This study aims to create and evaluate a kaempferol (KAE) ophthalmic solution based on polyvinylpyrrolidone (PVP) nanocomplexes. KAE can be highly complexed with PVP K-17PF (17PF) to formulate an aqueous ophthalmic solution named 17PF-KAE. The optimized 17PF-KAE displays high complexing efficiency, an ultra-small size (8.628 ± 0.066 nm), and good aqueous dispersibility. 17PF-KAE did not show any obvious cytotoxicity or in vivo ocular tissue toxicity. Further, 17PF-KAE was observed to facilitate significant improvement in in vitro parallel artificial membrane permeability, in vitro cellular uptake, and ex vivo corneal permeation of KAE. Regarding the in vivo ocular absorption test, the KAE levels in the cornea and aqueous humor determined from the 17PF-KAE group were much higher than those in the free KAE solution group in addition to conjunctiva and the iris-ciliary body at certain time points. 17PF-KAE was also observed to promote remarkable improvement in in vitro antioxidant activity and in vivo anti-inflammatory activity. Moreover, a topical 17PF-KAE solution in mice eyes showed significant improvement in the treatment efficacy of corneal alkali burns over the free KAE solution. The therapeutic mechanism was also associated with inhibiting the production of key mediators of inflammation (CD54, IL-6, and TGF-β1) and angiogenic factors (VEGF). Therefore, these results demonstrate that 17PF-KAE may be a promising new ophthalmic formulation for the prophylaxis and treatment of oxidative stress and inflammation-related ocular diseases.

中文翻译：

---

基于聚乙烯吡咯烷酮K-17PF的超小型纳米复合物：山萘酚的眼部递送的潜在纳米平台。

这项研究旨在创建和评估基于聚乙烯吡咯烷酮（PVP）纳米复合物的山萘酚（KAE）眼药水。KAE可以与PVP K-17PF（17PF）高度配合，配制出一种名为17PF-KAE的眼科水溶液。经过优化的17PF-KAE具有很高的络合效率，超小尺寸（8.628±0.066 nm）和良好的水分散性。17PF-KAE没有显示任何明显的细胞毒性或体内眼组织毒性。此外，观察到17PF-KAE促进了体外平行人工膜通透性，体外细胞摄取和KAE的离体角膜渗透的显着改善。关于体内眼吸收测试，除了结膜和虹膜睫状体，在某些时间点，由17PF-KAE组测定的角膜和房水中的KAE水平远高于游离KAE溶液组的KAE水平。还观察到17PF-KAE促进体外抗氧化活性和体内抗炎活性的显着改善。此外，与游离KAE溶液相比，在小鼠眼睛中局部使用17PF-KAE溶液显示出对角膜碱烧伤的治疗效果有了显着改善。该治疗机制还与抑制炎症的关键介质（CD54，IL-6和TGF-β1）和血管生成因子（VEGF）的产生有关。因此，