Abstract: Objective: To address the inherent limitations of conventional chemotherapeutic agents, including low drug loading efficiency and a lack of light-controllable cytotoxicity, we developed a self-delivering, dual-functional nanodrug of CQ-GA-Fe NPs integrating chemodynamic therapy（CDT） and photodynamic therapy（PDT）, assembled via Fe²⁺-mediated coordination using phosphorylated glycyrrhetinic acid（GA-P） as the ligand and phosphorylated carbazole-quinoline hexanol（CQ-P） as the photosensitizer, and the platform was preliminarily evaluated for its potential in the treatment of hepatocellular carcinoma. Methods: Key intermediates were synthesized via nucleophilic substitution and condensation reactions. Subsequently, CQ-GA-Fe NPs were prepared through ion-coordination self-assembly and characterized using proton nuclear magnetic resonance spectroscopy（1H-NMR） and Fourier-transform infrared spectroscopy（FT-IR）. The pH-responsive drug release behavior was evaluated using dialysis method. The generation of hydroxyl radicals（·OH） and singlet oxygen（¹O₂） was detected by methyl violet degradation and ABDA probe, respectively. Hemolysis assay was performed to evaluate its hemocompatibility. Cell counting kit-8（CCK-8） assay was used to detect its cytotoxicity against HepG2 and L02 cells and DCFH-DA fluorescent probe was adopted to measure the levels of intracellular reactive oxygen species（ROS）. Results: The as-prepared CQ-GA-Fe NPs exhibited an average particle size of（202.0±1.6） nm, an average polydispersity index（PDI） of（0.130±0.029）, and an average zeta potential of（-23.93±0.23） mV. In addition, they demonstrated pH-responsive drug release behavior. Within 96 h, their average cumulative release rate at pH 6.8 reached（53.90%±3.14%）, which was markedly higher than that at pH 7.4（37.98%±0.90%）. Furthermore, CQ-GA-Fe NPs could generate ¹O₂ and ·OH. In vitro experiments revealed that CQ-GA-Fe NPs exhibited negligible cytotoxicity toward normal L02 hepatocytes but exerted selective cytotoxicity against HepG2 cells through a strong synergistic effect of CDT and PDT（combination index CI<0.16）, with an IC₅₀ value of 12.46 μg/mL. Conclusion: The constructed CQ-GA-Fe NPs demonstrate excellent biocompatibility and light-controlled selective cytotoxicity against hepatocellular carcinoma cells. Through the strong synergistic effect of CDT and PDT, the constructed CQ-GA-Fe NPs induce intracellular ROS accumulation in the hepatocellular carcinoma cells and exert anti-tumor effects via oxidative stress, thus providing experimental evidence and theoretical references for multimodal synergistic therapy of hepatocellular carcinoma.