Nucleus-targeting orange-emissive carbon dots delivery adriamycin for enhanced anti-liver cancer therapy

Abstract

Carbon dots (CDs) with precise targeting function show great potential in the field of drug delivery therapeutics. In this study, the functionalized nucleus-targeting orange-emissive CDs with nuclear localization sequence (NLS) were loaded with adriamycin (DOX) to obtain a nucleus-targeting orange-emissive CDs drug delivery system (CDs-NLS-DOX), which delivered DOX to tumor cell nuclei to enhance its anti-tumor activity. The drug carrier orange-emissive CDs showed excitation-independent behavior, stable and enhanced imaging capability and good biocompatibility in vitro and in vivo. Meanwhile, the CDs-NLS could target the nuclei efficiently, and the CDs-NLS-DOX complexes had a high drug loading rate (59.4%) after loading DOX, exhibiting pH-dependent DOX release behavior through breaking acylhydrazone bond in a weak acidic environment. In addition, the CDs-NLS-DOX complexes exhibited an enhanced killing activity against human hepatoma cells (HepG2). The in vivo therapeutic effects on HepG2 nude mice transplanted tumors indicated the CDs-NLS-DOX had a stronger ability to inhibit tumor growth compared to free DOX. In short, CDs-NLS-DOX is expected to be a precise and efficient nucleus-targeting nano-drug delivery system for tumor treatment.