With a novel approach to targeted therapy, nanomaterial-based drug delivery systems offer unprecedented opportunities to enhance the accuracy, effectiveness, and safety of treatments for various diseases, including cancer, infectious diseases, and genetic disorders. To reduce systemic adverse effects and enhance treatment outcomes, these systems utilize the unique physicochemical properties of nanomaterials, such as liposomes, nanowires, nanoparticles, and quantum dots, to deliver therapeutic agents directly to damaged tissues or cells. Recent developments in the design and functionalization of nanomaterials for drug delivery applications are examined in this chapter, with an emphasis on their ability to target specific sites, permit controlled release, and overcome biological barriers. Basic concepts, including drug loading and release processes, nanocarrier biodistribution, and interactions with biological systems, are covered. The chapter also discusses barriers in transferring these nanocarriers from laboratory models to clinical settings, including issues with cost, manufacturing scalability, regulatory approval, and biocompatibility. Long-term impacts and patient safety are two ethical considerations of nanotechnology in medication delivery. With an emphasis on current research and potential future possibilities, the chapter concludes with a forward-looking perspective on incorporating nanomaterial-based delivery methods into conventional therapeutic medicines.