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The delivery of drugs to central nervous system (CNS) is a
challenge in the treatment of neurological disorders. Drugs may be
administered directly into the CNS or administered systematically
(e.g., by intravenous injection) for targeted action in the CNS.
The major challenge to CNS drug delivery is the blood-brain barrier
(BBB), which limits the access of drugs to the brain substance.
Advances in understanding of the cell biology of the BBB have
opened new avenues and possibilities for improved drug delivery to
the CNS. Several carrier or transport systems, enzymes, and
receptors that control the penetration of molecules have been
identified in the BBB endothelium. Receptor-mediated transcytosis
can transport peptides and proteins across the BBB. Methods are
available to assess the BBB permeability of drugs at the discovery
stage to avoid development of drugs that fail to reach their target
site of action in the CNS.
Various strategies that have been used for manipulating the
blood-brain barrier for drug delivery to the brain include osmotic
and chemical opening of the blood-brain barrier as well as the use
of transport/carrier systems. Other strategies for drug delivery to
the brain involve bypassing the BBB. Various pharmacological agents