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用于干性年龄相关性黄斑变性的黄芩素纳米乳原位凝胶

Baicalein nanoemulsion in situ GEL for dry age-related macular degeneration.

作者信息

Pan Wanbing, Sun Rong, Yu Yaoyuan, Liu Yuxin, Mu Yinling, Gong Hanyan, Fan Hongxia, Zhang Yingchao, He Lutong, He Haibing, Gou Jingxin, Tang Xing, Yin Tian, Zhang Yu

机构信息

School of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang 110016 Liaoning, China.

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110116, China.

出版信息

Int J Pharm. 2025 Apr 30;675:125494. doi: 10.1016/j.ijpharm.2025.125494. Epub 2025 Mar 17.

DOI:10.1016/j.ijpharm.2025.125494
PMID:40107466
Abstract

Effective management of posterior ocular segment disorders necessitates sustained retinal drug delivery and rational therapeutic selection. Despite significant advances, developing drug delivery systems that simultaneously achieve deep tissue penetration and prolonged ocular surface retention remains challenging. To bridge this gap, we engineered a borneol- decorated baicalein nanoemulsion in-situ gel (Bor/Bai-N@GEL) ophthalmic formulation for dry age-related macular degeneration (d-AMD). The system integrates a borneol-decorated baicalein nanoemulsion with an ion- sensitive hydrogel. Comparative analysis revealed Bor/Bai-N@GEL's superior therapeutic performance, attributable to the prolonged ocular residence time and enhanced transcorneal permeability. Pharmacodynamic profiling demonstrated marked attenuation of inflammatory cytokines, oxidative markers, and apoptotic signaling in murine d-AMD models. In summary, our work provided a meaningful delivery strategy and research basis to treat fundus diseases. This approach offers the potential to conveniently treat early-stage d-AMD at home, improving patient adherence and overall treatment outcomes.

摘要

有效管理眼后段疾病需要持续的视网膜药物递送和合理的治疗选择。尽管取得了重大进展,但开发能够同时实现深部组织渗透和延长眼表滞留时间的药物递送系统仍然具有挑战性。为了弥补这一差距,我们设计了一种用于干性年龄相关性黄斑变性(d-AMD)的冰片修饰黄芩素纳米乳原位凝胶(Bor/Bai-N@GEL)眼科制剂。该系统将冰片修饰的黄芩素纳米乳与离子敏感水凝胶相结合。对比分析显示Bor/Bai-N@GEL具有卓越的治疗性能,这归因于其延长的眼内滞留时间和增强的角膜透过性。药效学分析表明,在小鼠d-AMD模型中,炎性细胞因子、氧化标志物和凋亡信号明显减弱。总之,我们的工作为治疗眼底疾病提供了一种有意义的递送策略和研究基础。这种方法有可能在家中方便地治疗早期d-AMD,提高患者的依从性和整体治疗效果。

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