Department of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi'an, 710032, China.
Key Laboratory of Gastrointestinal Pharmacology of Chinese Materia Medica of the State Administration of Traditional Chinese Medicine, Fourth Military Medical University, Xi'an, 710032, China.
Colloids Surf B Biointerfaces. 2021 Aug;204:111786. doi: 10.1016/j.colsurfb.2021.111786. Epub 2021 Apr 27.
Exposure to ultraviolet (UV) irradiation leads to the generation of reactive oxygen species (ROS) and DNA damage in skin tissue, which can further result in skin cancers. Using sunscreens is one of the most popular and the most effective method to resist UV irradiation. Resveratrol (RES) shows high absorbance in UV region and significant anti-oxidant effects. However, RES is easily degraded by UV irradiation, resulting in the decrease of bioactivity and the limitation of its application in the pharmaceutical preparations of skin. In this paper, a nanostructured lipid carrier gel loaded with RES (RES-NLC-gel) was prepared to improve the stability of RES and the accumulation of RES in the epidermis. Moreover, RES-NLC-gel could scavenge free radical effectively and protect human keratinocyte from UV irradiation by inhibiting the generation of ROS, decreasing the protein expression of cleaved caspase-3 and Bax and increasing the protein expression of Bcl-2. When mice skin was pretreated with RES-NLC-gel, there were less erythema, wrinkles and scabs on mice skin. The epidermal thickness of mice skins obviously reduced in dose-dependent manner. The activities of catalase (CAT), glutathione peroxidase (GPx) and superoxide dismutase (SOD) in mice skin tissue significantly increased. Thus, RES-NLC-gel exhibited an obvious anti-UV irradiation and anti-oxidant activity in vivo. RES-NLC-gel displayed great application potential in protecting skin from UV irradiation.
暴露于紫外（UV）辐射会导致皮肤组织中活性氧（ROS）和 DNA 损伤，进而导致皮肤癌。使用防晒霜是抵抗 UV 辐射的最流行和最有效的方法之一。白藜芦醇（RES）在 UV 区域具有高吸收率和显著的抗氧化作用。然而，RES 很容易被 UV 辐射降解，导致生物活性降低，限制了其在皮肤药物制剂中的应用。本文制备了负载 RES 的纳米结构化脂质载体凝胶（RES-NLC-gel），以提高 RES 的稳定性和 RES 在表皮中的积累。此外，RES-NLC-gel 可以通过抑制 ROS 的产生、降低 cleaved caspase-3 和 Bax 的蛋白表达以及增加 Bcl-2 的蛋白表达来有效清除自由基并保护人角质形成细胞免受 UV 照射。当用 RES-NLC-gel 预处理小鼠皮肤时，小鼠皮肤上的红斑、皱纹和结痂较少。小鼠皮肤表皮厚度呈剂量依赖性明显减少。小鼠皮肤组织中过氧化氢酶（CAT）、谷胱甘肽过氧化物酶（GPx）和超氧化物歧化酶（SOD）的活性显著增加。因此，RES-NLC-gel 在体内表现出明显的抗 UV 辐射和抗氧化活性。RES-NLC-gel 在保护皮肤免受 UV 辐射方面显示出巨大的应用潜力。
