Luqian Deng, Peng Zhang, Xian Qin, Linghan Tang, Ruonan Liu, Fanghan Li, Jiangwei Xiao, Maoru Zhao
KRAS mutations drive poor outcomes in colorectal cancer (CRC), largely by conferring resistance to radiotherapy. In clinical samples, we trace this resistance to an upregulated SLC7A11/GPX4 axis, a defense that shields cancer cells from ferroptosis. Targeting this pathway to re-enable ferroptosis, therefore, represents a rational strategy to restore radiosensitivity. Sulfasalazine (SAS), an FDA-approved drug, inhibits SLC7A11 and induces ferroptosis, but its clinical application is restricted by systemic toxicity and poor tumor accumulation. To bypass these limitations, we develop multifunctional SAS-loaded hafnium oxide nanoparticles (HfO2@SAS). Ultra-small HfO2@SAS enables efficient local drug retention and subsequent clearance, minimizing long-term retention risks and supporting favorable biocompatibility. HfO2@SAS serves a dual function: HfO2 amplifies radiotherapy via physical radiosensitization through X-ray energy deposition, while SAS disables antioxidant defenses to induce ferroptosis. In KRAS-mutant CRC, this nanoplatform overcomes radioresistance by integrating physical and biochemical mechanisms. Consistent with clinical sample data, we validate the efficacy of HfO2@SAS in cell and animal levels. Patient-derived organoids provide a human-relevant platform that further supports these findings. Collectively, these findings validate the potential of nanomedicine in combating refractory KRAS-mutant CRC and provide a proof-of-concept for advancing radio-drug combination therapy.