Background: Lutein is the primary macular pigment with an especially 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 based electrolyte triggered in-situ gel (GEL) was prepared for the treatment of AMD.Methods: A nanoemulsion (NE) was prepared and modified with penetratin (P-NE) to improve the penetration of NE. The effect of penetratin on permeability was evaluated by cell uptake and intraocular distribution assays. A dry AMD model was induced in mice using NaIO3, and after treatment the therapeutic effect was evaluated by electroretinography (ERG), the number of apoptosis cells and the reactive oxygen species (ROS) level in the eye.Results: Lutein showed a good ability to protect ARPE-19 from the damage of H2O2. Cell uptake and intraocular distribution assays showed that the uptake rate of P-NE was significantly higher than that of NE. In the in vivo efficacy experiments, the structure of retina was significantly improved after treatment with P-NE GEL, the apoptosis rate of retinal cells decreased from 31.98% (control) to 2.05% and the level of ROS in retina was significantly decreased (P <0.0001).Conclusions: With the aid of penetratin, lutein could be delivered to the retina effectively via a noninvasive administration route. The P-NE GEL could evidently inhibit the apoptosis and ROS induced by oxidative stress, demonstrating that the P-NE GEL has a good application prospect in the treatment of AMD.

中文翻译：

---

Penetratin修饰的叶黄素纳米乳液原位凝胶用于治疗年龄相关性黄斑变性。

背景：叶黄素是主要的黄斑色素，对治疗与年龄有关的黄斑变性（AMD）具有特别有利的作用。然而，叶黄素的水溶性差阻碍了其吸收和递送。本研究制备了一种以渗透素修饰的叶黄素纳米乳液为基础的电解质触发原位凝胶（GEL），用于治疗AMD。方法：制备了纳米乳液（NE）并以渗透素（P-NE）进行修饰以提高其渗透性。 NE。通过细胞摄取和眼内分布测定评估了渗透素对渗透率的作用。用NaIO3诱导小鼠产生干AMD模型，治疗后通过视网膜电图（ERG），眼睛中的凋亡细胞数和活性氧（ROS）水平评估治疗效果。叶黄素显示出保护ARPE-19免受H2O2损害的良好能力。细胞摄取和眼内分布测定表明，P-NE的摄取率显着高于NE。在体内功效实验中，经P-NE GEL处理后，视网膜的结构得到了显着改善，视网膜细胞的凋亡率从31.98％（对照）降低到2.05％，并且视网膜中的ROS水平显着降低（P <0.0001）。结论：借助于渗透素，可通过无创给药途径将叶黄素有效地递送至视网膜。P-NE GEL可以明显抑制氧化应激诱导的细胞凋亡和ROS，表明P-NE GEL在治疗AMD中具有良好的应用前景。细胞摄取和眼内分布测定表明，P-NE的摄取率显着高于NE。在体内功效实验中，经P-NE GEL处理后，视网膜的结构得到了显着改善，视网膜细胞的凋亡率从31.98％（对照）降低到2.05％，并且视网膜中的ROS水平显着降低（P <0.0001）。结论：借助渗透素，可通过无创给药途径将叶黄素有效地递送至视网膜。P-NE GEL可以明显抑制氧化应激诱导的细胞凋亡和ROS，表明P-NE GEL在治疗AMD中具有良好的应用前景。细胞摄取和眼内分布测定表明，P-NE的摄取率显着高于NE。在体内功效实验中，经P-NE GEL处理后，视网膜的结构得到了显着改善，视网膜细胞的凋亡率从31.98％（对照）降低到2.05％，并且视网膜中的ROS水平显着降低（P <0.0001）。结论：借助渗透素，可通过无创给药途径将叶黄素有效地递送至视网膜。P-NE GEL可以明显抑制氧化应激诱导的细胞凋亡和ROS，表明P-NE GEL在治疗AMD中具有良好的应用前景。P-NE GEL治疗后视网膜结构明显改善，视网膜细胞凋亡率从31.98％（对照组）下降至2.05％，视网膜中ROS水平明显降低（P <0.0001）。叶黄素可以通过无渗透给药途径有效地传递到视网膜上。P-NE GEL可以明显抑制氧化应激诱导的细胞凋亡和ROS，表明P-NE GEL在治疗AMD中具有良好的应用前景。P-NE GEL治疗后视网膜结构明显改善，视网膜细胞凋亡率从31.98％（对照组）下降至2.05％，视网膜中ROS水平明显降低（P <0.0001）。叶黄素可以通过无渗透给药途径有效地传递到视网膜上。P-NE GEL可以明显抑制氧化应激诱导的细胞凋亡和ROS，表明P-NE GEL在治疗AMD中具有良好的应用前景。叶黄素可以通过无创给药途径有效地传递到视网膜。P-NE GEL可以明显抑制氧化应激诱导的细胞凋亡和ROS，表明P-NE GEL在治疗AMD中具有良好的应用前景。叶黄素可以通过无创给药途径有效地传递到视网膜。P-NE GEL可以明显抑制氧化应激诱导的细胞凋亡和ROS，表明P-NE GEL在治疗AMD中具有良好的应用前景。