In this study, zinc oxide nanoparticles (ZnO‐NPs) are synthesized and combined with chitosan (Cs) to create Cs/ZnO‐NPs nanomicelles, aiming to investigate their potential as a novel cancer treatment. The ZnO‐NPs are produced through a sintering process at temperatures ranging from 300 to 700 °C. The most effective nanoparticles are obtained at 600 °C, as determined by X‐ray diffraction (XRD) and Fourier‐transform infrared spectroscopy (FTIR) analyses, which confirmed their crystallinity and purity. Transmission electron microscopy (TEM) and scanning electron microscopy (SEM) are employed to characterize the size and shape of the nanoparticles, revealing predominantly spherical and hexagonal structures with stable dimensions. The cytotoxic effects of the Cs/ZnO‐NPs are evaluated against various cancer cell types. The results show that at a concentration of 125 µg mL−1, the Cs/ZnO‐NPs demonstrate significantly higher cancer cell toxicity compared to ZnO‐NPs alone, while remaining non‐toxic to normal cells. This indicates that Cs/ZnO‐NPs have a superior ability to selectively target cancer cells. These findings suggest that Cs/ZnO‐NPs nanomicelles hold promise as an effective and safe nanotherapeutic approach in the realm of cancer treatment, meriting further exploration for clinical applications.