Atapour-Mashhad Hoda, Tayarani-Najaran Zahra, Golmohammadzadeh Shiva
Nanotechnology Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
Department of Pharmaceutics, Faculty of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Heliyon. 2024 May 22;10(11):e31429. doi: 10.1016/j.heliyon.2024.e31429. eCollection 2024 Jun 15.
We developed novel and optimal Q10-NLC/SLN formulations as antioxidant and anti-tyrosinase agents. The formulations were analyzed for particle size, morphology, entrapment efficiency (EE %), and long-term stability. The drug release and skin penetration were evaluated using dialysis bag diffusion and Sprague Dawley (SD) rats, respectively. Cytotoxicity and protecting effects were assessed by AlamarBlue® assay, ROS level by DCFH-DA, and tyrosinase activity by l-DOPA assay, measuring the absorbance at 470 nm. The selected formulations had optimal surface characterizations, including Z-average size, PDI, and Zeta potential ranging from 125 to 207 nm, 0.09-0.22, and -7 to -24, respectively. They also exhibited physiochemical stability for up to 6 months and EE% above 80 %. The lipids ratio and co-Q10 amount as variable factors significantly affected particle size and zeta potential but were insignificant on PDI. The release diagram showed that Q10-NLC/SLN revealed a fast release during the first 8 h and prolonged release afterward. The skin permeation revealed a higher accumulative uptake of co-Q10 in the skin for Q10-NLC/SLN compared to Q10 emulsions. Both selected Q10-NLC and Q10-SLN could reduce intracellular ROS after exposure to HO. The Q10-NLC was found to be more potent for inhibiting the tyrosinase activity compared to O10-SLN. The results suggest that the new formulations are promising carriers for topical delivery of co-Q10 as an anti-aging and skin-whitening agent.
我们开发了新型且优化的辅酶Q10纳米脂质载体/固体脂质纳米粒配方,作为抗氧化剂和抗酪氨酸酶剂。对这些配方进行了粒径、形态、包封率(EE%)和长期稳定性分析。分别使用透析袋扩散法和斯普拉格-道利(SD)大鼠评估药物释放和皮肤渗透性。通过AlamarBlue® 检测评估细胞毒性和保护作用,通过DCFH-DA检测评估活性氧水平,通过L-多巴检测评估酪氨酸酶活性,并在470nm处测量吸光度。所选配方具有最佳的表面特性,包括Z-平均粒径、多分散指数(PDI)和zeta电位,分别为125至207nm、0.09 - 0.22和 - 7至 - 24。它们还表现出长达6个月的物理化学稳定性,包封率高于80%。脂质比例和辅酶Q10含量作为可变因素,对粒径和zeta电位有显著影响,但对多分散指数无显著影响。释放曲线表明,辅酶Q10纳米脂质载体/固体脂质纳米粒在前8小时显示快速释放,随后为缓释。皮肤渗透实验表明,与辅酶Q10乳剂相比,辅酶Q10纳米脂质载体/固体脂质纳米粒在皮肤中的辅酶Q10累积摄取量更高。所选的辅酶Q10纳米脂质载体和辅酶Q10固体脂质纳米粒在暴露于过氧化氢后均能降低细胞内活性氧水平。发现辅酶Q10纳米脂质载体比辅酶Q10固体脂质纳米粒在抑制酪氨酸酶活性方面更有效。结果表明,这些新配方有望作为辅酶Q10的局部递送载体,用于抗老化和美白皮肤。