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November 1982

Retinoid Permeability and Uptake in Corneas of Normal and Vitamin A-Deficient Rabbits

Author Affiliations

From the Departments of Physiology (Drs Ubels and Edelhauser) and Ophthalmology (Dr Edelhauser), Medical College of Wisconsin, Milwaukee.

Arch Ophthalmol. 1982;100(11):1828-1831. doi:10.1001/archopht.1982.01030040808021

• In vitro perfusion of corneas of normal and vitamin A-deficient rabbits provided a model in which to study the pharmacokinetics of corneal permeability and uptake of retinoic acid and retinol. The permeability coefficients of retinoic acid and retinol were 1.49 × 10-5 and 0.61 × 10-5 cm/s, respectively. Removal of the corneal epithelium did not affect the permeability of these lipid-soluble retinoids; however, diffusion through xerophthalmic, vitamin A-deficient corneas was significantly reduced. The corneal uptake of retinoic acid and retinol was reduced by 50% on removal of the epithelium, was nonspecific, and was not affected by xerophthalmia. High-performance liquid chromatography indicated that these retinoids were not metabolized during diffusion through the cornea. These results show that topical application of retinoids is a rational approach to the treatment of such corneal diseases as xerophthalmia and epithelial defects.