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• W2029206557 endingPage "S3" @default.
• W2029206557 startingPage "S3" @default.
• W2029206557 abstract "Substances cross the blood-brain barrier (BBB) by a variety of mechanisms. These include transmembrane diffusion, saturable transporters, adsorptive endocytosis, and the extracellular pathways. Here, we focus on the chief characteristics of two mechanisms especially important in drug delivery: transmembrane diffusion and transporters. Transmembrane diffusion is non-saturable and depends, on first analysis, on the physicochemical characteristics of the substance. However, brain-to-blood efflux systems, enzymatic activity, plasma protein binding, and cerebral blood flow can greatly alter the amount of the substance crossing the BBB. Transport systems increase uptake of ligands by roughly 10-fold and are modified by physiological events and disease states. Most drugs in clinical use to date are small, lipid soluble molecules that cross the BBB by transmembrane diffusion. However, many drug delivery strategies in development target peptides, regulatory proteins, oligonucleotides, glycoproteins, and enzymes for which transporters have been described in recent years. We discuss two examples of drug delivery for newly discovered transporters: that for phosphorothioate oligonucleotides and for enzymes." @default.
• W2029206557 created "2016-06-24" @default.
• W2029206557 creator A5054959155 @default.
• W2029206557 date "2009-01-01" @default.
• W2029206557 modified "2023-10-11" @default.
• W2029206557 title "Characteristics of compounds that cross the blood-brain barrier" @default.
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• W2029206557 doi "https://doi.org/10.1186/1471-2377-9-s1-s3" @default.
• W2029206557 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2697631" @default.
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