Chen Xiang, Wu Jicheng, Lin Xueqi, Wu Xingdi, Yu Xuewen, Wang Ben, Xu Wen
Eye Center, The Second Affiliated Hospital of Zhejiang University School of Medicine, Hangzhou, China.
Cancer Institute (Key Laboratory of Cancer Prevention and Intervention, China National Ministry of Education), The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China.
Front Pharmacol. 2022 Feb 4;13:838168. doi: 10.3389/fphar.2022.838168. eCollection 2022.
Eye drops are ophthalmic formulations routinely used to treat dry eye. However, the low ocular bioavailability is an obvious drawback of eye drops owing to short ocular retention time and weak permeability of the cornea. Herein, to improve the ocular bioavailability of eye drops, a cationic liposome eye drop was constructed and used to treat dry eye. Tacrolimus liposomes exhibit a diameter of around 300 nm and a surface charge of +30 mV. Cationic liposomes could interact with the anionic ocular surface, extending the ocular retention time and improving tacrolimus amount into the cornea. The cationic liposomes notably prolonged the ocular retention time of eye drops, leading to an increased tacrolimus concentration in the ocular surface. The tacrolimus liposomes were also demonstrated to reduce reactive oxygen species and dry eye-related inflammation factors. The use of drug-loaded cationic liposomes is a good formulation in the treatment of ocular disease; the improved ocular retention time and biocompatibility give tremendous scope for application in the treatment of ocular disease, with further work in the area recommended.
眼药水是常用于治疗干眼症的眼科制剂。然而，由于眼内滞留时间短和角膜通透性弱，眼药水的低眼生物利用度是一个明显的缺点。在此，为了提高眼药水的眼生物利用度，构建了一种阳离子脂质体眼药水并用于治疗干眼症。他克莫司脂质体的直径约为300纳米，表面电荷为+30毫伏。阳离子脂质体可与阴离子眼表相互作用，延长眼内滞留时间并提高他克莫司进入角膜的量。阳离子脂质体显著延长了眼药水的眼内滞留时间，导致眼表他克莫司浓度增加。他克莫司脂质体还被证明可减少活性氧和干眼症相关炎症因子。载药阳离子脂质体的应用是治疗眼部疾病的良好制剂；改善的眼内滞留时间和生物相容性为眼部疾病的治疗提供了巨大的应用空间，建议在该领域进一步开展工作。
