Lipid nanoparticles for drug targeting to the brain.

In this chapter, the main production methods of lipid nanostructures such as solid lipid nanoparticles and nanostructured lipid carriers, and their application are described. In particular, we describe the strategies commonly used to obtain lipid nanoparticles to overcome the blood-brain barrier (BBB) for the treatment of several brain diseases. The use of these carriers as targeted drug delivery systems is associated with many advantages that include excellent storage stability, easy production without the use of any organic solvent, the possibility of steam sterilization and lyophilization, and large scale production. They exhibit good stability during long-term storage, consist of physiologically well-tolerated ingredients often already approved for pharmaceutical applications in humans, and are generally recognized as safe. Under optimized conditions, they can be produced to incorporate several drugs and therapeutic proteins. Formulation in solid lipid nanostructures confers improved drug loading and protein stability, targeting, and sustained release of the incorporated molecules. Moreover, their lipophilic features lead them to the central nervous system by an endocytotic mechanism, overcoming the BBB. Many drugs have been incorporated into solid lipid nanosystems and several therapeutic applications may be foreseen, such as targeting with molecules useful for treatment of brain diseases.