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

https://doi.org/10.1016/j.colsurfb.2019.110352Get rights and content

Highlights

  • 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.

Abstract

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.

Section snippets

Psoriasis

Psoriasis, a chronic non-infectious disease, has been reported worldwide. Because registration of psoriasis cases is not compulsory, there are few studies about the onset of psoriasis and these studies are not very reliable [1]. It is roughly estimated that 3% of people worldwide have psoriasis [2,3]. Psoriasis could be divided into five types according to its pathological manifestation, and the most common type being plaque psoriasis, which causes pain and itching in affected patients. In

Materials

Cel were obtained from Chengdu Pufei De Biotech Co., Ltd. (Chengdu, China). Span 20, Span 60, and cholesterol were all purchased from Aladdin Industrial Corporation (Shanghai, China). Carbopol 974 powder was obtained from Chineway (Shanghai, China). Imiquimod cream (IMQ; 5%) as Aldara and tacrolimus ointment (0.1%) as Protopic were purchased from Kangaiduo Drug Store (Guangzhou, China). Paraformaldehyde (4%) was purchased from Phygene (Fuzhou, China). High-performance liquid chromatography

Characterization of Cel Nio

After preliminary screening of the formulation (data not shown), a Span 20, Span 60, and cholesterol ratio of 3:1:1 (w/w/w), hydration time of 30 min, and sonication time of 2 min were selected. This optimized formulation had a smaller particle size and higher drug loading ability. Therefore, this formulation was selected to be used in the subsequent experiment. A graph of size distribution is shown in Fig. 1(A). The particle size of Cel Nio was approximately 147.4 nm ± 5.6 nm with a PDI of

Conclusion

In this study, Nio hydrogels loaded with Cel were developed as an effective treatment of psoriasis-like mouse model induced by IMQ. Cel Nio had an average particle size of approximately147 nm with small PDI. Encapsulation of Cel into Nio increased the water-solubility and permeation of Cel in the skin, significantly improving its anti-psoriasis activity in the mice model. Thus, the results indicated the potential application of Cel Nio hydrogel in psoriasis therapy.

Acknowledgement

This study was financially supported by the Macao Science and Technology Development Fund (0013/2018/A1).

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