Brain permeability of inhaled corticosteroids
P-glycoprotein
DOI:
10.1211/jpp.57.9.0010
Publication Date:
2005-08-04T22:50:15Z
AUTHORS (5)
ABSTRACT
Abstract The aim of this study was to evaluate if the permeability inhaled corticosteroids entering brain is reduced and P-glycoprotein (P-gp) transporters are involved. Currently employed were given intravenously intratracheally rats at a dose 100 μg kg−1. An ex-vivo receptor binding assay used monitor over 12 h glucocorticoid occupancy in systemic reference organ (kidney). involvement P-gp triamcinolone acetonide assessed wild-type mice mdr1a(-/-) knockout (mice lacking gene for expressing P-gp). After both forms administration, average occupancies 20–56% those organ, with more lipophilic drugs showing pronounced occupation. While liver similar after administration acetonide, significantly greater (mdr1a(-/-): 47.6%, 40.2–55.0%, n = 2; wild-type: 11.5±33.0%, 3). Penetration into (especially lower lipophilicity) reduced. Experiments confirmed transporters. Further studies needed assess whether potential drug interactions transporter level pharmacological significance.
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