Background <p>Psoriasis is a chronic, inflammatory skin disorder that requires long-term care. Fumaric acid, while useful, is restricted by systemic side effects when taken orally. The purpose of the present research was to develop and optimize a fumaric acid-loaded ethosomes formulation (FA) for better topical use and therapeutic efficacy in psoriasis.</p> Methods <p>The ethosomes formulation was optimized using Box-Behnken Design (BBD), Response Surface Methodology (RSM) software based on vesicle size, polydispersity index (PdI), and entrapment efficiency (EE). The improved ethosomes formulation was characterized using dynamic light scattering and transmission electron microscopy (TEM). Confocal laser scanning microscopy (CLSM), skin penetration studies, in-vitro permeation study, texture analysis, and in vivo evaluation in a psoriasis plaque like psoriasis mice model were conducted to assess performance.</p> Results <p>The optimized formulation had a vesicle size of 153.93 ± 0.05&#xa0;nm, PdI of 0.362 ± 0.001, and EE of 73.26 ± 0.05%. TEM showed spherical vesicles with a uniform shape. CLSM and skin permeation studies demonstrated enhanced penetration (up to 84.9&#xa0;μm) compared to the control (59.9&#xa0;μm). The ethosomes gel exhibited sustained drug release over 24&#xa0;h and favourable texture properties for topical application. In vivo results indicated significant anti-inflammatory, antioxidant, and anti-psoriatic activities. Skin irritation studies confirmed its safety for topical Application.</p> Conclusion <p>Fumaric acid-loaded ethosomes gel is a potential topical therapy for psoriasis, focusing on local action by delivering high drug concentrations directly to the affected area while minimizing systemic absorption. This targeted approach reduces the risk of systemic side effects, making it well-suited for the treatment of inflammatory skin conditions.</p>

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Application of Box-Behnken Design for the Optimization of Fumaric Acid Loaded Nano-Ethosomes for the Management of Psoriasis in Mice

  • Hina Kausar,
  • Mohd. Mujeeb,
  • Abdul Ahad,
  • Mohd. Aqil,
  • Ozair Alam

摘要

Background

Psoriasis is a chronic, inflammatory skin disorder that requires long-term care. Fumaric acid, while useful, is restricted by systemic side effects when taken orally. The purpose of the present research was to develop and optimize a fumaric acid-loaded ethosomes formulation (FA) for better topical use and therapeutic efficacy in psoriasis.

Methods

The ethosomes formulation was optimized using Box-Behnken Design (BBD), Response Surface Methodology (RSM) software based on vesicle size, polydispersity index (PdI), and entrapment efficiency (EE). The improved ethosomes formulation was characterized using dynamic light scattering and transmission electron microscopy (TEM). Confocal laser scanning microscopy (CLSM), skin penetration studies, in-vitro permeation study, texture analysis, and in vivo evaluation in a psoriasis plaque like psoriasis mice model were conducted to assess performance.

Results

The optimized formulation had a vesicle size of 153.93 ± 0.05 nm, PdI of 0.362 ± 0.001, and EE of 73.26 ± 0.05%. TEM showed spherical vesicles with a uniform shape. CLSM and skin permeation studies demonstrated enhanced penetration (up to 84.9 μm) compared to the control (59.9 μm). The ethosomes gel exhibited sustained drug release over 24 h and favourable texture properties for topical application. In vivo results indicated significant anti-inflammatory, antioxidant, and anti-psoriatic activities. Skin irritation studies confirmed its safety for topical Application.

Conclusion

Fumaric acid-loaded ethosomes gel is a potential topical therapy for psoriasis, focusing on local action by delivering high drug concentrations directly to the affected area while minimizing systemic absorption. This targeted approach reduces the risk of systemic side effects, making it well-suited for the treatment of inflammatory skin conditions.