Nanotechnology-enabled drug delivery systems have emerged as a promising tool for overcoming the Blood Brain Barrier (BBB) and delivering drugs to the Central Nervous System (CNS).This mini-review provides an overview of recent advancements in nanotechnology to improve blood-brain barrier penetration.It covers different approaches, such as using targeted ligands and receptors, engineered carriers and transporters, and surface modifications for targeting the blood-brain barrier.Polymeric nanoparticles, liposomes, and metallic nanoparticles, such as silver and zinc oxide, are discussed in the context of their unique properties and applications.Preclinical and clinical advances in nanotechnology-based BBB delivery are discussed, including transcellular nanotechnology-based brain drug delivery and preclinical and clinical studies of nanocarriers for CNS disorders.Although nanotechnology has shown great potential for treating CNS diseases, several challenges remain.The major challenges and future perspectives for constructing brain-targeted delivery systems are also discussed, particularly limitations associated with the blood-brain barrier and clinical obstacles to CNS disease treatment.In conclusion, the development of nanotechnology-based drug delivery systems promises to revolutionize the treatment of CNS diseases.