Breast cancer is the second most common cancer that causes death among women worldwide. Incidence of breast cancer is increasing worldwide, and the age at which breast cancer develops has shifted from 50-70 years to 30-40 years. Chemotherapy is the most commonly used effective treatment strategy to combat breast cancer. However, one of the major drawbacks is low selective site-specificity and the consequent toxic insult to normal healthy cells. The nanocarrier system is consistently utilised to minimise the various limitations involved in the conventional treatment of breast cancer. The nanocarrier based targeted drug delivery system provides better bioavailability, prolonged circulation with an effective accumulation of drugs at the tumour site either by active or passive drug targeting. Active targeting has been achieved by receptor/protein anchoring and externally guided magnetic nanocarriers, whereas passive targeting accomplished by employing the access to the tunnel via leaky tumour vasculature, utilising the tumour microenvironment, because the nanocarrier systems can reduce the toxicity to normal cells. As of now a few nanocarrier systems have been approved by FDA, and various nanoformulations are in the pipeline at the preclinical and clinical development for targeting breast cancer; among them, polymeric micelles, microemulsions, magnetic microemulsions, liposomes, dendrimers, carbon nanotubes, and magnetic Nanoparticles (NPs) are the most common. The current review highlights the active and passive targeting potential of nanocarriers in breast cancer and discusses their role in targeting breast cancer without affecting normal healthy cells.