One of the major challenges in drug development is the delivery of therapeutics to the central nervous system (CNS). The blood-brain barrier (BBB), which modulates the passage of molecules from the CNS, presents a formidable obstacle that limits brain uptake of therapeutics and, therefore, impedes the treatment of multiple neurological pathologies. Targeted nanocarriers present an excellent opportunity for drug delivery into the brain leveraging on endogenous receptors to transport therapeutics across the BBB endothelium. Receptor-mediated transport endows multiple benefits over other conventional delivery methods such as the transient permeabilization of the BBB or the direct depositioning of intracranial depots. Herein, different strategies for nanocarrier targeting to the CNS are discussed, highlighting the challenges and recent developments.
Keywords: CNS BBB NPs RVG CTX.