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Characteristics of compounds that cross the blood-brain barrier
- Source :
- BMC Neurology, Vol 9, Iss Suppl 1, p S3 (2009), BMC Neurology
- Publication Year :
- 2009
- Publisher :
- Springer Science and Business Media LLC, 2009.
-
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.
- Subjects :
- Clinical Neurology
Plasma protein binding
Blood–brain barrier
lcsh:RC346-429
03 medical and health sciences
Drug Delivery Systems
0302 clinical medicine
Animals
Humans
Medicine
lcsh:Neurology. Diseases of the nervous system
030304 developmental biology
chemistry.chemical_classification
0303 health sciences
business.industry
Biological Transport
Transporter
General Medicine
Transmembrane protein
3. Good health
Proceedings
medicine.anatomical_structure
chemistry
Blood-Brain Barrier
Nanoparticles for drug delivery to the brain
Drug delivery
Biophysics
Neurology (clinical)
Efflux
Glycoprotein
business
Neuroscience
030217 neurology & neurosurgery
Central Nervous System Agents
Subjects
Details
- ISSN :
- 14712377
- Volume :
- 9
- Database :
- OpenAIRE
- Journal :
- BMC Neurology
- Accession number :
- edsair.doi.dedup.....3134dd73aeeeaf517f0ab0e62b76bb6b