Distribution of salicylate in lens and intraocular fluids and its effect on cataract formation.

Retrospective studies on cataract development in patients with rheumatoid arthritis or osteoarthritis revealed a retardant effect of aspirin on diabetic and non-diabetic cataracts. The effect of aspirin is dose-dependent. The correlation coefficient between years delay for various cataracts subcategories versus aspirin taken (in tablets per day X years of intake) was 0.69. The ocular pharmacokinetics of 14C acetylsalicylic acid or salicylate were determined after intravenous or intraperitoneal administration to rabbits. 14C acetylsalicylic acid penetrates rapidly into rabbit lens and aqueous humor after intravenous administration. After intraperitoneal administration, salicylate levels in rabbit plasma, similar to those of humans receiving four to six aspirin tablets (325 mg each), result in accumulation of salicylate by lens (mean +/- SD) of 405 +/- 72 mumoles/g and 620 +/- 30 mumoles/g at two and four hours, respectively. At those dosages, salicylate is cleared in 24 hours from rabbit plasma and intraocular fluids, but retained by lens. Penetration of salicylate into rabbit lens and rat lens is dose-dependent. The retardant aspirin effect in diabetic cataracts is linked to inhibition of tissue aldose reductase and lens protein glycosylation. Deceleration of galactose cataract formation in rats occurs after daily salicylate intraperitoneal injections of 100 mg/kg a day.