© 2022 University of Ankara. All rights reserved.Objective: In the last 20 years, with the nanotechnological developments, there has been an increase in studies aimed at targeting drug molecules to the brain. The brain is separated from bloodstream by a unique barrier. This structure, called the blood-brain barrier, which consists of astrocytes, pericytes, endothelial cells and tight junctions between them. Apart from the enzymatic activity that prevents the passage of molecules to the brain, the separation of the brain from the systemic blood circulation by the blood-brain barrier negatively affects the passage of therapeutic molecules. The structure of the brain and the blood-brain barrier must be known and the penetration mechanisms of drug molecules to the brain must be elucidated. In this review, we aimed to mention the blood-brain barrier and drug targeting methods to the brain. Also, importance of the solid lipid nanoparticles in targeting drug molecules to the brain will be emphasized. Result and Discussion: Blood-brain barrier is the biggest obstacle in targeting drug molecules to the brain. One of the systems developed to overcome this obstacle is solid lipid nanoparticles. It has been observed that the effectiveness of drugs in central nervous system disorders can be increased by targeting.