Penetratin-modified lutein nanoemulsion in-situ gel for the treatment of age-related macular degeneration. (2nd April 2020)

• Record Type: Journal Article
• Authors: Ge, Ying; Zhang, Anan; Sun, Rong; Xu, Jiawen; Yin, Tian; He, Haibing; Gou, Jingxin; Kong, Jun; Zhang, Yu; Tang, Xing
• Is Part Of: Expert opinion on drug delivery. Volume 17:Number 4(2020)
• Page Start: 603
• Page End: 619
• Publication Date: 2020-04-02
• Subjects: Age-related macular degeneration -- lutein -- nanoemulsion -- penetratin -- in-situ gel -- antioxidant; Drug delivery devices -- Periodicals; Drug delivery systems -- Periodicals; 615.605
• DOI: 10.1080/17425247.2020.1735348
• Languages: English
• ISSNs: 1742-5247

Abstract

ABSTRACT: Background : 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 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. The effect of penetratin was evaluated by cell uptake and intraocular distribution assays. A dry AMD model was induced using NaIO3, and the therapeutic effect was evaluated by electroretinography, the number of apoptosis cells and the reactive oxygen species (ROS) level. Results : Lutein showed a good ability to protect ARPE-19 from the damage of H2 O2 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 ( p < 0.0001). Conclusions : 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.