The blood-brain barrier (BBB) is a dynamic barrier essential for maintaining the micro-environment of the
brain. Although the special anatomical features of the BBB determine its protective role for the central nervous system
(CNS) from blood-born neurotoxins, however, the BBB extremely limits the therapeutic efficacy of drugs into the CNS,
which greatly hinders the treatment of major brain diseases. This review summarized the unique structures of the BBB,
described a variety of in vivo and in vitro experimental methods for determining the transport properties of the BBB, e.g.,
the permeability of the BBB to water, ions, and solutes including nutrients, therapeutic agents and drug carriers, and presented
newly developed mathematical models which quantitatively correlate the anatomical structures of the BBB with its
barrier functions. Finally, on the basis of the experimental observations and the quantitative models, several strategies for
drug delivery through the BBB were proposed.
Keywords: Drug delivery, in vivo and in vitro blood-brain barrier models, paracellular pathway, permeability of the bloodbrain
barrier, transcellualr pathway, transport models.
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