Toxicological evaluation of cyclosporine eyedrops.
OBJECTIVE
The short-term toxicological effects of two cyclosporine A eyedrop formulations are compared.


METHODS
Formula A was based on Sandimmune (Novartis, Switzerland) infusion concentrate with a final ethanol concentration of 1% (w/w), and formula B on Sandimmune oral solution. Both formulations were diluted in sterile peanut oil (10 mg/ml). The left eyes of 12 rabbits were treated with the cyclosporine eyedrops over a two-week period. The right eyes served as controls. Slit-lamp and scanning electron microscopic examinations were performed, and the total protein concentration in aqueous humor was measured in treated and control eyes.


CONCLUSIONS
Both Sandimmune oral solution and infusion concentrate-derived eyedrops were found to be non-toxic to rabbit eyes and there were no significant differences between the two formulations. More definite conclusions as to the safety of these cyclosporine formulations cannot be made without long-term trials.
D000818:Animals; D001082:Aqueous Humor / Q000187:drug effects / Q000378:metabolism; D002452:Cell Count / Q000187:drug effects; D003315:Cornea / Q000166:cytology / Q000187:drug effects*; D016572:Cyclosporine / Q000633:toxicity*; D004728:Endothelium, Corneal / Q000648:ultrastructure; D000431:Ethanol / Q000633:toxicity; D005136:Eye Proteins / Q000378:metabolism; D005260:Female; D008855:Microscopy, Electron, Scanning; D009883:Ophthalmic Solutions / Q000633:toxicity*; D004364:Pharmaceutical Preparations; D011817:Rabbits; D018675:Toxicity Tests