The Effect of Topical Corticosteroids, Topical Antihistamines, and Preservatives on Human Ciliary Beat Frequency

Abstract

Background: The aim of this study was to investigate the effect of the corticosteroids, the antihistamines, and the preservatives benzalkonium chloride (BKC) and potassium sorbate (PS) in intranasal medications on human nasal epithelial ciliary beat frequency (CBF). Methods: Primary ciliated epithelial cell cultures from the human nasal mucosa of chronic sinusitis patients were established. Changes in CBF of epithelial cell cultures treated/untreated with intranasal medications or preservatives were assessed using high-speed digital imaging methods. Results: Budesonide caused a rapid but reversible ciliostasis and showed no ciliotoxic effect at 10% dilution. Fluticasone propionate induced an irreversible ciliostatic activity and showed a reversible decrease in CBF at 10% dilution. Azelastine hydrochloride and levocabastine hydrochloride both induced a dose-dependent and irreversible decrease in CBF, although the ciliotoxic effect was not evident at 5% dilution. BKC resulted in an irreversible ciliostasis at 0.005 or 0.01% concentrations, whereas PS did not show any change in CBF at 0.12 or 0.24% concentrations. Conclusions: Crystalline BKC and BKC-containing intranasal medications, including fluticasone propionate, azelastine hydrochloride and levocabastine hydrochloride, but not PS or PS-containing intranasal budesonide spray, led to irreversible ciliostasis in human nasal epithelial cell cultures when applied at clinically relevant concentrations.

Nasal cytology: Methodology with application to clinical practice and research

“…Several studies investigating the effect of antihistamines on nasal cytology: data are available mainly for levocetirizine, desloratadine and rupatadine as far as oral antihistamines are concerned, and for azelastine hydrochloride and levocabastine hydrochloride ad far as nasal sprays are concerned.…”

“…Only 3 studies investigated the effect of topical azelastine hydrochloride on nasal cytology: in 2 of them, a significant reduction of nasal eosinophils was found in allergic patients, while the third one was not able to show any significant change in total cell numbers and/or differential count in nasal lavage fluid . As far as levocabastine hydrochloride, only 1 study evaluated its effect on nasal cells showing reduced ciliary beat frequency at nasal epithelial level …”

Fast effectiveness of a solubilized low‐dose budesonide nasal spray in allergic rhinitis

“…The aqueous formulation is also free of preservatives such as benzalkonium chloride, paraben or phenyl-ethyl-alcohol, which reportedly have negative effects in the nasal cavity. 35,36 Moreover, treatment with Budesolv 10 led to a fast relief of allergic rhinitis symptoms, reported as TNSS. In addition, Budesolv 10 appears to be the first intranasal formulation of budesonide that reveals a significant effect on respiratory symptoms, exemplified by cough, wheezing and dyspnoea.…”

Effect of Cellulose Powder on Human Nasal Epithelial Cell Activity and Ciliary Beat Frequency

“…Ideally, the drug for nasal delivery should be inert within the applied concentration ranges, and not cause harm to the epithelium, particularly ciliary motility [24]. Recently, some studies documented that many preservatives may have cumulative adverse effects on the CBF and result in irreversible ciliostasis, even after they have been withdrawn and the nasal mucosa has been rinsed [25, 26]. Ciliary motility may recover once the stimuli (such as inflammatory mediators, pathogens, and allergens) are removed [27].…”