TY - JOUR
T1 - Treatment of corneal xerophthalmia in rabbits with micromolar doses of topical retinoic acid
AU - Ubels, John L.
AU - Rismondo, Vivian
AU - Edelhauser, Henry F.
N1 - Funding Information:
ACKNOWLEDGEMENTS This study was supported by NIH grants EY05640 and EY01931 and by a grant from Alcon Laboratories, Fort Worth, TX.
PY - 1987
Y1 - 1987
N2 - Several reports have appeared on the efficacy of topically applied 0.01% or 0.1% all-trans retinoic acid (0.04-0.4 millimolar) for treatment of xerophthalmia, conjunctival squamous metaplasia, and corneal epithelial erosions in humans and animals. An observation common to many of these studies is the occurrence of an adverse reaction to retinoic acid in the form of lid margin hyperemia and blepharoconjunctivitis. Since retinoic acid is biologically active at micro-molar to nanomolar concentrations, it may be possible to reduce side effects while maintaining therapeutic effectiveness by reducing the retinoic acid concentration in ophthalmic formulations. In the present study, topical 0.005% retinoic acid in petrolatum ointment reversed corneal keratinization in xerophthalmic, vitamin A-deficient rabbits in 3-4 days while 0.0005% (2 micromolar) retinoic acid ointment was effective in 4-6 days. Further clinical trials of topical retinoic acid for treatment of ocular surface disease should be conducted using micromolar concentrations of retinoic acid which are expected to maintain a therapeutic effect while reducing adverse reactions.
AB - Several reports have appeared on the efficacy of topically applied 0.01% or 0.1% all-trans retinoic acid (0.04-0.4 millimolar) for treatment of xerophthalmia, conjunctival squamous metaplasia, and corneal epithelial erosions in humans and animals. An observation common to many of these studies is the occurrence of an adverse reaction to retinoic acid in the form of lid margin hyperemia and blepharoconjunctivitis. Since retinoic acid is biologically active at micro-molar to nanomolar concentrations, it may be possible to reduce side effects while maintaining therapeutic effectiveness by reducing the retinoic acid concentration in ophthalmic formulations. In the present study, topical 0.005% retinoic acid in petrolatum ointment reversed corneal keratinization in xerophthalmic, vitamin A-deficient rabbits in 3-4 days while 0.0005% (2 micromolar) retinoic acid ointment was effective in 4-6 days. Further clinical trials of topical retinoic acid for treatment of ocular surface disease should be conducted using micromolar concentrations of retinoic acid which are expected to maintain a therapeutic effect while reducing adverse reactions.
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U2 - 10.3109/02713688709034838
DO - 10.3109/02713688709034838
M3 - Article
C2 - 3595183
AN - SCOPUS:0023258911
SN - 0271-3683
VL - 6
SP - 735
EP - 737
JO - Current Eye Research
JF - Current Eye Research
IS - 5
ER -