Multiple sclerosis (MS) is a chronic, immune-mediated neurological disorder characterized by demyelination and neurodegeneration within the central nervous system. Traditional pharmacological treatments for MS often lack specificity, resulting in systemic side effects and limited therapeutic efficacy. Recent advances in targeted drug delivery systems offer promising avenues for improving disease management by enhancing drug bioavailability at specific sites of action while minimizing off-target effects. This chapter explores the evolving landscape of targeted drug delivery approaches in MS, including nanoparticle-based systems, ligand-receptor targeting, and blood-brain barrier-penetrating carriers. Emphasis is placed on the mechanisms of action, preclinical and clinical developments, and the potential of these systems to transform the therapeutic paradigm of MS. The chapter also addresses the challenges and future directions in optimizing targeted therapies for personalized and effective MS treatment.