Cai Maoyu, Zhong Haiping, Wang Xindi, Li Liangpin, Zhou Xueyan, Wang Yan, Hua Xia, Guo Shutao, Yuan Xiaoyong
Clinical College of Ophthalmology, Tianjin Medical University, Tianjin, 300020, China.
Tianjin Key Laboratory of Ophthalmology and Visual Science, Tianjin Eye Institute, Tianjin Eye Hospital, Tianjin, 300020, China.
Bioact Mater. 2025 Apr 22;50:396-413. doi: 10.1016/j.bioactmat.2025.04.011. eCollection 2025 Aug.
Fungal keratitis (FK) is a challenging-to-manage blinding corneal infectious disease that often leads to severe sequelae, such as corneal leukoplakia regardless of curative care. Moreover, the unique anatomical structure and tear turnover of the eye significantly limit the bioavailability and therapeutic efficacy of traditional eye drops. Inspired by the unique pathological features of corneal ulcers, we report a thermosensitive multifunctional eye drop, designated PX-TA, based on a poloxamer (PX) and a collagen-adhesive tannic acid (TA), for prolonged and efficient treatment of FK. PX-TA transforms into a gel at body temperature and adheres to exposed collagen at the ulcer site; this significantly improves the corneal retention time and bioavailability. PX-TA maintains corneal retention for at least 90 min, substantially exceeding both the 15-min limit of commercial mucoadhesive eye drops and the 30-min threshold of conventional in situ gels. When loaded with amphotericin B (AmB), once-daily PX-TA-AmB administration effectively suppresses inflammation and corneal scarring, demonstrating superior efficacy over six-times-daily free AmB drops and a good safety profile. Mechanistic investigations reveal that PX-TA-AmB mediates its therapeutic effects through the MAPK6/PI3K/AKT signaling pathway. Moreover, the metal-chelating properties of TA inhibit the copper-dependent enzyme lysyl oxidase (LOX), resulting in reduced matrix fibrosis. Overall, the use of PX-TA-AmB drops represents a simplified yet effective strategy for the potential clinical management of FK, inspiring the design of eye drop formulations.
真菌性角膜炎(FK)是一种难以治疗的致盲性角膜感染性疾病,无论治疗如何,常常会导致严重的后遗症,如角膜白斑。此外,眼睛独特的解剖结构和泪液更新显著限制了传统眼药水的生物利用度和治疗效果。受角膜溃疡独特病理特征的启发,我们报道了一种基于泊洛沙姆(PX)和胶原黏附性单宁酸(TA)的热敏多功能眼药水,命名为PX-TA,用于长期有效治疗FK。PX-TA在体温下转变为凝胶,并黏附于溃疡部位暴露的胶原上;这显著提高了角膜滞留时间和生物利用度。PX-TA可维持角膜滞留至少90分钟,大大超过了市售黏膜黏附性眼药水15分钟的限度以及传统原位凝胶30分钟的阈值。当负载两性霉素B(AmB)时,每日一次给予PX-TA-AmB可有效抑制炎症和角膜瘢痕形成,显示出优于每日六次给予游离AmB眼药水的疗效,且安全性良好。机制研究表明,PX-TA-AmB通过MAPK6/PI3K/AKT信号通路介导其治疗作用。此外,TA 的金属螯合特性抑制了铜依赖性酶赖氨酰氧化酶(LOX),导致基质纤维化减少。总体而言,使用PX-TA-AmB眼药水代表了一种用于FK潜在临床管理的简化而有效的策略,为眼药水制剂的设计提供了灵感。