Brain-targeted drug delivery represents one of the most challenging frontiers in pharmacology due to the presence of the blood–brain barrier (BBB), enzymatic degradation, and efflux transporters. Integration of biopharmaceutics with neuropharmacology has enabled the design of advanced delivery systems that enhance drug bioavailability, specificity, and therapeutic efficacy in central nervous system (CNS) disorders. This review explores current strategies for brain-targeted delivery, including nanoparticles, liposomes, polymeric carriers, and ligand-mediated systems. Mechanistic insights into BBB penetration, pharmacokinetic considerations, and clinical translation challenges are discussed. Future directions involve stimuli-responsive carriers, nanotheranostics, and precision neuropharmacology for personalized CNS therapy.