Penetration of topical cyclosporine into the rabbit cornea, aqueous humor, and serum
M. W. Mosteller, B. M. Gebhardt, A. M. Hamilton and H. E. Kaufman
Systemic and ocular absorption of topically applied 10% cyclosporine
ointment was determined in rabbit cornea, aqueous humor, and serum by
radioimmunoassay. The concentration of the drug in the cornea reached a
peak of 900 ng/mL three hours after application. Substantial levels were
still present at 24 hours. Relatively low concentrations were measured in
the aqueous humor and serum, suggesting corneal stromal pooling of this
hydrophobic cyclic peptide. Topical ocular application of cyclosporine may
reduce or eliminate the drug's systemic toxic effects while maintaining a
therapeutic level of local immunosuppressive activity.
