Background: Intranasal application of glucocorticoids is an efficacious treatment of allergic rhinitis and some cases of nonallergic rhinitis. However, no data on binding of glucocorticoids to nasal tissue are available. Pronounced binding of the compound to the target tissue is favorable as it might serve as a local deposit delivering the glucocorticoid to specific receptors and it slows down the efflux of the compound into systemic circulation. Methods: Human nasal tissue was incubated with fluticasone propionate, budesonide, flunisolide and beclomethasone-17-monopropionate. Kinetics of binding and redistribution of the tissue-bound fraction into human plasma was monitored. Results: Binding of glucocorticoids to human nasal tissue was fast and highest for the lipophilic fluticasone propionate, followed by beclomethasone-17-monopropionate. Also, highest concentrations of these lipophilic glucocorticoids remained in nasal tissue after equilibration of drug-saturated tissue with plasma. Conclusions: Lipophilic compounds exhibit a high tissue binding and retention which is an important property of topically applied glucocorticoids. It is the basis for prolonged action and low concentration of the compound in systemic circulation.
© 2000 S. Karger AG, Basel
Correspondence to: Prof. Dr. Peter Rohdewald
Institute of Pharmaceutical Chemistry
Hittorfstrasse 58–62, D–48149 Münster (Germany)
Tel. +49 251 833 3347, Fax +49 251 833 2144
Received: Received: December 16, 1999
Accepted after revision: March 17, 2000
Number of Print Pages : 4
Number of Figures : 4, Number of Tables : 0, Number of References : 6
International Archives of Allergy and Immunology
Vol. 122, No. 2, Year 2000 (Cover Date: June 2000)
Journal Editor: D. Kraft, Vienna
ISSN: 1018–2438 (print), 1423–0097 (Online)
For additional information:http://www.karger.com/journals/iaa
Article / Publication Details
Published online: 6/27/2000
Issue release date: June 2000
Number of Print Pages: 4
Number of Figures: 4
Number of Tables: 0
ISSN: 1018-2438 (Print)
eISSN: 1423-0097 (Online)
For additional information: http://www.karger.com/IAA
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