Department of Pharmaceutics, Faculty of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Center for Nanotechnology in Drug Delivery, Shiraz University of Medical Sciences, Shiraz, Iran
Department of Pharmaceutics, Nanotechnology Research Center, Faculty of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran
Curr Drug Deliv. 2020;17(9):787-798. doi: 10.2174/1567201817666200722141807.
Psoriasis is an inflamed skin disorder associated with the activation of phosphorylation signals in keratinocytes, which leads to proliferation. Phosphorylation signal inhibitors, such as silibinin can inhibit cell proliferation. Unlike current psoriasis treatment approaches that are associated with dangerous side effects; natural components can introduce new trends in psoriasis treatment. The major problem in the topical treatment of psoriasis is drug localization through the psoriasis lesions.
In this study, silibinin-loaded polymeric micelles prepared and characterized for drug loading and release and ex vivo permeation through psoriatic and normal mice skin. The optimized batch was used for the treatment of psoriasis lesions in the mice model.
The optimized batch demonstrated mean particle size 18.3 ± 2.1 nm, entrapment efficiency 75.8 ± 5.8%, and prolonged silibinin release. % Silibinin permeated through psoriatic skin after 48 treated by polymeric micelle and aqueous control was 80.35, and 92.6, respectively. Polymeric micelles increased silibinin localization in the psoriatic skin in comparison with control. In psoriatic skin after 7- 10 days treatment by silibinin- loaded polymeric micelle, there was no evidence of psoriasis and the histological evaluation showed no sign of psoriasis. Silibinin-loaded polymeric micelles reduced Psoriasis area index by more than 78% after 14 days.
It seems that polymeric micelles increased the effectiveness of silibinin by drug localization into the psoriatic plaque. Topical STAT- 3inhibitors can be introduced as a new strategy in psoriasis treatment.
银屑病是一种炎症性皮肤疾病,与角质形成细胞中磷酸化信号的激活有关,导致细胞增殖。磷酸化信号抑制剂,如水飞蓟素,可以抑制细胞增殖。与目前与危险副作用相关的银屑病治疗方法不同;天然成分可以为银屑病治疗带来新趋势。银屑病局部治疗的主要问题是通过银屑病病变部位的药物定位。
在这项研究中,制备并表征了负载水飞蓟素的聚合物胶束,用于药物负载和释放以及通过银屑病和正常小鼠皮肤的体外渗透。优化批次用于治疗小鼠模型中的银屑病病变。
优化批次的平均粒径为 18.3±2.1nm,包封效率为 75.8±5.8%,并延长了水飞蓟素的释放。经聚合物胶束和水相对照处理 48 小时后,%水飞蓟素透过银屑病皮肤分别为 80.35 和 92.6。与对照相比,聚合物胶束增加了水飞蓟素在银屑病皮肤中的定位。在银屑病皮肤经水飞蓟素负载聚合物胶束治疗 7-10 天后,没有银屑病的证据,组织学评估显示没有银屑病的迹象。水飞蓟素负载聚合物胶束在 14 天后使银屑病面积指数降低了 78%以上。
似乎聚合物胶束通过将药物定位到银屑病斑块中增加了水飞蓟素的疗效。局部 STAT-3 抑制剂可以作为银屑病治疗的一种新策略。