Abstract

The blood-brain barrier (BBB), which impedes drug penetration into the central nervous system, is composed of specific structures formed by brain capillary endothelial cells and sheathed by astrocytic end-feet through basement membrane. Many brain drug delivery strategies have focused on adsorptive-mediated transcytosis (AMT), which is triggered by electrostatic interaction between cationic molecules and anionic microdomains on the cytoplasm membrane of the brain capillary endothelial cells. AMT-based drug delivery to the brain can be achieved by using cationic proteins and basic oligopeptides such as cell-penetrating peptides as targetors. Large therapeutic molecules such as neuropeptides and proteins or even drug-encapsulated vectors such as liposomes and nanoparticles can be allowed to access brain parenchyma through AMT when conjugated with these cationic targetors. In this review, I briefly discuss adsorptive-mediated brain delivery systems that may provide physiologic-based strategies for enhanced delivery of therapeutic substances through the BBB.

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