A method to determine the ability of drugs to diffuse through the blood-brain barrier

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A method to determine the ability of drugs to diffuse through the blood-brain barrier

JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)

ID	155458
Author(s)	Seelig, A; Gottschlich, R; Devant, R M
Author(s) at UniBasel	Seelig-Löffler, Anna
Year	1994
Title	A method to determine the ability of drugs to diffuse through the blood-brain barrier
Journal	Proceedings of the National Academy of Sciences of the United States of America
Volume	91
Number	1
Pages / Article-Number	68-72
Keywords	Blood-Brain Barrier; Chromatography; High Pressure Liquid; Humans; Models; Chemical; Pharmaceutical Preparations/chemistry/metabolism; Solubility; Surface Properties
Abstract	A method has been devised for predicting the ability of drugs to cross the blood-brain barrier. The criteria depend on the amphiphilic properties of a drug as reflected in its surface activity. The assessment was made with various drugs that either penetrate or do not penetrate the blood-brain barrier. The surface activity of these drugs was quantified by their Gibbs adsorption isotherms in terms of three parameters: (i) the onset of surface activity, (ii) the critical micelle concentration, and (iii) the surface area requirement of the drug at the air/water interface. A calibration diagram is proposed in which the critical micelle concentration is plotted against the concentration required for the onset of surface activity. Three different regions are easily distinguished in this diagram: a region of very hydrophobic drugs which fail to enter the central nervous system because they remain adsorbed to the membrane, a central area of less hydrophobic drugs which can cross the blood-brain barrier, and a region of relatively hydrophilic drugs which do not cross the blood-brain barrier unless applied at high concentrations. This diagram can be used to predict reliably the central nervous system permeability of an unknown compound from a simple measurement of its Gibbs adsorption isotherm.
Publisher	National Academy of Sciences
ISSN/ISBN	0027-8424
edoc-URL	http://edoc.unibas.ch/dok/A5258486
Full Text on edoc	No
Digital Object Identifier DOI	10.1073/pnas.91.1.68
PubMed ID	http://www.ncbi.nlm.nih.gov/pubmed/8278409
ISI-Number	WOS:A1994MQ47900014
Document type (ISI)	Article

25/04/2024

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