细胞外囊泡作为药物递送载体,可提高虾青素的生物活性。

Extracellular Vesicles, as Drug-Delivery Vehicles, Improve the Biological Activities of Astaxanthin.

作者信息

Jang Young Jun, Cha Byung Seok, Kim Doyeon, Lee Eun Sung, Kim Seokjoon, Han Jinjoo, Shin Jiye, Kim Seokhwan, Park Ki Soo

机构信息

Department of Biological Engineering, College of Engineering, Konkuk University, Seoul 05029, Republic of Korea.

出版信息

Antioxidants (Basel). 2023 Feb 13;12(2):473. doi: 10.3390/antiox12020473.

Abstract

Astaxanthin (AST) exhibits potent antioxidant and anti-inflammatory activities but poor stability and biological efficacy, which limit its application in the food and medical industries. In the present study, a new strategy was proposed to enhance the biological activities of AST using fetal bovine serum-derived extracellular vesicles (EVs). Saponin-assisted incubation was used to load AST owing to its high encapsulation efficiency and loading capacity. AST-incorporated EVs (EV-ASTs) maintained their original EV morphology and showed high stability at 4 °C, 25 °C, and 37 °C over a 28-day period, which was attributed to the protective environment provided by the phospholipid bilayer membrane of the EVs. Additionally, the EV-ASTs exhibited excellent antioxidant and anti-inflammatory activities in HaCaT keratinocytes and RAW 264.7 macrophage cells, respectively; these were significantly higher than those of free AST. Furthermore, the mechanism associated with the enhanced biological activities of EV-ASTs was evaluated by analyzing the expression of genes involved in antioxidation and anti-inflammation, in parallel with cellular in vitro assays. These results provide insights into methods for improving the performance of hydrophobic drugs using nature-derived EVs and will contribute to the development of novel drug-delivery systems.

摘要

虾青素(AST)具有强大的抗氧化和抗炎活性,但稳定性和生物学功效较差,这限制了其在食品和医药行业的应用。在本研究中,提出了一种新策略,即利用胎牛血清衍生的细胞外囊泡(EVs)来增强AST的生物学活性。由于皂苷辅助孵育具有高包封效率和载药量,因此被用于负载AST。负载AST的EVs(EV-ASTs)保持了其原始的EV形态,并且在4°C、25°C和37°C下28天内表现出高稳定性,这归因于EVs的磷脂双分子层膜提供的保护环境。此外,EV-ASTs分别在HaCaT角质形成细胞和RAW 264.7巨噬细胞中表现出优异的抗氧化和抗炎活性;这些活性显著高于游离AST。此外,通过分析参与抗氧化和抗炎的基因表达以及细胞体外试验,评估了与EV-ASTs增强生物学活性相关的机制。这些结果为利用天然来源的EVs改善疏水性药物性能的方法提供了见解,并将有助于新型药物递送系统的开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a781/9952194/f47f720bec66/antioxidants-12-00473-sch001.jpg

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