Recently, targeted drug delivery systems have gained much importance for delivering many kinds of drugs as well as imaging agents, particularly to the targeted disease cells or tissues. The diagnosis and treatment of brain disorders is an extremely challenging task. The blood-brain barrier (BBB) is the primary obstacle in conveying the chemotherapeutic and diagnostic agents that prompt the insufficient delivery of drug at the brain-targeted site. Many drug molecules are non-soluble in aqueous systems, unable to cross BBB, or present severe side effects. Lipid-based nanoparticle (LBNP) systems represent one of the most potential colloidal carriers. They are preferred over polymeric nanoparticles due to their high stability, excellent targeting ability,increased loading capacity, non-toxicity, low production costs, and ease of preparation. Combining drug with lipid nanoparticles reduces the therapeutic dose and toxicity, decreases drug resistance, and increases drug levels in the targeted tissue. This review presents the different types of LBNPs developed in recent years and theirapplication in brain disorders.