Loading of water-insoluble celastrol into niosome hydrogels for improved topical permeation and anti-psoriasis activity

[Display omitted] •Celastrol niosomes were successfully prepared by the thin film hydration method.•Encapsulation of celastrol into noisome increased the water-solubility and permeation of Celastrol in the skin.•Celastrol niosome hydrogel showed good anti-psoriasis activity in the imiquimod-induced...

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Veröffentlicht in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2019-10, Vol.182, p.110352-110352, Article 110352
Hauptverfasser: Meng, Shikang, Sun, Lin, Wang, Lun, Lin, Zibei, Liu, Zeyu, Xi, Long, Wang, Zhenping, Zheng, Ying
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Sprache:eng
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Zusammenfassung:[Display omitted] •Celastrol niosomes were successfully prepared by the thin film hydration method.•Encapsulation of celastrol into noisome increased the water-solubility and permeation of Celastrol in the skin.•Celastrol niosome hydrogel showed good anti-psoriasis activity in the imiquimod-induced psoriasis-like mouse model. 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.
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2019.110352