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Vol. 122, No. 2, 2000
Issue release date: June 2000
Int Ach Allergy Immunol 2000;122:151–154
(DOI:10.1159/000024371)

Binding of Glucocorticoids to Human Nasal Tissue in vitro

Esmailpour N. · Högger P. · Rohdewald P.
Institute of Pharmaceutical Chemistry, Westfälische Wilhelms-Universität Münster, Germany

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Abstract

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.

Copyright © 2000 S. Karger AG, Basel



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References

  1. Mygind N: Glucocorticosteroids and rhinitis. Allergy 1993;48:476–490.
  2. Högger P, Rawert J, Rohdewald P: Dissolution, tissue binding and kinetics of receptor binding of inhaled glucocorticoids. Eur Respir J 1993;6(suppl 17):584.
  3. Würthwein G, Rehder S, Rohdewald P: Lipophilicity and receptor affinity of glucocorticoids. Pharm Ztg Wiss 1992;137:161–167.
  4. Rohdewald P, Bonsmann U, Högger P: Die Bindung inhalativer Glukokortikoide an menschliches Lungengewebe in vitro; in Leupold W, Nolte D (eds): Neue Aspekte der inhalativen Glukokortikoid-Therapie des Asthma bronchiale. München, Dustri Verlag, 1995, pp 14–27.
  5. Esmailpour N, Högger P, Rabe KF, Heitmann U, Nakashima M, Rohdewald P: Distribution of inhaled fluticasone propionate between human lung tissue and serum in vivo. Eur Respir J 1997;10:1496–1499.
  6. Van den Bosch JMM, Westermann CJJ, Aumann J, Edsbäcker S, Tönnisson M, Selroos O: Relationship between lung tissue and blood plasma concentrations of inhaled budesonide. Biopharm Drug Dispos 1993;14:455–459.


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