1. Many neurodegenerative diseases, cancer and infections of the brain become more prevalent as populations become older. Despite major advances in neuroscience, the blood-brain barrier (BBB) ensures that many potential therapeutic cannot reach the central nervous system (CNS). The BBB is formed by the complex tight junctions between the endothelial cells of the brain capillaries and their low endocytic activity. This results in the capillary wall that behaves as a continuous lipid bilayer and prevents the passage of polar and lipid-insoluble substances. It is, therefore, the major obstacle to drugs that may combat diseases affecting the CNS. 2. Several strategies for delivering drugs to the CNS have been developed. These enhance the capacity of therapeutic molecules to cross the BBB by modifying the drug itself, or by coupling it to a vector for receptor-mediated or adsorption-mediated transcytosis. 3. The current challenge is to develop drug-delivery systems that ensure that drugs cross the BBB in a safe and effective manner. This review focuses on the strategies developed to enhance drug delivery across the BBB.