Nanotechnology has gained much interest over the past few years due to its ability to efficiently detect and treat different types of cancers. To overcome the limitations associated with traditional cancer treatment strategies such as lack of specificity, toxic effects, the pre-mature release of the drug, and multidrug resistance, nanomaterials have been widely utilized. Nanomaterials not only enhance the drug accumulation at a specific site but also improve the therapeutic efficacy of anti-cancer drugs. Some other advantages of nanocarriers include targeted and controlled drug delivery, less toxic effects, enhanced solubility and stability, and greater availability of chemotherapeutic agents to the cancer cells due to enhanced permeability and retention effect. The physicochemical properties of nanocarriers can be modified by varying their shapes, sizes, and surface characteristics (PEGylation, ligand, or functional group attachment). Various types of nanomaterials have been utilized for pharmaceutical and medical purposes, most importantly for cancer therapy, depending upon their nature and composition, such as lipid-based, polymeric-based, protein-based, carbon-based, and hybrid nanomaterials. Many of these nanocarrier drug delivery systems have been developed, among which only a few have been clinically approved for anti-cancer drug delivery. The rationale of using nanotechnology for anticancer drugs is to achieve targeted delivery via active or passive targeting and diminish the damages to healthy tissues. So, the ultimate objective of these nanocarriers is to effectively treat the diseases with fewer side effects.