Breast cancer is among the most prevalent and diverse malignancies affecting women. Conventional chemotherapy faces various limitations, such as development of multidrug resistance, which prompts for smoother flow the exploration of targeted therapeutics. Nanoparticles emerge as a promising alternative to overcome multidrug resistance in targeted cancer treatment. This study examined the anticancer effects of Albendazole combined with Zinc Oxide nanoparticles (ZnO NPs). The Albendazole-loaded Zinc Oxide nanoparticles (ALB ZnO NPs) were prepared and a 1:1 ratio was selected for further investigation because of the maximum percentage yield. Entrapment and loading efficacy were estimated at 80.3 and 40.2% respectively. Drug release in gastric media was significantly improved over time. Physicochemical characterization revealed maximum absorbance at 261 nm, average size of 128 nm with a zeta potential of +28.1 mV, and smooth spherical morphology. FTIR spectra shift further confirmed the successful chemical bonding of Albendazole with ZnO NPs. MTT assay revealed ALB ZnO NPs induce dose dependent apoptosis in MCF-7 breast cancer cells. IC50 of Albendazole was reduced from 84.85 μg/mL to 43.35 μg/mL when combined with ZnO NPs indicated marked increase in therapeutic potency. Furthermore, selective index of 4.057 reveals ALB ZnO NPs have high selective cytotoxicity towards cancer cells with a favorable safety profile for normal Vero cells. These findings suggest that ALB ZnO NPs have potential as targeted therapeutic strategy in breast cancer treatment, offering a more effective and selective alternative to conventional chemotherapy.