The brain acts as the central processing unit of the human body, coordinating all physiological systems. Delivering drugs to the brain remains a major challenge due to the restrictive nature of the Blood–Brain Barrier (BBB). This review discusses various techniques that facilitate the passage of drugs across the BBB, such as prodrugs, liposomes, nanotechnology, microspheres, polymeric micelles, microemulsions, and dendrimers. These approaches improve the ability of drugs to reach their targeted brain sites effectively. Central Nervous System (CNS) disorders affect over one billion people globally, and one of the greatest challenges in CNS drug development is overcoming the BBB, which limits the entry of most therapeutic agents. This article provides an overview of emerging strategies for brain-targeted delivery, emphasizing nanotechnology-based systems that offer advantages such as reduced side effects, enhanced bioavailability, non-invasive routes, and improved patient compliance.