Breast cancer is the form of cancer most prevalent and intensified progressively among the women population. The propagation of breast cancers takes place in different stages and diagnosed lately. Various approaches have been emerged to treat this clinical condition but these are also integrated with varied side effects. The reason might be attributed to undesired effects of the chemotherapeutic agent and/or haphazard damage to both healthy and cancerous cells. These hitches induce the urge for targeting cancerous cells by the utilization of novel therapeutic platforms. Nano-drug delivery systems are a cluster of different approaches to treating various severe diseases. Henceforward this concept is also applied in the treatment of breast cancer. Nanoparticles exhibits numerous benefits mainly, reduction in dose and low toxicity, solubility enhancement of certain drugs, increased cellular uptake etc. These are the efficient carrier of hydrophobic drugs as these drugs possess challenges in solubility and bioavailability. Cellular uptake by tumor cells is better by nanocarriers owing to a smaller size. The current review is aimed to through light on recent advances in nano-drug targeting in the management of breast cancer. © 2021, Hacettepe University, Faculty of Pharmacy. All rights reserved.