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Effect of the non-ionic surfactant Poloxamer 188 on passive permeability of poorly soluble drugs across Caco-2 cell monolayers

Drug permeability of the model drugs ketoprofen and nadolol across Caco-2 cell monolayers was determined in the absence and presence of the non-ionic surfactant Poloxamer 188 (Pluronic® F68, P-188). Stringent controls confirmed that P-188 in concentrations up to 50mg/ml did not adversely affect cell...

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Bibliographic Details
Main Authors: Fischer, Sarah Maud (Author) , Brandl, Martin (Author) , Fricker, Gert (Author)
Format: Article (Journal)
Language:English
Published: 2011
In: European journal of pharmaceutics and biopharmaceutics
Year: 2011, Volume: 79, Issue: 2, Pages: 416-422
ISSN:1873-3441
DOI:10.1016/j.ejpb.2011.04.010
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1016/j.ejpb.2011.04.010
Verlag, lizenzpflichtig, Volltext: https://www.sciencedirect.com/science/article/pii/S0939641111001524
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Author Notes:Sarah Maud Fischer, Martin Brandl, Gert Fricker
Description
Summary:Drug permeability of the model drugs ketoprofen and nadolol across Caco-2 cell monolayers was determined in the absence and presence of the non-ionic surfactant Poloxamer 188 (Pluronic® F68, P-188). Stringent controls confirmed that P-188 in concentrations up to 50mg/ml did not adversely affect cell viability or monolayer integrity. Equilibrium experiments confirmed that the drugs were merely passively transported. Caco-2 permeability of both drugs was found to be decreased by the surfactant in a concentration-dependent manner. Ultrafiltration revealed that both drugs were associated with surfactant micelles. The systematic investigation of micellization on passive absorption showed that association of drugs with P-188 micelles appears to depress their passive permeability under conditions where other transport mechanisms can be neglected.
Item Description:Online verfügbar 28 April 2011
Gesehen am 16.01.2023
Physical Description:Online Resource
ISSN:1873-3441
DOI:10.1016/j.ejpb.2011.04.010

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