Chemotherapeutic agents have been used extensively in breast cancer remedy. However,
most anticancer drugs cannot differentiate between cancer cells and normal cells, leading to toxic side
effects. Also, the resulted drug resistance during chemotherapy reduces treatment efficacy. The development
of targeted drug delivery offers great promise in breast cancer treatment both in clinical applications
and in pharmaceutical research. Conjugation of nanocarriers with targeting ligands is an effective
therapeutic strategy to treat cancer diseases. In this review, we focus on active targeting methods
for breast cancer cells through the use of chemical ligands such as antibodies, peptides, aptamers, vitamins,
hormones, and carbohydrates. Also, this review covers all information related to these targeting
ligands, such as their subtypes, advantages, disadvantages, chemical modification methods with nanoparticles
and recent published studies (from 2015 to present). We have discussed 28 different targeting
methods utilized for targeted drug delivery to breast cancer cells with different nanocarriers delivering
anticancer drugs to the tumors. These different targeting methods give researchers in the field of drug
delivery all the information and techniques they need to develop modern drug delivery systems.