通过阳离子纳米脂质体增强他克莫司的眼部递送：减轻炎症并重新平衡干眼病中的Th17/Treg反应
Enhanced ocular delivery of tacrolimus via cationic nanoliposomes: Mitigating inflammation and rebalancing Th17/Treg responses in dry eye disease.
摘要(中文译文)
干眼病（DED）是一种常见的眼表疾病，以持续性炎症和免疫失衡为特征，可导致视力损害和生活质量显著下降。尽管局部药物治疗仍是干眼病管理的主要手段，但其疗效常受限于角膜穿透性差、眼部生物利用度低以及长期给药相关的潜在安全性问题。为解决这一问题，我们设计了一种低剂量阳离子型他克莫司纳米脂质体递送系统（FK506 NLPs），旨在提高眼表药物可利用度并靶向免疫炎症失调。带正电荷的纳米脂质体通过黏膜黏附作用表现出延长的角膜滞留时间和改善的药物渗透性。在干眼病小鼠模型中，FK506 NLPs加速了眼表修复，改善了泪膜稳定性，并保护了结膜杯状细胞和泪腺结构。在机制上，FK506 NLPs抑制了角膜和泪腺组织中关键促炎介质的表达，并通过重建Th17细胞与调节性T细胞之间的平衡恢复了免疫稳态。重要的是，FK506 NLPs还表现出良好的生物相容性。综上所述，这些研究结果表明，FK506 NLPs将改善的眼部递送与协同的抗炎和免疫调节作用相结合，凸显了其作为干眼病管理中有前景的治疗策略的潜力。
Abstract
Dry eye disease (DED) is a common ocular surface disorder characterized by persistent inflammation and immune imbalance, leading to visual impairment and substantial deterioration in quality of life. Although topical medications remain the mainstay of DED management, their therapeutic effectiveness is frequently limited by poor corneal penetration, low ocular bioavailability, and potential safety issues associated with long-term administration. To address this, we engineered a low-dose cationic tacrolimus nanoliposome delivery system (FK506 NLPs) designed to enhance ocular surface drug availability while targeting immune-inflammatory dysregulation. The positively charged NLPs exhibited prolonged corneal residence via mucoadhesion and improved drug permeation. In a murine model of DED, FK506 NLPs accelerated ocular surface repair, improved tear film stability, and preserved conjunctival goblet cells and lacrimal gland structure. Mechanistically, they suppressed the expression of key proinflammatory mediators in both corneal and lacrimal tissues and restored immune homeostasis by re-establishing the balance between Th17 and regulatory T cells. Importantly, FK506 NLPs also exhibited favorable biocompatibility. Taken together, these findings demonstrated that FK506 NLPs combined improved ocular delivery with coordinated anti-inflammatory and immunoregulatory effects, highlighting their potential as a promising therapeutic strategy for the management of DED.
如何引用
AMA
Lirui Liu, Dan Chen, Siting Sheng, Xueqi Lin, Huiling Zhao, Chujun Liu, et al. Enhanced ocular delivery of tacrolimus via cationic nanoliposomes: Mitigating inflammation and rebalancing Th17/Treg responses in dry eye disease.. Materials today. Bio. 2026; doi:10.1016/j.mtbio.2026.103248.
APA
Lirui Liu, Dan Chen, Siting Sheng, Xueqi Lin, Huiling Zhao, Chujun Liu, et al (2026). Enhanced ocular delivery of tacrolimus via cationic nanoliposomes: Mitigating inflammation and rebalancing Th17/Treg responses in dry eye disease.. Materials today. Bio. https://doi.org/10.1016/j.mtbio.2026.103248
GB/T 7714
Lirui Liu, Dan Chen, Siting Sheng, Xueqi Lin, Huiling Zhao, Chujun Liu, et al. Enhanced ocular delivery of tacrolimus via cationic nanoliposomes: Mitigating inflammation and rebalancing Th17/Treg responses in dry eye disease.[J]. Materials today. Bio, 2026 doi:10.1016/j.mtbio.2026.103248.
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