Cancer represents a diverse and complex spectrum of diseases characterized by the abnormal growth and proliferation of cells, establishing a formidable global health challenge. Within the array of diverse cancers, breast cancer arises as one of the primary contributors to cancer-related fatalities in females. Breast cysts, thickenings, alterations in breast size or form, etc., are all prevalent and well-known signs of breast cancer. Despite remarkable progression in cancer research and the abundance of potent drugs, the effectiveness of conventional therapy is still hindered by various complications. In this avenue, nanocarriers present considerable promise for delivering therapeutics to cancerous cells, however, still numerous challenges persist in achieving successful targeted drug delivery and localization. Recent progress has emphasized the utilization of ligand-functionalized nanocarriers to enhance the delivery at target tissues and improve uptake by cancer cells. This approach contributes to increased accuracy and efficacy, which ultimately leads to enhanced patient outcomes. Lactoferrin, a multifunctional glycoprotein, is currently receiving significant attention as a promising ligand for targeted drug delivery in cancerous cells, especially breast cancer cells. This review provides new insight into ligand-targeted therapy, emphasizing the key benefits and notable features of utilizing lactoferrin as a targeting ligand for delivering drug-loaded nanocarriers to tumor sites.