Yang HeeSeon, Yu Sohyeon, Kim Jisu, Baek KumJu, Lee Young-Ran, Lee Hye Sun, Choi Won Il, Sung Daekyung
Center for Bio-Healthcare Materials, Bio-Convergence Materials R&D Division, Korea Institute of Ceramic Engineering and Technology, 202 Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, Korea.
Department of Chemical Engineering, Hanyang University, 222 Wangsimni-ro, Seongdong-gu, Seoul 04763, Korea.
Pharmaceutics. 2022 Feb 26;14(3):521. doi: 10.3390/pharmaceutics14030521.
The excessive production of reactive oxygen species (ROS) causes harmful effects, including biomolecular damage and inflammation. ROS due to ultraviolet rays, blue light, and fine dust harm the skin, causing urban-related aging. Therefore, a strong antioxidant that relieves oxidative stress in the skin and removes ROS is required. Idebenone (IB) is a powerful antioxidant but is poorly soluble and thus has low solubility in water, resulting in low bioavailability. In this study, IB-loaded nanoparticles (IB@NPs) were synthesized by loading IB without an organic solvent into nanoparticles that can provide high loading efficiency and stability for solubilization. Indeed, the synthesized IB@NPs exhibited long-term stability through dynamic light scattering, methylene blue staining, and redispersion assays, and IB@NPs prepared with a 5 wt% IB loading content were found to be optimal. The antioxidant activity of IB@NPs evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay was significantly higher than that of unloaded IB. In addition, IB@NPs showed excellent biocompatibility, inhibited oxidative damage to mouse NIH-3T3 fibroblasts, and reduced intracellular ROS generation according to an in vitro DPPH antioxidant assay. Most notably, IB@NPs significantly promoted wound healing in vitro, as demonstrated by scratch assays. Therefore, as carriers with excellent stability, IB@NPs have potential cosmetic and pharmaceutical applications.
活性氧（ROS）的过量产生会造成有害影响，包括生物分子损伤和炎症。紫外线、蓝光和细粉尘产生的ROS会损害皮肤，导致与城市环境相关的皮肤老化。因此，需要一种强大的抗氧化剂来缓解皮肤中的氧化应激并清除ROS。艾地苯醌（IB）是一种强大的抗氧化剂，但溶解性差，在水中的溶解度低，导致生物利用度低。在本研究中，通过将不含有机溶剂的IB负载到能够为增溶提供高负载效率和稳定性的纳米颗粒中，合成了负载IB的纳米颗粒（IB@NPs）。事实上，通过动态光散射、亚甲基蓝染色和再分散试验，合成的IB@NPs表现出长期稳定性，并且发现负载量为5 wt%的IB@NPs是最优的。使用2,2-二苯基-1-苦基肼（DPPH）测定法评估的IB@NPs的抗氧化活性显著高于未负载的IB。此外，根据体外DPPH抗氧化试验，IB@NPs表现出优异的生物相容性，抑制了对小鼠NIH-3T3成纤维细胞的氧化损伤，并减少了细胞内ROS的产生。最值得注意的是，划痕试验表明，IB@NPs在体外显著促进了伤口愈合。因此，作为具有优异稳定性的载体，IB@NPs具有潜在的化妆品和药物应用价值。
