An in vitro comparison of commonly used topical glucocorticoid preparations.
BACKGROUND
Glucocorticoids (GC) are potent inhibitors of peripheral blood eosinophil, basophil, and airway epithelial cell function.


OBJECTIVE
We compared in vitro the inhibitory activity of synthetic GC used for topical treatment in asthma and rhinitis on basophil histamine release (HR), eosinophil viability, and expression of vascular cell adhesion molecule-1 (VCAM-1) in the human bronchial epithelial cell line BEAS-2B.


METHODS
Cells were treated for 24 hours with increasing concentrations (range 10(-13) to 10(-6) mol/L) of fluticasone propionate (FP), mometasone furoate (MF), budesonide (BUD), beclomethasone dipropionate (BDP), triamcinolone acetonide (TAA), hydrocortisone (HC), or dimethyl sulfoxide diluent before challenge. HR was measured by a fluorometric assay, viability of purified eosinophils was assessed by erythrosin B dye exclusion, and expression of VCAM-1 was measured by flow cytometry.


RESULTS
GC induced a concentration-dependent inhibition of anti-IgE-induced HR. Maximum inhibition ranged from 59. 7% to 81%, with a rank order of GC potency of FP > MF > BUD > BDP congruent with TAA >> HC. Three-day treatment of eosinophils with GC concentration-dependently inhibited IL-5-induced eosinophil viability, with a rank of potency almost identical to that observed with basophil HR. The rank order of potency of GC for inhibition of the expression of VCAM-1 in BEAS-2B cells was MF congruent with FP >> BUD > TAA > HC congruent with BDP. Inhibitory concentration of 50% values revealed that epithelial cells were the most sensitive and eosinophils were the least sensitive.


CONCLUSIONS
These data, combined with information on pharmacodynamics of these drugs in vivo, may be useful in estimating GC local anti-inflammatory effects.
Stellato
C
C
Johns Hopkins Asthma and Allergy Center, Baltimore, Md, and the Mie National Hospital, Tsu Mie, Japan.
Atsuta
J
J
Bickel
C A
CA
Schleimer
R P
RP
D000287:Administration, Topical; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D001491:Basophils / Q000166:cytology / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D004804:Eosinophils / Q000187:drug effects; D005938:Glucocorticoids / Q000494:pharmacology*; D006636:Histamine Release / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D019010:Vascular Cell Adhesion Molecule-1 / Q000096:biosynthesis
D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D019010:Vascular Cell Adhesion Molecule-1