Improving sustained drug delivery from ophthalmic lens materials through the control of temperature and time of loading
Improving sustained drug delivery from ophthalmic lens materials through the control of temperature and time of loading
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DOI：
10.1016/j.ejps.2018.02.017
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发表时间：
2018-05
影响因子：
4.6
通讯作者：
A. Topete;A. Oliveira;Anabela C. Fernandes;T. Nunes;A. P. Serro;B. Saramago
中科院分区：
文献类型：
--
作者：
A. Topete;A. Oliveira;Anabela C. Fernandes;T. Nunes;A. P. Serro;B. Saramago
虽然使用载药眼镜片来促进药物缓释的可能性已经得到了彻底的探索，但与不同的替代品相关的问题仍然有待解决。在这项工作中，我们回到了传统的药物溶液浸泡载药的方法，并试图通过改变加载温度和时间来优化释放曲线。选择了两种市面上可买到的材料，名称分别为CI26Y和Definitive 50。CI26Y用于人工晶状体(IOL)，Definitive 50用于软性隐形眼镜(SCL)。测试了三种药物：抗生素莫西沙星和两种抗炎药双氯芬酸和酮咯酸。莫西沙星和双氯芬酸可使载药温度提高到60 °C或将载药时间延长到2个月，可获得至少15 d的药物缓释。酮咯酸的缓释时间限制在8 d左右。相反，改变加载条件并不能改善最终的50个圆盘的药物释放。用固体核磁共振和差示扫描量热法解释了负载条件对药物释放行为的影响。这些研究表明，CI26Y与药物莫西沙星和双氯芬酸之间存在可逆的吸热相互作用。负载温度对载药的CI26Y样品的力学和光学性能影响不大，仍保持了作为人工晶状体材料的良好性能。用一个简化的数学模型来估计房水中的药物浓度，以预测在60 °C下载药两周的CI_(26)Y样品的体内疗效。估计的浓度被发现符合治疗需要，至少是莫西沙星和双氯芬酸。
Although the possibility of using drug-loaded ophthalmic lens to promote sustained drug release has been thoroughly pursued, there are still problems to be solved associated to the different alternatives. In this work, we went back to the traditional method of drug loading by soaking in the drug solution and tried to optimize the release profiles by changing the temperature and the time of loading. Two materials commercially available under the names of CI26Y and Definitive 50 were chosen. CI26Y is used for intraocular lenses (IOLs) and Definitive 50 for soft contact lenses (SCLs). Three drugs were tested: an antibiotic, moxifloxacin, and two anti-inflammatories, diclofenac and ketorolac. Sustained drug release from CI26Y disks for, at least 15 days, was obtained for moxifloxacin and diclofenac increasing the loading temperature up to 60 °C or extending the loading time till two months. The sustained release of ketorolac was limited to about 8 days. In contrast, drug release from Definitive 50 disks could not be improved by changing the loading conditions. An attempt to interpret the impact of the loading conditions on the drug release behavior was done using solid-state NMR and differential scanning calorimetry. These studies suggested the establishment of reversible, endothermic interactions between CI26Y and the drugs, moxifloxacin and diclofenac. The loading temperature had a slight effect on the mechanical and optical properties of drug loaded CI26Y samples, which still kept adequate properties to be used as IOL materials. Thein vivoefficacy of CI26Y samples, drug loaded at 60 °C for two weeks, was predicted using a simplified mathematical model to estimate the drug concentration in the aqueous humor. The estimated concentrations were found to comply with the therapeutic needs, at least, for moxifloxacin and diclofenac.