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Penetratin-modified lutein nanoemulsion in-situ gel for the treatment of age-related macular degeneration

Ying Ge,Anan Zhang,Rong Sun,Jiawen Xu,Tian Yin,Haibing He,Jingxin Gou,J. Kong,Yu Zhang,Xing Tang

Published 2020 in Expert Opinion on Drug Delivery

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 H2O2 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.

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