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  • Title: Pharmacokinetic of topical cyclosporin A in the rabbit eye.
    Author: Wiederholt M, Kössendrup D, Schulz W, Hoffmann F.
    Journal: Invest Ophthalmol Vis Sci; 1986 Apr; 27(4):519-24. PubMed ID: 3957569.
    Abstract:
    3H labelled cyclosporin A (CS-A) eye drops (2% in castor oil) were applied in rabbits. When a single drop of 10 microliters was given CS-A reached a maximal concentration of 900-1400 ng/ml in the cornea 6 hr after application and then slowly decreased. A substantial level of 600-900 ng/ml was still present after 48 hr. When corneas were analysed for their cellular compartments, 67% of CS-A was found in the epithelium, 25% in the stroma (probably in keratocytes), and 8% in the endothelium. In corneas denervated by circular keratotomy, slightly reduced concentrations were found after surgery, the reduction was not therapeutically significant. Using the HPLC method a significant corneal metabolism of CS-A could be excluded. Scleral concentrations of CS-A as high as 180 ng/ml were found. Concentrations of CS-A in aqueous humor, lens, vitreous body and uvea/retina were below the therapeutic range.
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