv) to form pH sensitive benzoic imine bond. Owing to the slightly acidic tumor extracellular microenvironment (pH 6.8), the benzoic imine bond was then hydrolyzed, leading to charge reversal and decrease in the hydration radius of the drug-carrying, which facilitated in vivo circulation and tumor targeting. Notably, the cytotoxicity of the drug delivery system on cancer cells was comparable to that of cisplatin, while the side effects on normal cells were significantly reduced. In addition, the system realized recognition of cancer cells by the high-contrast fluorescent imaging. In conclusion, the CDs-Pt(iv)-PEG system provided a promising potential for effective delivery of anticancer drugs and cancer cells screening.
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