He Enxue, Li Hailing, Li Xiaokun, Wu Xunxun, Lei Kun, Diao Yong
School of Biomedical Science, Huaqiao University, Quanzhou 362021, China.
School of Medical Technology and Engineering, Henan University of Science and Technology, Luoyang 471023, China.
Int J Mol Sci. 2022 Mar 30;23(7):3798. doi: 10.3390/ijms23073798.
Psoriasis is an immune disease caused by rapid and incomplete differentiation of skin basal cells. Natural products such as indirubin have historically served as excellent sources for the treatments of psoriasis. However, the poor solubility and bioavailability due to its plane and rigid crystal structure, which limits its efficacy. Herein, to improve the efficacy of indirubin, a hydrogel-based microemulsion drug delivery system was developed for transdermal delivery. The mean droplet size of the optimized microemulsion was 84.37 nm, with a polydispersity index (PDI) less than 0.2 and zeta potential value of 0~-20 mV. The transdermal flux and skin retention of indirubin at 24 h were 47.34 ± 3.59 μg/cm and 8.77 ± 1.26 μg/cm, respectively. The optimized microemulsion was dispersed in carbomer 934 hydrogel to increase the consistency. The indirubin-loaded microemulsion gel was tested on an imiquimod-induced psoriasis mouse model. Results showed that this preparation can improve psoriasis symptoms by down-regulating the expression of IL-17A, Ki67, and CD4T. This experiment provides great scalability for researchers to treat psoriasis, avoid first-pass effects, and increase the concentration of targeted drugs.
银屑病是一种由皮肤基底细胞快速且不完全分化引起的免疫疾病。诸如靛玉红等天然产物历来都是治疗银屑病的优质药物来源。然而,由于其平面且刚性的晶体结构导致溶解度和生物利用度较差,这限制了其疗效。在此,为提高靛玉红的疗效,开发了一种基于水凝胶的微乳药物递送系统用于透皮给药。优化后的微乳平均粒径为84.37 nm,多分散指数(PDI)小于0.2,zeta电位值为0~ -20 mV。24小时时靛玉红的透皮通量和皮肤滞留量分别为47.34±3.59 μg/cm和8.77±1.26 μg/cm。将优化后的微乳分散在卡波姆934水凝胶中以增加稠度。对咪喹莫特诱导的银屑病小鼠模型进行了载靛玉红微乳凝胶的测试。结果表明,该制剂可通过下调IL-17A、Ki67和CD4T的表达来改善银屑病症状。该实验为研究人员治疗银屑病提供了很大的可扩展性,避免了首过效应,并提高了靶向药物的浓度。