Li Jiani, Ma Panqin, Guo Shujia, Qin Danyi, Wang Yuqian, Liu Yuwen, Yang Zixuan, Huang Caihong, Han Yi, Liu Zuguo
Xiamen University Affiliated Xiamen Eye Center, Fujian Provincial Key Laboratory of Ophthalmology and Visual Science, Fujian Engineering and Research Center of Eye Regenerative Medicine, Eye Institute of Xiamen University, School of Medicine, Xiamen University, Xiamen 361005, China.
Department of Ophthalmology, The First Affiliated Hospital of University of South China, Hengyang Medical School, University of South China, Hengyang 421001, China.
Pharmaceutics. 2025 Mar 4;17(3):332. doi: 10.3390/pharmaceutics17030332.
Blepharitis is a condition often caused by infestations, resulting in significant ocular discomfort and surface damage. Current treatments offer only temporary relief and fail to eliminate mites effectively. This study evaluates nano-niclosamide (nano-NCL), a lipophilic nanosuspension designed to enhance solubility and permeability, for targeting . Nano-NCL was characterized by particle size, zeta potential, transmission electron microscopy, pH measurement, bacterial culture, and HPLC. Viable Demodex mites were collected from patients' eyelashes and assigned to six treatment groups: DDW, F127, 0.15% nano-NCL, 0.3% nano-NCL, 20% TTO, and Okra. Mite survival was analyzed using Kaplan-Meier curves. The ocular surface safety was assessed via slit-lamp examination, corneal fluorescein staining, and in vivo confocal microscopy. The nano-NCL particles are uniformly rod-shaped, approximately 291 nm in size, and exhibit good stability, remaining suspended in various media for up to 20 days. The formulation has a stable pH of 6 and demonstrated no bacterial growth, indicating sterility and suitability for clinical use. In vitro, both 0.15% (/) and 0.30% (/) nano-NCL significantly reduced Demodex survival, with mortality rates ranging from 70.6% to 92.3% within 2 h. Safety evaluations showed minimal corneal staining and inflammation. Notably, 0.15% nano-NCL displayed efficacy comparable to that of 20% tea tree oil (TTO) and Okra, which are established anti-Demodex treatments. Nano-NCL, particularly at 0.15%, rapidly eliminates mites while maintaining excellent ocular tolerability, making it a promising treatment for Demodex-related ocular surface diseases.
睑缘炎是一种常由寄生虫感染引起的病症，会导致严重的眼部不适和眼表损伤。目前的治疗方法只能提供暂时缓解，无法有效清除螨虫。本研究评估了纳米氯硝柳胺（nano-NCL），这是一种旨在提高溶解度和渗透性的亲脂性纳米混悬液，用于靶向治疗。通过粒度、zeta电位、透射电子显微镜、pH测量、细菌培养和高效液相色谱对nano-NCL进行了表征。从患者睫毛上收集活的蠕形螨，并将其分为六个治疗组：双蒸水（DDW）、泊洛沙姆F127（F127）、0.15% nano-NCL、0.3% nano-NCL、20%茶树油（TTO）和秋葵。使用Kaplan-Meier曲线分析螨虫存活率。通过裂隙灯检查、角膜荧光素染色和体内共聚焦显微镜评估眼表安全性。nano-NCL颗粒呈均匀的棒状，大小约为291nm，具有良好的稳定性，可在各种介质中悬浮长达20天。该制剂的pH稳定在6，未显示细菌生长，表明无菌且适合临床使用。在体外，0.15%（/）和0.30%（/）的nano-NCL均能显著降低蠕形螨的存活率，2小时内死亡率在70.6%至92.3%之间。安全性评估显示角膜染色和炎症极小。值得注意的是，0.15%的nano-NCL显示出与20%茶树油（TTO）和秋葵相当的疗效，而TTO和秋葵是已确立的抗蠕形螨治疗方法。nano-NCL，尤其是0.15%的nano-NCL，能快速清除螨虫，同时保持极佳的眼耐受性，使其成为治疗与蠕形螨相关的眼表疾病的有前景的治疗方法。
