Nanotechnology is crucial in electronics, life sciences, and medical sciences. Its applications can be assessed as they involve materials' atomic and molecular design. Nanomaterials have proven to be effective drug delivery agents due to their distinctive morphology, making them valuable for encapsulating pharmaceuticals and enabling precise targeting with controlled drug release. The complexity of certain diseases and the inherent toxicity of some drugs have driven interest in developing and refining drug delivery systems. Due to their adaptability, nanomaterials offer a promising solution for tailoring drug delivery systems to specific needs, improving biocompatibility, and ensuring targeted distribution at active sites. This review highlights recent advancements in functional nanomaterials for drug delivery systems, focusing on those that have demonstrated therapeutic efficacy in human studies. It provides insights into nanocarriers and drug release mechanisms based on both in vitro and in vivo results. Additionally, it explores the advantages and limitations of various nanomaterial types, including polymeric, lipid-based, and inorganic-based systems.