This chapter provides a comprehensive review of recent advances in nanomaterials for drug delivery, focusing on the design and preparation of nanocarriers. It also dissects the intricate mechanisms underpinning drug loading and release, and delves into the strategic planning inherent in achieving target delivery. It further outlines the potential applications of these nanomaterials in treating various diseases, including cancer, infectious diseases, and neurological disorders. A distinct case study is incorporated into the chapter, elucidating the promising utility of electrospun nanofibers in drug delivery paradigms. In its concluding remarks, the chapter engages in a thoughtful discourse about the persistent challenges within this rapidly evolving field. It also forecasts the potential trajectories for future exploration and innovation in the captivating domain of nanomaterials for drug delivery.