In vitro safety of ketotifen as a topical nasal rinse

Int Forum Allergy Rhinol. 2020 Feb;10(2):265-270. doi: 10.1002/alr.22461.

Abstract

Background: Ketotifen is a second-generation noncompetitive H1-antihistamine and mast-cell stabilizer. It is commonly used to treat or prevent allergic conjunctivitis, asthma, chronic urticaria, anaphylaxis, mast-cell, and other allergic-type disorders. However, it has never been studied in aspirin-exacerbated respiratory disease (AERD), an aggressive phenotype of chronic rhinosinusitis with nasal polyps, where the mast cell plays a prominent role its pathogenesis.

Methods: Human sinonasal epithelial cells were grown at an air-liquid interface (ALI). Ketotifen powder was dissolved in saline to make 4 test solutions at 1.04, 2.08, 10.4, and 20.8 µg/mL. Control (saline) or ketotifen solution was added apically to ALI cultures from tissue of 5 unique patients, and ciliary beat frequency (CBF) changes were recorded. Lactate dehydrogenase was measured at 24 and 48 hours to estimate long-term cellular toxicity.

Results: Apical application of ketotifen at all concentrations was neither ciliotoxic nor ciliostimulatory, with no change in CBF over a period of 15 minutes after application. Cellular toxicity for all concentrations at 24 and 48 hours after application was <3% and <7%, respectively, that of lysed cultures.

Conclusion: Topical application of ketotifen to an in vitro model of sinonasal epithelium is safe, as evaluated by CBF and lactate dehydrogenase. Ketotifen is neither ciliotoxic nor ciliostimulatory, and no long-term cellular toxicity was observed. Ketotifen may have promise as a topical nasal rinse in the treatment of AERD.

Keywords: allergy immunotherapy; ciliary motility; immunotherapy; irrigations; therapeutics.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Administration, Topical
  • Anti-Allergic Agents / pharmacology*
  • Cells, Cultured
  • Cilia / drug effects
  • Cilia / physiology
  • Epithelial Cells / drug effects
  • Epithelial Cells / physiology
  • Histamine H1 Antagonists / pharmacology*
  • Humans
  • Ketotifen / pharmacology*
  • L-Lactate Dehydrogenase / metabolism
  • Therapeutic Irrigation

Substances

  • Anti-Allergic Agents
  • Histamine H1 Antagonists
  • L-Lactate Dehydrogenase
  • Ketotifen