Li Jiahao, Wei Yushuang, Lai Qin, Li Xiangyang, Wang Yu, Wang Xun, Chen Yinghua, Liu Hong, Yang Kai, Yuan Bing
Key Laboratory of Theoretical Chemistry of Environment Ministry of Education, School of Environment, South China Normal University, Guangzhou 510006, Guangdong, China.
Songshan Lake Materials Laboratory, Dongguan 523808, Guangdong, China.
Nanoscale. 2025 May 23;17(20):12937-12949. doi: 10.1039/d5nr00691k.
Resveratrol (RSV) is a natural polyphenolic compound known for its anti-oxidant, anti-inflammatory, anticancer, and cardioprotective properties. However, the limited water solubility and poor bioavailability of RSV significantly hinder its application in the food and pharmaceutical industries. To address these challenges, we developed a facile, scalable, and specifically, organic-solvent-free method to prepare highly stable and concentrated RSV nanoformulations. By utilizing an ethoxylated hydrogenated castor oil (EHCO) aqueous solution, we successfully dissolved RSV in water at concentrations of up to 30 mg mL. This RSV solution could be subsequently incorporated with hydrogenated lecithin S10 to formulate stable lipid nanoparticles, sized 140-180 nm. The entire process was performed under heating and stirring, eliminating the need for organic solvents and ensuring simplicity and high reproducibility. The resulting RSV-CO60@S10 nanoformulations exhibited relatively high encapsulation efficiency (with final RSV concentrations of up to 30 mg mL), long-term stability (exceeding 6 months), preserved antioxidant activity, and effective cellular internalization capabilities that could alleviate oxidative stress. Additionally, these nanoparticles exhibited promising therapeutic efficacy toward atopic dermatitis in mice. These findings offer valuable insights into the potential utilization of RSV across diverse applications.
白藜芦醇（RSV）是一种天然多酚化合物，以其抗氧化、抗炎、抗癌和心脏保护特性而闻名。然而，RSV有限的水溶性和较差的生物利用度显著阻碍了其在食品和制药行业的应用。为应对这些挑战，我们开发了一种简便、可扩展且无有机溶剂的方法来制备高度稳定且浓缩的RSV纳米制剂。通过使用乙氧基化氢化蓖麻油（EHCO）水溶液，我们成功地将RSV以高达30mg/mL的浓度溶解于水中。随后，这种RSV溶液可与氢化卵磷脂S10混合，以制备尺寸为140 - 180nm的稳定脂质纳米颗粒。整个过程在加热和搅拌下进行，无需有机溶剂，确保了操作简便且重现性高。所得的RSV-CO60@S10纳米制剂表现出相对较高的包封效率（最终RSV浓度高达30mg/mL）、长期稳定性（超过6个月）、保留的抗氧化活性以及能够减轻氧化应激的有效细胞内化能力。此外，这些纳米颗粒对小鼠特应性皮炎显示出有前景的治疗效果。这些发现为RSV在各种应用中的潜在利用提供了有价值的见解。
