Department of Ophthalmology, Shaanxi Provincial People's Hospital, Shaanxi 710068, China.
Innoscience Research Sdn Bhd, Jalan USJ 25/1, Subang Jaya, Selangor 47650, Malaysia.
J Pharm Sci. 2020 May;109(5):1714-1724. doi: 10.1016/j.xphs.2020.01.022. Epub 2020 Jan 31.
Olopatadine HCl is an antiallergic drug used for the management of allergic conjunctivitis. Currently, it is delivered via eye drop solution, which is highly inefficient due to low bioavailability. Silicone contact lenses can be used to sustain the release of ophthalmic drugs. However, the presence of drug alters the optical transmittance and physical properties of the contact lens. The objective was to design a novel polyvinyl pyrrolidone (PVP)-coated olopatadine-ethyl cellulose microparticles-laden doughnut contact lens to sustained ocular delivery with limited alteration to the optical and swelling properties of the contact lens. The doughnut was implanted within the periphery of the lens using modified casting technique. Olopatadine HCl was loaded by soaking (SM-OL), direct loading (DL-OL), and doughnut casting method (DNT-OL). PVP (comfort agent) was loaded on the surface of contact lens for all the batches via novel curing technique. The in vitro olopatadine HCl release data of SM-OL (up to 48-72 h) and DL-OL batches (up to 72 h) showed high burst release, whereas DNT-OL batch showed sustained release up to 120 h without significant (p > 0.05) alteration in the optical and swelling properties of contact lens. All the batches showed sustained release of PVP up to 120 h. The in vivo studies in the rabbit tear fluid showed improvement in the olopatadine HCl and PVP retention time in comparison to eye drop solution. The PVP-loaded DNT-OL-500 lens showed tear stabilization (comfort wear) in Schirmer strip test (rabbits) with no protein adherence in comparison to DNT-OL-500 lens without PVP. The study demonstrated the successful delivery of olopatadine HCl and PVP-K30 from the doughnut contact lens for the extended period with limited alteration to the optical and swelling properties of contact lens.
盐酸奥洛他定是一种用于治疗过敏性结膜炎的抗过敏药物。目前，它通过眼药水溶液给药，但由于生物利用度低，效率非常低。硅酮隐形眼镜可用于维持眼用药物的释放。然而，药物的存在会改变隐形眼镜的光透射率和物理性质。本研究旨在设计一种新型的聚乙烯吡咯烷酮（PVP）涂层的盐酸奥洛他定-乙基纤维素微球载药甜甜圈隐形眼镜，以实现有限改变隐形眼镜的光学和膨胀性能的情况下持续眼部给药。通过改良铸模技术将甜甜圈植入镜片的周边。盐酸奥洛他定通过浸泡（SM-OL）、直接加载（DL-OL）和甜甜圈铸模法（DNT-OL）进行加载。所有批次均通过新型固化技术在接触镜表面加载 PVP（舒适剂）。SM-OL（长达 48-72 小时）和 DL-OL 批次（长达 72 小时）的体外盐酸奥洛他定释放数据显示，药物突释较高，而 DNT-OL 批次在不显著改变（p＞0.05）隐形眼镜光学和膨胀性能的情况下，可达到长达 120 小时的持续释放。所有批次均能持续释放 PVP 长达 120 小时。在兔泪液中的体内研究表明，与滴眼剂相比，盐酸奥洛他定和 PVP 的保留时间得到了改善。与未加载 PVP 的 DNT-OL-500 镜片相比，PVP 负载的 DNT-OL-500 镜片在 Schirmer 条试验（兔子）中显示出泪液稳定性（舒适佩戴），且无蛋白黏附。该研究表明，从甜甜圈隐形眼镜中成功地递达了盐酸奥洛他定和 PVP-K30，延长了药物释放时间，同时对隐形眼镜的光学和膨胀性能的改变有限。
