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Strategic photosafety screening system consisting of in chemico photoreactivity and in vitro skin exposure for quinolone derivatives.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-02-05 , DOI: 10.1016/j.ejps.2020.105257 Yosuke Iyama 1 , Hideyuki Sato 1 , Yoshiki Seto 1 , Satomi Onoue 1
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-02-05 , DOI: 10.1016/j.ejps.2020.105257 Yosuke Iyama 1 , Hideyuki Sato 1 , Yoshiki Seto 1 , Satomi Onoue 1
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The main objective of this study was to verify the applicable domain of a proposed photosafety screening system, consisting of a reactive oxygen species (ROS) assay and in vitro skin permeation test, for dermally-applied chemicals. Quinolones (QNLs) were selected as test compounds, including enoxacin, flumequine, moxifloxacin, nalidixic acid, orbifloxacin, and oxolinic acid. The ROS assay and in vitro skin permeation test were employed to evaluate photoreactivity and skin deposition of QNLs, respectively. All QNLs exhibited significant ROS generation on exposure to simulated sunlight; in particular, enoxacin was indicative of potent photoreactivity compared with the other 5 QNLs. Steady-state concentration values of flumequine and nalidixic acid were calculated to be 5.0 and 8.2 μg/mL, respectively, and higher than those of the other QNLs. Based on the photoreactivity and skin exposure of QNLs, the phototoxic risk was ranked, and the predicted phototoxic risk by the proposed system was mostly in agreement with observed in vivo phototoxicity, suggesting the applicability of the proposed strategy to photosafety assessment of QNLs. The proposed screening would be efficacious to predict phototoxic risk of dermally-applied chemicals.
中文翻译：
战略性的光安全性筛选系统，包括化学光反应性和喹诺酮衍生物的体外皮肤暴露。
这项研究的主要目的是验证所提议的光安全性筛选系统的适用领域，该系统由用于皮肤应用的化学物质的活性氧（ROS）分析和体外皮肤渗透测试组成。选择喹诺酮类（QNLs）作为测试化合物，包括依诺沙星，氟美喹嗪，莫西沙星，萘啶酸，奥比沙星和草酸。用ROS测定法和体外皮肤渗透测试分别评估QNL的光反应性和皮肤沉积。所有QNL在暴露于模拟阳光下均表现出明显的ROS生成；特别是，与其他5个QNL相比，依诺沙星具有较强的光反应性。氟美卡因和萘啶酸的稳态浓度值经计算分别为5.0和8.2μg/ mL，高于其他QNL的稳态浓度值。根据QNL的光反应性和皮肤暴露程度，对光毒性风险进行了排名，并且所提出的系统预测的光毒性风险与观察到的体内光毒性基本一致，这表明所提出的策略可用于QNL的光安全性评估。拟议的筛选将有效地预测皮肤应用化学物质的光毒性风险。
更新日期：2020-02-06
中文翻译：
战略性的光安全性筛选系统，包括化学光反应性和喹诺酮衍生物的体外皮肤暴露。
这项研究的主要目的是验证所提议的光安全性筛选系统的适用领域，该系统由用于皮肤应用的化学物质的活性氧（ROS）分析和体外皮肤渗透测试组成。选择喹诺酮类（QNLs）作为测试化合物，包括依诺沙星，氟美喹嗪，莫西沙星，萘啶酸，奥比沙星和草酸。用ROS测定法和体外皮肤渗透测试分别评估QNL的光反应性和皮肤沉积。所有QNL在暴露于模拟阳光下均表现出明显的ROS生成；特别是，与其他5个QNL相比，依诺沙星具有较强的光反应性。氟美卡因和萘啶酸的稳态浓度值经计算分别为5.0和8.2μg/ mL，高于其他QNL的稳态浓度值。根据QNL的光反应性和皮肤暴露程度，对光毒性风险进行了排名，并且所提出的系统预测的光毒性风险与观察到的体内光毒性基本一致，这表明所提出的策略可用于QNL的光安全性评估。拟议的筛选将有效地预测皮肤应用化学物质的光毒性风险。
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