Drug transport across the blood-brain barrier
It is expected that improved knowledge of the anatomical and physiological aspects of the blood-brain barrier and its regulation will provide a scientific basis for the development of strategies to improve the transport of drugs into the central nervous system.
Multidrug resistance protein 1 protects the choroid plexus epithelium and contributes to the blood-cerebrospinal fluid barrier.
- J. Wijnholds, E. C. DeLange, P. Borst
- Biology, MedicineJournal of Clinical Investigation
- 1 February 2000
It is shown that the lack of Mrp1 protein causes etoposide levels to increase about 10-fold in the CSF after intravenous administration of the drug.
The influence of cytokines on the integrity of the blood-brain barrier in vitro
The blood-brain barrier in neuroinflammatory diseases.
- H. D. de Vries, J. Kuiper, A. D. De Boer, T. V. van Berkel, D. Breimer
- BiologyPharmacological Reviews
- 1 June 1997
The existence of the blood-brain barrier (BBB)bwas revealed through studies by [Ehrlich (1885)] in the late 19th century, describing that brain tissue remained unstained after injection of a vital…
Establishment and functional characterization of an in vitro model of the blood-brain barrier, comprising a co-culture of brain capillary endothelial cells and astrocytes.
Penetration of dexamethasone into brain glucocorticoid targets is enhanced in mdr1A P-glycoprotein knockout mice.
- O. Meijer, E. D. De Lange, D. Breimer, A. D. De Boer, J. Workel, E. D. de Kloet
- Biology, MedicineEndocrinology
- 1 April 1998
It was found that brain areas expressing the glucocorticoid receptor in high abundance, such as the hippocampal cell fields and the paraventricular nucleus, showed a 10-fold increase in cell nuclear uptake of radiolabeled steroid, which supports the concept of a pituitary site of action of dexamethasone in blockade of stress-induced ACTH release.
Methodological considerations of intracerebral microdialysis in pharmacokinetic studies on drug transport across the blood–brain barrier
Methodological issues in microdialysis sampling for pharmacokinetic studies.
Assessment of active transport of HIV protease inhibitors in various cell lines and the in vitro blood–brain barrier
Investigation of the transport behaviour of ritonavir, indinavir and amprenavir in the presence and absence of Pgp modulators and probenecid indicates that inhibition of P gp could be useful therapeutically to increase HIV protease inhibitor concentrations in the brain and in other tissues and cells expressing Pgp.
Astrocytes Increase the Functional Expression of P-Glycoprotein in an In Vitro Model of The Blood-Brain Barrier
Astrocytes increase the functional expression of Pgp in the in vitroBBB model, illustrating that an important role for Pgp on the BBB is to protect the barrier against intracellular accumulation of cytotoxic BBB disrupting compounds.