Non-small cell lung cancer (NSCLC) is a prevalent form of lung cancer, primarily including adenocarcinomas and squamous cell carcinomas. Advances in targeted therapies have significantly improved NSCLC treatment. In this study, we developed a multifunctional fluorescent imaging nanodrug delivery system using fructose as a natural cross-linker due to its biocompatibility and low toxicity. The incorporation of zinc phthalocyanine-perfluorinated resin (ZnPc-PFR) into chitosan-fructose (CH-Fru) resulted in a nanocomposite with superior fluorescent properties and high loading capacity for compound 1, creating CH-Fru@ZnPc-PFR@1. Furthermore, the combination of compound 1 and gefitinib formed the CH-Fru@ZnPc-PFR@1@Gefitinib composite system, which demonstrated a synergistic effect in inhibiting NSCLC cell proliferation. This study not only developed an effective nanodrug delivery system but also highlighted the potential therapeutic benefits of combining compound 1 with gefitinib for lung cancer treatment.