State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau, China.
Zhuhai Campus of Zunyi Medical University, Department of Pharmaceutical Sciences, China.
Colloids Surf B Biointerfaces. 2019 Oct 1;182:110352. doi: 10.1016/j.colsurfb.2019.110352. Epub 2019 Jul 8.
Psoriasis is a severe disfiguring skin disease affecting approximately 3% of people worldwide and negatively affecting their daily lives. The pathogenesis of psoriasis is complicated, and typical therapeutic strategies for psoriasis mainly focus on anti-inflammation. Considering the side effects, withdrawal rebound, high cost, and many other disadvantages of existing treatments, we developed a new topical therapeutic formulation consisting of niosomes loaded with celastrol, a triterpenoid extracted from Tripterygium. Celastrol niosomes were prepared by the thin film hydration method and probe sonication. The niosomes were composed of Span 20, Span 60, and cholesterol at a weight ratio of 3:1:1. The particle size of the niosomes was approximately 147 nm, with yield of up to 90%. Celastrol niosomes showed improved in vitro permeation ability compared to the raw drug. In our in vivo study, celastrol niosomes effectively alleviated erythema and scaling on the dorsal skin of psoriasis mouse models. Spleen weight and the levels of cytokines, including IL-22, IL-23, and IL-17, decreased after the treatment, indicating the high therapeutic potential of this formulation for psoriasis. In conclusion, encapsulation of celastrol by niosomes increased the water-solubility and permeation of celastrol into the skin, significantly improving its anti-psoriasis activity in mice.
银屑病是一种严重的毁容性皮肤病,影响全球约 3%的人群,并对他们的日常生活产生负面影响。银屑病的发病机制很复杂,典型的银屑病治疗策略主要集中在抗炎上。考虑到现有治疗方法的副作用、停药反弹、成本高和许多其他缺点,我们开发了一种新的局部治疗制剂,该制剂由榄香烯制成,榄香烯是从雷公藤中提取的一种三萜类化合物。采用薄膜水化法和探针超声法制备榄香烯囊泡。囊泡由重量比为 3:1:1 的司盘 20、司盘 60 和胆固醇组成。囊泡的粒径约为 147nm,产率高达 90%。与原料药相比,榄香烯囊泡显示出改善的体外渗透能力。在我们的体内研究中,榄香烯囊泡有效地缓解了银屑病小鼠模型背部皮肤的红斑和鳞屑。治疗后脾脏重量和细胞因子(包括 IL-22、IL-23 和 IL-17)的水平降低,表明该制剂对银屑病具有很高的治疗潜力。总之,通过囊泡包封榄香烯增加了榄香烯的水溶性和向皮肤的渗透,显著提高了其在小鼠中的抗银屑病活性。