保护作用和加强黄素在视网膜细胞中的细胞内吸收,使用自乳化药物递送系统 (SNEDDS)
Elide Zingale1,2,3, Sebastiano Masuzzo1, Tatu Lajunen4,5
1Department of Drug and Health Sciences, University of Catania, 95125 Catania, Italy.
Pharmaceuticals (Basel, Switzerland)
|February 26, 2025
概括
这项研究开发了黄素 (CUR) 的自纳米乳化药物输送系统 (SNEDDS),用于治疗糖尿病视网膜病变 (DR). 这种新的CUR-SNEDDS配方增强了眼部输送,抗氧化活性和视网膜细胞中的Sirtuin-1 (SIRT1) 表达.
科学领域:
- 眼部药理学和药物输送
- 生物医学工程 生物医学工程
- 分子生物学分子生物学
背景情况:
- 赛尔图因-1 (SIRT1) 对于保护眼组织免受退行性疾病的影响至关重要.
- 降低SIRT1水平与糖尿病视网膜病变 (DR) 有关,需要使用SIRT1增强疗法.
- 黄素 (CUR) 是一种潜在的SIRT1激动剂,但其溶解性差和眼球透性限制局部输送.
研究的目的:
- 开发和表征自纳米乳化药物递送系统 (SNEDDS) 用于局部眼部递送黄素 (CUR).
- 评估CUR-SNEDDS在增强CUR递送,抗氧化活性和SIRT1表达在视网膜细胞中的有效性.
主要方法:
- 经过与模拟液溶解后,优化CUR载荷的SNEDDS被准备并进行物理化学和技术性质的表征.
- 试验室评估包括捕获效率,稳定性,药物释放,粘合性,对人类角膜上皮细胞 (HCE) 的细胞毒性,视网膜色素上皮细胞 (ARPE-19) 中的抗氧化活性和细胞吸收.
- 在使用CUR-SNEDDS治疗后测量了SIRT1表达水平.
主要成果:
- CUR-SNEDDS在模拟的眼液中表现出高的捕获效率 (~99%) 和稳定性.
- 与自由CUR相比,修改后的CUR-SNEDDS显示出增强的粘膜粘合和优越的抗氧化活性.
- CUR-SNEDDS表现出良好的细胞相容性,在视网膜细胞中增加细胞吸收,并有效诱导SIRT1表达.
结论:
- 开发的CUR-SNEDDS是一种有前途的配方,用于局部眼部递送黄素.
- 这些系统提供了改善的视网膜输送,抗氧化作用,以及对DR的潜在治疗益处.
- 增强的细胞吸收和SIRT1诱导突显了SNEDDS在治疗眼部疾病方面的潜力.
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