Department of Pharmaceutics, College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, PR China.
Department of Pharmacy, Fuwai Hospital Chinese Academy of Medical Sciences, Shenzhen, PR China.
Expert Opin Drug Deliv. 2020 Apr;17(4):603-619. doi: 10.1080/17425247.2020.1735348. Epub 2020 Mar 9.
: Lutein is the primary macular pigment with an favorable effect on the treatment of age-related macular degeneration (AMD). However, the poor water solubility of lutein hinders its absorption and delivery. In this study, a penetratin-modified lutein nanoemulsion gel (GEL) was prepared for the treatment of AMD.: A nanoemulsion (NE) was prepared and modified with penetratin (P-NE) to improve the penetration. The effect of penetratin was evaluated by cell uptake and intraocular distribution assays. A dry AMD model was induced using NaIO, and the therapeutic effect was evaluated by electroretinography, the number of apoptosis cells and the reactive oxygen species (ROS) level.: Lutein showed a good ability to protect ARPE-19 from the damage of HO and the uptake rate of P-NE was significantly higher than NE. In the efficacy experiments, the structure of retina was significantly improved after treatment, the apoptosis rate decreased from 31.98% to 2.05%, and the level of ROS was significantly decreased ( < 0.0001).: With the aid of penetratin, lutein could be delivered to the retina effectively. The P-NE GEL could evidently inhibit the apoptosis and ROS, demonstrating that the P-NE GEL has a good application prospect in the treatment of AMD.
叶黄素是主要的黄斑色素，对治疗年龄相关性黄斑变性（AMD）有良好的效果。然而，叶黄素的水溶性差阻碍了其吸收和传递。在这项研究中，制备了一种穿透肽修饰的叶黄素纳米乳凝胶（GEL），用于治疗 AMD。
制备了纳米乳（NE）并通过穿透肽（P-NE）进行修饰以提高穿透性。通过细胞摄取和眼内分布试验评估穿透肽的效果。使用 NaIO 诱导干性 AMD 模型，并通过视网膜电图、凋亡细胞数量和活性氧（ROS）水平评估治疗效果。
叶黄素显示出良好的保护 ARPE-19 免受 HO 损伤的能力，并且 P-NE 的摄取率明显高于 NE。在疗效实验中，经治疗后视网膜结构明显改善，凋亡率从 31.98%降至 2.05%，ROS 水平显著降低（<0.0001）。
在穿透肽的辅助下，叶黄素可以有效地递送到视网膜。P-NE GEL 可以明显抑制细胞凋亡和 ROS，表明 P-NE GEL 在治疗 AMD 方面具有良好的应用前景。
