凯托洛拉克,黑激素和拉坦诺普罗斯特三重装载的PLGA微球,用于青光眼中神经保护
Miriam Ana González-Cela-Casamayor1,2, María J Rodrigo3,4, Marco Brugnera1,2,5
1Innovation, Therapy and Pharmaceutical Development in Ophthalmology (InnOftal) Research Group, UCM 920415, Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, Madrid, Spain.
Drug delivery
|April 11, 2025
概括
这项研究开发了新型可生物降解的微球,装有低血压,抗氧化和抗炎药物,用于持续治疗眼. 微球表现出良好的细胞耐受性,并有效降低了老鼠的眼内压力.
科学领域:
- 眼科医生 眼科 眼科
- 生物材料科学 生物材料科学
- 神经科学是一个神经科学.
背景情况:
- 玻璃眼是不可逆转的失明的主要原因,其特点是逐渐损伤视神经.
- 目前的治疗方法往往需要频繁的管理,可能无法解决疾病的所有方面.
- 开发持续释放药物输送系统对于改善患者服药性和治疗结果至关重要.
研究的目的:
- 将低血压 (拉塔诺普罗斯特),抗氧化剂 (美拉素) 和抗炎症 (凯托洛拉克) 剂共同封装成聚 (乳酸-同-葡萄糖酸) (PLGA) 微球.
- 为了创建一个长期起作用的内视膜输送系统,用于治疗青光眼.
- 为了评估安全性,药物释放动力学和多重载荷微球在临床前玻璃眼瘤模型中的治疗效果.
主要方法:
- 可生物降解的聚 (乳酸-co-糖酸) (PLGA) 微球 (MSs) 使用油在水乳液溶剂提取-蒸发技术制造.
- 用维生素E作为添加剂的含有黑素,黄素和拉坦诺普罗斯特的三重载荷微球 (KMLVE) 在物理化学上进行了表征.
- 在70天内持续释放药物得到证实,并在视网膜色素上皮细胞中评估了配方的生物相容性.
- 内注射KMLVE给了长埃文斯老鼠,这些老鼠患有诱导的慢性玻璃眼瘤,随后进行了眼科评估.
主要成果:
- 该KMLVE配方表现出有利的颗粒大小 (33.58±5.44μm) 和药物负载.
- 三次装载维生素E的MS在24小时后显示出高视网膜色素表皮细胞活力 (>90%).
- 在体内研究表明,与未经治疗的对照组相比,接受治疗的玻璃眼病老鼠可以显著降低眼内压力.
- 在接受治疗的动物中,光学连贯性断层扫描显示了增强的神经网膜厚度和改善视网膜质细胞功能.
结论:
- 在PLGA微球中同时封装拉坦诺普罗斯特,黑激素和凯托洛拉克,为玻璃眼提供了一个有前途的持续释放系统.
- KMLVE配方耐受性良好,有效降低眼内压力,并保持视网膜结构,在慢性青光瘤的老鼠模型中.
- 这种多种药物输送方法为改善青光眼的管理提供了潜在的战略,减少了重复管理的需要.
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