Gullstrand Lab, Ophthalmology, Dept. of Neuroscience, Uppsala University, Sweden.
Analytical Chemistry, Dept. of Chemistry-BMC and Science for Life Laboratory, Uppsala University, Sweden.
Exp Eye Res. 2014 May;122:94-101. doi: 10.1016/j.exer.2014.03.009. Epub 2014 Apr 1.
Topically applied caffeine was recently identified as a promising candidate molecule for cataract prevention. Little is known about the pharmacokinetics for topically applied caffeine. Potential toxicity of 72 mM caffeine on the ocular surface and the lens was qualitatively monitored and no toxic effects were observed. The concentration of caffeine was measured in the lens and the blood after topical application of 72 mM caffeine to groups of 10 animals sacrificed at 30, 60, 90 and 120 min after topical application. The lens concentration decreased throughout the observation period while the blood concentration increased up to 120 min. Further, the concentration of caffeine in the lens and blood was measured 30 min after topical application of caffeine, the concentration of caffeine being 0.72, 3.34, 15.51 and 72 mM depending on group belonging, in groups of 10 animals. The caffeine concentration in lens and blood, respectively, increased proportionally to the caffeine concentration topically applied. The rat blood concentrations achieved were far below the equivalent threshold dose of FDA recommended daily dose for humans. This information is important for further development of caffeine eye drops for cataract prevention.
局部应用的咖啡因最近被确定为预防白内障的有前途的候选分子。关于局部应用咖啡因的药代动力学知之甚少。定性监测了 72mM 咖啡因对眼表面和晶状体的潜在毒性，未观察到毒性作用。在局部应用 72mM 咖啡因后，将其施用于 10 只动物组，在局部应用后 30、60、90 和 120 分钟处死，测量了晶状体和血液中的咖啡因浓度。在整个观察期间，晶状体中的咖啡因浓度降低，而血液中的咖啡因浓度增加至 120 分钟。此外，在局部应用咖啡因后 30 分钟测量了晶状体和血液中的咖啡因浓度，根据所属组，在 10 只动物的组中，咖啡因的浓度分别为 0.72、3.34、15.51 和 72mM。晶状体和血液中的咖啡因浓度分别与局部应用的咖啡因浓度成正比增加。大鼠血液中的浓度远低于 FDA 推荐的每日剂量的等效阈值剂量。这些信息对于进一步开发用于预防白内障的咖啡因眼药水很重要。
