The current conventional cancer therapies do not offer a radical cure and frequently result in significant adverse effects. The present study presents an alternative by repackaging doxorubicin, a commonly used chemotherapy drug, into doxorubicin-loaded kaolinite as a treatment for breast cancer. We characterized the synthesized nanoparticles using a transmission electron microscope (TEM), dynamic light scattering (DLS), and zeta potential. After 18 days of treatment, we assessed the anti-cancer efficacy based on tumor weight and tumor tissue histopathology. Furthermore, the cyto/genotoxic effects of the treatment on the liver were evaluated via oxidative stress measurement, histopathological examination, and a comet assay. Additionally, we assessed the hemocompatibility of the nanoparticles by measuring the hemolysis percentage. The characterization techniques confirmed that the nanoparticles demonstrated acceptable physico-chemical characteristics. Moreover, the histopathological examination of the tumor tissue corresponds with the reduction in tumor size. Furthermore, the formulation reduced cancer-related stress on the liver by reducing oxidative stress and subsequent inflammation, preventing metastasis of tumor cells, and reducing DNA damage. Moreover, the hemolysis test revealed its blood biocompatibility. These results strengthen the formulation's anti-cancer efficacy and safety, providing more biocompatible and benign cancer treatment alternatives. The formula's clinical effectiveness must be confirmed by further clinical studies.