State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
Translational Chinese Medicine Key Laboratory of Sichuan Province, Sichuan Academy of Chinese Medicine Sciences, Chengdu, China.
Int J Biol Macromol. 2023 Dec 1;252:126480. doi: 10.1016/j.ijbiomac.2023.126480. Epub 2023 Aug 25.
LED-related blue-light-induced damage can cause eye diseases. However, drug delivery in patients with ocular diseases is faced with various challenges. In this study, we developed flexible liposomes based on trimethylated chitosan (TMC-Lipo) to deliver resveratrol for the treatment of retinal diseases. Flexible liposomes can easily cross various biological barriers. Chitosan and its derivatives have adhesive properties and are widely used in mucoadhesive drug delivery systems. Therefore, we wrapped flexible liposomes with trimethylated chitosan via electrostatic adsorption. The charge of the flexible liposomes became positive after encapsulation in TMC, and they remained stable in artificial tears. We assessed the safety of TMC-Lipo in cellular and zebrafish experiments and found that it can be safely used. In addition, treatment with TMC-Lipo significantly reduced HO-induced damage to ARPE-19 cells, restored mitochondrial membrane potential, and protected the cells. TMC-Lipo more easily reached the posterior ocular segment of the mice than liposome nanoparticles and attenuated blue-light-induced retinal cytopathy. Our study demonstrates that effective eye drop formulations can be developed based on trimethylated chitosan, which provides a promising approach for the treatment of ocular diseases.
LED 相关的蓝光诱导损伤可导致眼部疾病。然而，眼部疾病患者的药物输送面临着各种挑战。在这项研究中，我们开发了基于三甲基壳聚糖（TMC-Lipo）的柔性脂质体来输送白藜芦醇，以治疗视网膜疾病。柔性脂质体可以轻松穿越各种生物屏障。壳聚糖及其衍生物具有粘性，广泛应用于粘膜粘附药物传递系统。因此，我们通过静电吸附将柔性脂质体包裹在三甲基壳聚糖中。TMC 包封后，柔性脂质体带正电荷，在人工泪液中保持稳定。我们在细胞和斑马鱼实验中评估了 TMC-Lipo 的安全性，发现它可以安全使用。此外，TMC-Lipo 处理可显著减轻 HO 诱导的 ARPE-19 细胞损伤，恢复线粒体膜电位并保护细胞。与脂质体纳米颗粒相比，TMC-Lipo 更容易到达小鼠的后眼部段，并减轻蓝光诱导的视网膜细胞病变。我们的研究表明，可以基于三甲基壳聚糖开发有效的滴眼剂配方，为眼部疾病的治疗提供了一种有前途的方法。
