As a consequence of the growing ageing population, many neurodegenerative diseases, cancer and infections of the brain will become more prevalent. Despite major advances in neuroscience, many potential therapeutic agents are denied access to the central nervous system (CNS) because of the existence of the blood-brain barrier (BBB). This barrier is formed by the endothelial cells of the brain capillaries and its primary characteristic is the impermeability of the capillary wall due to the presence of complex tight junctions and a low endocytic activity. The BBB behaves as a continuous lipid bilayer and prevents the passage of polar and lipid-insoluble substances. The BBB is, therefore, the major obstacle to drugs that are potentially useful for combating diseases affecting the CNS. Extensive efforts have been made to develop CNS drug delivery strategies in order to enhance delivery of therapeutic molecules across the BBB. The current challenge is to develop drug-delivery strategies that will allow the passage of therapeutic drugs through the BBB in a safe and effective manner. This review focuses specifically on the strategies developed to enhance drug delivery across the BBB with an emphasis on the vector-mediated strategy.