Dose-Effect Response of the Rabbit Eye to Cetylpyridinium Chloride

Abstract
Dose-effect characterization of various ocular parameters (conjunctival hyperemia and edema, corneal thickness, and corneal epithelial fluorescein permeability) has been obtained for a topically applied cationic surfactant, cetylpyridinium chloride (CPC). At doses of 100 μg and less (applied as a dry powder), CPC caused some ocular irritation but no substantive corneal changes. With increasing concentration above 100 μg CPC (to 1,000 μg) the duration and severity of the response was increased over the 28-day experimental period. At 1,000 μg CPC the corneas did not return to normal by 28 days. Changes in epithelial integrity were paralleled by changes in corneal thickness, indicating that the effects of CPC were restricted to the anterior corneal surface. The maximum concentration of CPC that could safely be applied to the eye on a continual basis (i.e., as included in a topical ophthalmic medication), would be less than 3 mM because even this concentration caused some conjunctival hyperemia. The in vivo ocular responses are less severe than those noted during in vitro measurements of CPC effects. The effects of CPC both internally and externally added to a toner used in xerography were also assessed. Although the concentration levels were only 2% for both toners, there were no adverse effects noted on ocular irritation. These toners were, therefore, judged to be harmless even if accidental exposure to the eye occurred.

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