© 2014, Hacettepe University, Faculty of Pharmacy. All rights reserved.Delivery Systems for Brain Drug Targeting, Ankara, 2013. Blood-brain barrier is the main factor which maintains homeostasis by protecting brain from toxic and harmful compounds, but it also represents the main limiting factor for a number of drug molecules to reach the aimed areas in brain. The only way to overcome this treatment-limiting obstacle could be reached by the help of new strategies. Nanoscale colloidal systems are promising strat- egies in the treatment of central nervous system (CNS) diseases by passive and active targeting. Receptor mediated transport systems (RMT) are in the spotlıght of targeting strategies.By the help of Molecular Trojan Technology, which is developed for receptor targeting, large molecule drugs will be transported to brain. Nowadays, research interest in targeted delivery systems in the treatment of CNS disorders has been focused on brain cancer, stroke, Alzheimer’s disease, Parkinson disease. Therefore, the aim of this present review is to evaluate the targeting approaches of colloidal systems and current studies for the development of new strategies.