CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, Institute of High Energy Physics, Chinese Academy of Sciences, Beijing, 100049, China.
Center of Materials Science and Optoelectronics Engineering, College of Materials Science and Optoelectronic Technology, University of Chinese Academy of Sciences, Beijing, 100049, China.
Small. 2021 Sep;17(37):e2102035. doi: 10.1002/smll.202102035. Epub 2021 Aug 1.
Radiation dermatitis is a common but torturous side effect during radiotherapy, which greatly decreases the life quality of patients and potentially results in detrimental cessation of tumor treatment. Fullerenol, known as "free radical sponge," is a great choice for skin radioprotection because of its broad-spectrum free radical scavenging performance, good chemical stability, and biosafety. In this work, a facile scalable and eco-friendly synthetic method of fullerenols by catalyst assistant mechanical chemistry strategy is provided. As no organic solvent or high concentration of acid and alkali is introduced to this synthetic system, large-scale (>20 g) production of fullerenols with high yield (>95%) is obtained and no complicated purification is required. Then, the skin radioprotective performance of fullerenols is systematically explored for the first time. In vitro results indicate that fullerenols significantly block the reactive oxygen species-induced damage and enhance the viability of irradiated human keratinocyte cells. In vivo experiments suggest that medical sodium hyaluronate hydrogels loaded with fullerenols are suitable for skin administration and powerfully mitigate radiodermatitis via effectively protecting epidermal stem cells. The work not only provides an efficient gram-scale and eco-friendly synthetic method of fullerenols, but also promotes the development of fullerenols as potential skin radioprotectors.
放射性皮炎是放疗中常见但痛苦的副作用，极大地降低了患者的生活质量，并可能导致肿瘤治疗的有害中断。富勒醇，被称为“自由基海绵”，由于其广谱的自由基清除性能、良好的化学稳定性和生物安全性，是皮肤放射防护的理想选择。在这项工作中，提供了一种通过催化剂辅助机械化学策略制备富勒醇的简便、可扩展和环保的合成方法。由于该合成体系中没有引入有机溶剂或高浓度的酸碱，因此可以获得高产率（>95%）和无需复杂纯化的大规模（>20g）富勒醇生产。然后，首次系统地探索了富勒醇的皮肤放射防护性能。体外结果表明，富勒醇可显著阻止活性氧诱导的损伤，并提高照射后人角质形成细胞的活力。体内实验表明，负载富勒醇的医用透明质酸钠水凝胶适合皮肤给药，并通过有效保护表皮干细胞，有力地减轻放射性皮炎。这项工作不仅提供了一种高效的克级和环保的富勒醇合成方法，还促进了富勒醇作为潜在皮肤放射防护剂的发展。
