Nanotechnology causes revolutionized in the field of medicine and drug delivery system with the help of unique properties of nanomaterials. Advancement in the nanomedicine has been proved as a great alternative to transform healthcare. Targeted drug delivery system and nanocarriers are the newly medications employed for the treatment of cancer and various diseases as well as for the development of diagnostic techniques. Nanomaterials play a crucial role in drug delivery system by increasing the efficiency of the drug toward the specific targeted site, causing fewer toxic effects to other body areas. These nanomaterials are liposomes, polymers, micelles, exosomes, green particulate, carbon-based materials, etc. Such delivery systems are known as nanomaterial-based drug delivery system (NBDDS). One of the major functions of using nanomaterials is that they improve the safety and therapeutic effect of the drugs as they have different physiochemical, biological property, large surface area, and small size. This abstract provides an overview of the development of nanomedicines and drug delivery system with the help of nanobiomaterials. Moreover, it also emphasizes the potential of nanobiomaterials in drug delivery system to overcome various diseases and for improving patient outcomes. The further research in this field enlightens the future scope of this field.