Department of Ophthalmology, Zhengzhou Central Hospital Affiliated to Zhengzhou University, Zhengzhou City, Henan Province 450007, China.
Department of Ophthalmology, Jiaoyu Ophthalmology Clinic, Xingqing South Road, Southeast Gate of Xi'an Jiaotong University, Beilin District, Xi'an, Shaanxi 710049, China.
J Pharm Sci. 2020 Jun;109(6):1951-1957. doi: 10.1016/j.xphs.2020.02.008. Epub 2020 Feb 15.
Currently, conjunctivitis is treated by frequent high dose administration of sparfloxacin eye drop solution. However, the eye drops are inconvenient because of low bioavailability, short ocular drug residence time, and need of frequent instillation, which lead to patient noncompliance affecting the routine life style of patients. Silicone contact lenses can be used to sustain the release of sparfloxacin. However, the presence of sparfloxacin alters the optical and physical properties of the contact lens. To overcome the issues, a novel polyvinyl pyrrolidone (PVP)-coated sparfloxacin-laden ring contact lens was designed to provide sustained ocular drug delivery without altering the optical and swelling properties of contact lens. The ring was implanted within the periphery of the lens. Sparfloxacin was loaded by soaking (Sp-S), direct loading (Sp-L), and ring casting method (Sp-R). PVP (comfort agent) was coated on the surface of contact lens by novel short surface curing technique. The in vitro sparfloxacin release data of Sp-S (up to 12-36 h) and Sp-L batches (up to 12-24 h) showed high burst release, whereas Sp-R batch showed sustained release up to 36-48 h without significant (p > 0.05) alteration of the optical and swelling properties. All the batches showed sustained release of PVP up to 48 h. The in vivo release studies in the rabbit tear fluid showed improvement in the sparfloxacin [>MIC for Staphylococcus aureus] and PVP retention time in comparison to eye drop solution. The in vivo efficacy study in the S aureus-induced conjunctivitis showed improved healing effect with the single PVP-coated Sp-R-300 contact lens in comparison to the frequent high-dose sparfloxacin eye drop therapy. The study demonstrated the successful application to codeliver sparfloxacin and PVP from the contact lens for the extended period to treat conjunctivitis.
目前，结膜炎的治疗方法是频繁、大剂量使用氧氟沙星滴眼液。然而，由于生物利用度低、眼部药物滞留时间短以及需要频繁滴注，眼药水使用起来并不方便，这导致患者无法遵医嘱用药，影响了患者的日常生活。硅酮隐形眼镜可用于维持氧氟沙星的释放。但是，氧氟沙星的存在会改变隐形眼镜的光学和物理性质。为了解决这些问题，设计了一种新型的聚维酮（PVP）涂层氧氟沙星载药环型隐形眼镜，以提供持续的眼部药物递送，而不会改变隐形眼镜的光学和膨胀特性。该环被植入镜片的周边。氧氟沙星通过浸泡（Sp-S）、直接加载（Sp-L）和环铸法（Sp-R）加载。通过新型短表面固化技术将 PVP（舒适剂）涂覆在接触镜的表面。Sp-S（长达 12-36 小时）和 Sp-L 批次（长达 12-24 小时）的体外氧氟沙星释放数据显示，高突释，而 Sp-R 批次显示出长达 36-48 小时的持续释放，而光学和膨胀特性没有显著变化（p > 0.05）。所有批次均显示 PVP 持续释放长达 48 小时。在兔泪液中的体内释放研究表明，与滴眼液相比，氧氟沙星[金黄色葡萄球菌的 MIC 以上]和 PVP 的保留时间得到了改善。在金黄色葡萄球菌诱导的结膜炎的体内疗效研究中，与频繁的高剂量氧氟沙星滴眼液治疗相比，用单 PVP 涂层 Sp-R-300 隐形眼镜进行治疗显示出更好的愈合效果。该研究成功地将氧氟沙星和 PVP 从隐形眼镜中共同递送至延长的时间，用于治疗结膜炎。
