Abstract
BackgroundTo investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents (alcaftadine 0.25%, bepotastine besilate 1.5%, and olopatadine HCL 0.1%) on human corneal epithelial cells (HCECs) and their anti-allergic effects on cultured conjunctival epithelial cells.MethodsA Methylthiazolyltetrazolium(MTT)-based calorimetric assay was used to assess cytotoxicities using HCECs at concentrations of 10, 20 or 30% for exposure durations of 30 min, 1 h, 2 h, 12 h or 24 h. Cellular morphologies were evaluated by inverted phase-contrast and electron microscopy. Wound widths were measured 2 h, 18 h, or 24 h after confluent HCECs monolayers were scratched. Realtime PCR was used to quantify anti-allergic effects on cultured human conjunctival cells, in which allergic reactions were induced by treating them with Aspergillus antigen.ResultsCell viabilities decreased in time- and concentration-dependent manners. Cells were detached from dishes and showed microvilli loss, cytoplasmic vacuoles, and nuclear condensation when exposed to antiallergic agents; alcaftadine was found to be least cytotoxic. Alcaftadine treated HCECs monolayers showed the best wound healing followed by bepotastine and olopatadine (p < 0.0001). All agents significantly reduced the gene expressions of allergic cytokines (IL-5, IL-25, eotaxin, thymus and activation-regulated chemokine, and thymic stromal lymphopoietin) and alcaftadine had the greatest effect (p < 0.0001 in all cases).ConclusionsAlcaftadine seems to have less side effects and better therapeutic effects than the other two anti-allergic agents tested. It may be more beneficial to use less toxic agents for patients with ocular surface risk factors or presumed symptoms of toxicity.
Highlights
To investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents on human corneal epithelial cells (HCECs) and their anti-allergic effects on cultured conjunctival epithelial cells
6–30% of individuals are suffering from allergic conjunctivitis (AC) and 30~70% of them accompany other allergic diseases [3, 4]
The clinical manifestations of AC such as itching, hyperemia, chemosis, and eyelid swelling are the result of mast cell degranulation and the release of inflammatory chemical mediators, which are initiated by crosslinking between permeated allergen
Summary
To investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents (alcaftadine 0.25%, bepotastine besilate 1.5%, and olopatadine HCL 0.1%) on human corneal epithelial cells (HCECs) and their anti-allergic effects on cultured conjunctival epithelial cells. The prevalence rates of allergic diseases have been increasing due to hereditary factors, environmental pollution, increased allergen levels, and changes in life patterns including dietary [1, 2]. The fundamental treatment for AC is to avoid allergens that cause hypersensitive reactions as other allergic diseases. It is difficult to identify the causative allergens accurately and to avoid a known allergen completely if they are encountered in daily life. For these reasons, pharmacotherapy has been used to provide symptom relief and treatment in AC. The clinical manifestations of AC such as itching, hyperemia, chemosis, and eyelid swelling are the result of mast cell degranulation and the release of inflammatory chemical mediators (especially histamine), which are initiated by crosslinking between permeated allergen
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