Breast cancer is avertible yet one of the most widespread carcinomas globally. Though periodic screening and monitoring have resulted in reduced incidences, the malignancy claims increased death rates across the globe. Due to the non-specific and aggressive nature of available conventional cancer therapeutics, there is a crucial need for better treatment paradigms. Recent advancements in nanotechnology have aided in this by utilizing nanocarriers in targeted drug delivery approaches. Optimized nanoparticles have been used to enhance the circulation time and target the efficacy of conventional therapeutic drugs. Passive targeting comprises surface modulation to avoid drug elimination via a standard body defense system. Active targeting includes chemical interaction with various genes, receptors, and antigens overexpressed during cancer progression. Therefore, the present review recapitulates drug delivery approaches and nanoparticle-based targeting that can potentially overcome the limitations of conventional drug therapies.