Breast and ovarian cancers are the leading causes of death in women globally. The current therapeutic strategies possess their pros and cons, often resulting in poor therapeutic outcomes. The current treatment modalities, while being effective to some extent, face major drawbacks such as fatigue, resistance development, hypertension, gastrointestinal issues, bleeding, and limited treatment options, significantly impacting the life span and survival in patients. Hence, there is a need to explore an alternative modality to combat these cons, thereby leading to a promising outcome benefiting the patients. Over the past few decades, researchers have been keen on exploring new routes to this, and thus, the emergence of nanotechnology in cancer therapy has become the most advanced domain of science that has paved the way toward diagnostics and targeted drug delivery in battling cancer. The nanocarriers or biomaterials, used in such applications, have been strategically designed to be an efficacious vehicle for drug delivery to target the mechanism of interest in tumor suppression. This book chapter deals with the applications of such nanomaterials/nanocarriers in delivering therapeutic agents, along with diving deeper into the therapeutic and diagnostic potential of these drug-loaded carriers to tackle breast and ovarian cancer.