Breast cancer remains one of the world's most devastating diseases. However, better understanding of tumor biology and improved diagnostic devices could lead to improved therapeutic outcomes. Nanotechnology has the potential to revolutionize cancer diagnosis and therapy. Various nanocarriers have been introduced to improve the therapeutic efficacy of anticancer drugs, including liposomes, polymeric micelles, quantum dots, nanoparticles, and dendrimers. Recently, targeted drug delivery systems for anti-tumor drugs have demonstrated great potential to lower cytotoxicity and increase therapeutic effects. Various ligands/approaches have been explored for targeting breast cancer. This paper provides an overview of breast cancer, conventional therapy, potential of nanotechnology in management of breast cancer, and rational approaches for targeting breast cancer.