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In-vitro permeability of poorly water soluble drugs in the phospholipid vesicle-based permeation assay: the influence of nonionic surfactants

The aim of this study was to determine the influence of nonionic surfactants on drug permeability using the phospholipid vesicle-based permeation assay (PVPA), which excludes other than trans-membrane diffusion pathways.Barrier integrity was monitored both by electrical resistance and permeability m...

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Bibliographic Details
Main Authors: Fischer, Sarah Maud (Author) , Flaten, Gøril Eide (Author) , Hagesæther, Ellen (Author) , Fricker, Gert (Author) , Brandl, Martin (Author)
Format: Article (Journal)
Language:English
Published: 15 June 2011
In: Journal of pharmacy and pharmacology
Year: 2011, Volume: 63, Issue: 8, Pages: 1022-1030
ISSN:2042-7158
DOI:10.1111/j.2042-7158.2011.01301.x
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1111/j.2042-7158.2011.01301.x
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Author Notes:Sarah Maud Fischer, Gøril Eide Flaten, Ellen Hagesæther, Gert Fricker and Martin Brandl
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Summary:The aim of this study was to determine the influence of nonionic surfactants on drug permeability using the phospholipid vesicle-based permeation assay (PVPA), which excludes other than trans-membrane diffusion pathways.Barrier integrity was monitored both by electrical resistance and permeability measurement of the hydrophilic marker calcein. Permeability of the model drugs ketoprofen and nadolol across the PVPA-barrier was measured by HPLC-UV. Micelle association of the model drugs was determined using ultrafiltration, whereby micelle-bound drug and molecular drug were separated.The nonionic surfactant poloxamer 188 was demonstrated not to affect barrier integrity. Drug permeability was found depressed in the presence of poloxamer 188 in a concentration-dependent manner. Both drugs were found to associate with poloxamer 188 micelles. The extent of the decrease in permeability correlated mostly, but not in all cases, with the fraction of micelle-bound drug.Micelle association was one important but not the only factor affecting drug permeability across the PVPA-barrier.
Item Description:Gesehen am 16.01.2023
Physical Description:Online Resource
ISSN:2042-7158
DOI:10.1111/j.2042-7158.2011.01301.x

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