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克服在眼科纳米乳液中几乎不能溶解的 loteprednol etabonate 配方中的障碍
Josip Ljubica1, Bisera Jurišić Dukovski2, Iva Krtalić3
1University of Zagreb Faculty of Pharmacy and Biochemistry, Ante Kovačića 1, 10000 Zagreb, Croatia.
概括
一种新的油在水纳米乳液有效地提供 loteprednol etabonate (LE) 用于干眼治疗. 这种配方增强了对角膜上皮的LE吸收,提供了一个有前途的治疗方法.
科学领域:
- 眼科医生 眼科 眼科
- 药品制造 药品制造 药品制造
- 材料科学 材料科学 材料科学
背景情况:
- 洛特普雷德诺乙酸盐 (LE) 是一种用于治疗干眼疾病的软皮质类固醇.
- 目前的LE悬浮剂提供有限的眼表面药物释放和吸收.
- 需要增强的传递系统来提高LE的生物利用性.
研究的目的:
- 开发一种油在水纳米乳液 (NE),以改善 loteprednol etabonate (LE) 的输送.
- 评估开发的LE-NE的生物相容性和物理稳定性.
- 在模拟生理条件下调查LE释放和保留.
主要方法:
- 开发一个扩展通量3D角膜表皮模型.
- 使用选定的辅助剂 (油,Capryol® 90,Kolliphor® EL,Soluplus®) 制备油在水中的纳米乳液.
- 为优化设计实验;评估LE含量,保留和稳定性的评估.
- 生物相关的稀释研究来模拟眼周转效应.
主要成果:
- 成功开发了一种生物相容和物理稳定的LE-NE配方 (0.15%w/wLE).
- 在NE油滴 (>90%) 中实现了高的LE保留效率 (87%在10个月后).
- 尽管模拟了眼流量,但证明了持续的LE可用性,这表明角膜吸收的可能性.
结论:
- 开发的LE-NE配方显示出在干眼疾病中增强眼部药物递送的显著潜力.
- 该配方的稳定性和高LE保留率支持其适用于局部眼部应用的适用性.
- 需要进一步的体外和体内研究来确认透性和生物可用性.
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