Penetration of 0.3% ciprofloxacin, 0.3% ofloxacin, and 0.5% moxifloxacin into the cornea and aqueous humor of enucleated human eyes

We aimed to quantify the penetration of ciprofloxacin, ofloxacin, and moxifloxacin into the cornea and aqueous humor of cadaver eyes. A total of 60 enucleated eyes, not eligible for corneal transplantation, were divided into three groups and immersed in commercial solutions of 0.3% ciprofloxacin, 0.3% ofloxacin, or 0.5% moxifloxacin for 10 min. Whole corneas and samples of aqueous humor were then harvested and frozen, and drug concentrations analyzed by liquid chromatography tandem mass spectrometry. The mean corneal concentration of moxifloxacin was twice as high as ofloxacin, and the latter was twice as high as ciprofloxacin. The mean concentration of moxifloxacin in the aqueous humor was four times higher than the other antibiotics, and the mean concentrations of ciprofloxacin and ofloxacin were statistically similar. The amount of drug that penetrated the anterior chamber after a 10-min immersion was far below the safe limit of endothelial toxicity of each preparation. Moxifloxacin demonstrated far superior penetration into the cornea and anterior chamber of cadaver eyes compared to ciprofloxacin and ofloxacin. One should not expect endothelial toxicity with the commercial eye drops of ciprofloxacin, ofloxacin, and moxifloxacin that reach the anterior chamber through the cornea.

本研究旨在量化环丙沙星（ciprofloxacin）、氧氟沙星（ofloxacin）及莫西沙星（moxifloxacin）在尸体眼角膜与房水中的渗透情况。本研究共纳入60只不符合角膜移植适应证的摘除眼球，将其分为三组，分别浸泡于0.3%环丙沙星、0.3%氧氟沙星及0.5%莫西沙星的市售滴眼液中，持续10分钟。随后采集完整角膜及房水样本并进行冷冻保存，采用液相色谱-串联质谱法（liquid chromatography tandem mass spectrometry）分析药物浓度。莫西沙星的平均角膜药物浓度为氧氟沙星的2倍，氧氟沙星的平均浓度又为环丙沙星的2倍。房水中莫西沙星的平均药物浓度较其余两种抗生素高出4倍，环丙沙星与氧氟沙星的平均药物浓度在统计学上无显著差异。浸泡10分钟后渗透进入前房的药物剂量，远低于各制剂的内皮毒性安全阈值。相较于环丙沙星与氧氟沙星，莫西沙星在尸体眼角膜与前房中的渗透性能显著更优。经角膜渗透进入前房的市售环丙沙星、氧氟沙星及莫西沙星滴眼液，不会引发内皮毒性反应。