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Blood-brain barrier (BBB) is the preventive membranous sheath which act as barrier between blood and brain. Barrier observed at junction between brain and blood act as sealant along with tight junctions which inhibits any engulfing activity and restricting the molecular exchange of any cellular type transport. Passive transport is limited to drug with unionized, lipophilic and low molecular weight properties which enables the free diffusion or exchange of molecules from blood to brain. Carrier mediated transport system is best suited for brain transport across BBB. Amino acids, sugar based moieties, neuropeptides, proteins use carrier mediated transport system for permeation into brain. Disadvantage with BBB permeation is that most of therapeutic potential of moiety diminishes or the concentration delivered beyond BBB is below effective levels, thus compromising the activity and act as main cause in decreased activity to brain related disorders.

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