Abstract With an increase in lifespan and changing population demographics, the incidence of central nervous system (CNS) diseases is expected to increase significantly in the 21st century. Contrary to common belief, it is recognized that neurodegenerative diseases may be multisystemic in nature and this presents numerous difficulties for the potential treatment of these disorders. This review focuses on applications in the nano-delivery of therapeutic agents across the blood–brain barrier. We explore various types of nanoparticles, ranging from polymerics to liposomes. A brief discussion of the pharmacokinetic parameters and specific targeting strategies of these nanoparticles follows, presenting suggestions for the mechanisms of cellular and intracellular uptake and possible toxicity considerations of nanoparticles.