眼睛的CATIONIC 基于纳米载体的POSACONAZOLE的交付
Sagar Kothawade1, Ashlesha Pandit2, Udhav Bagul3
1Department of Pharmaceutics, Sinhgad Technical Education Society's Sinhgad College of Pharmacy (Affiliated to SPPU), Vadgoan (Bk), Pune, Maharashtra, 411041, India.
Annales pharmaceutiques francaises
|December 24, 2025
概括
一种新型的阴离子纳米载体配方 (leciplex) 有效地将波萨可纳输送到眼睛,增强抗真菌治疗真菌角膜炎的效果. 这种先进的输送系统显示出改善的角膜保留和安全性,为眼睛感染提供了有前途的解决方案.
科学领域:
- 眼科医生 眼科 眼科
- 药品制造 药品制造 药品制造
- 纳米技术纳米技术
背景情况:
- 在全球范围内,眼球真菌角膜炎的发病率正在增加,特别是在免疫受损的个体中.
- 眼睛障碍物,如角膜上皮和眼流量,阻碍了有效的药物输送和治疗结果.
- 阴离子纳米载体系统是克服这些药物输送挑战的有希望的策略.
研究的目的:
- 开发和表征一种新型的波萨康纳加载的阴离子纳米载体配方 (leciplex),用于增强眼部输送.
- 为了优化 leciplex 配方,使用 3^2 的全因数设计来对关键参数如粒子大小,捕获效率和泽塔潜力进行优化.
- 评估Posaconazole leciplex的体外和体外性能,包括透,角膜保留,粘膜粘合,眼睛安全性和抗真菌功效.
主要方法:
- 用Posaconazole装载的阴离子纳米载体 (leciplex) 通过一步技术使用大豆酸盐胆,二甲基二甲基氨基化物和Transcutol HP进行制造.
- 采用了3 ^ 2的全因数设计来优化粒子大小,捕获效率和泽塔潜力.
- 评估了体外透,体外角膜保留,粘膜凝固,眼睛安全性 (眼测试) 和对白菌候的抗真菌活性.
主要成果:
- 优化的leciplex表现出球形,小颗粒大小 (162.5±3.4 nm),高捕获效率 (97.7±1.8%),以及正的泽塔电位 (+62.5 mV).
- 试验室研究显示持续的药物透,ex vivo分析显示显著的角膜保留 (45.6%) 和长时间的眼部停留.
- 粘膜粘合性研究证实了对角膜层的强烈结合,而眼睛测试表明没有眼部刺激或毒性.
- 与药物溶液相比,抗真菌试验显示波萨科纳莱西普莱克斯对氏菌的有效性显著提高.
结论:
- 开发的含有波萨康纳的阴性莱西普莱克斯配方有效地将抗真菌剂传递到角膜表面.
- 莱西普勒克斯配方通过与角膜粘膜层的静电相互作用,表现出有利的粘膜粘合,导致长时间的停留和增强的药物透.
- 该研究证实了leciplex的眼部安全性和生物相容性,强调其作为治疗真菌角膜炎的先进治疗系统的潜力.
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