Scholarlink

Objective <p>To develop and optimize tapinarof-loaded proniosome gel for enhanced topical therapy for plaque psoriasis.</p> Methods <p>Tapinarof-loaded proniosomes were prepared via the coacervation phase separation method and optimized via the Box–Behnken design, with the surfactant concentration (Span 60: 900–1800&#xa0;mg), membrane stabilizer content (cholesterol: 200–300&#xa0;mg), and phospholipid amount (soyubicin: 800–900&#xa0;mg) as independent variables. The optimized proniosomal formulation was incorporated into different gel bases (Carbopol 934, HPMC K15M, their combination, and sodium alginate). The physicochemical properties, ex vivo permeation, stability, and in vivo antipsoriatic efficacy of the formulations were characterized in an imiquimod-induced psoriasis model.</p> Results <p>The optimized proniosomal formulation (Span 60: 1350&#xa0;mg, cholesterol: 250&#xa0;mg, soya lecithin: 850&#xa0;mg) exhibited excellent entrapment efficiency (90.93%), drug release (96.98%), and vesicle size (118.56&#xa0;nm) with minimal prediction error (0.066–2.166%). Among the gel formulations, NG3 (Carbopol 934-HPMC K15M combination) demonstrated superior properties, with an optimal pH (6.53), spreadability (15.74&#xa0;g·cm/sec), and drug content (97.92%). Ex vivo studies revealed significantly greater steady-state fluxes (28.37&#xa0;µg/cm²/h) and permeability coefficients (5.67 × 10⁻³ cm/h) for NG3 than for the other formulations. The formulation-maintained stability under accelerated conditions, with a statistically insignificant 5.9% reduction in drug content after 3 months (<i>p</i> &gt; 0.05). Compared with the marketed formulation, NG3 had significantly greater antipsoriatic efficacy in vivo, with lower PASI scores (1.75 vs. 2.86), reduced skin thickness (0.89&#xa0;mm vs. 1.14&#xa0;mm), and decreased inflammatory cytokine levels (TNF-α: 36.25 vs. 54.37 pg/mg).</p> Conclusion <p>The developed proniosomal gel significantly enhances the therapeutic efficacy of tapinarof for plaque psoriasis treatment through improved skin penetration and targeted delivery, offering potential for reduced application frequency and enhanced patient compliance in clinical settings.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Development and Optimization of a Tapinarof Loaded with a Proniosomal Gel to Treat Plaque Psoriasis

  • 期刊论文

  • 发表日期：

    2026年1月24日

查看全文
  • Rahul Godge,
  • Rutuja Gumnar,
  • Kavita Vikhe,
  • Rajashri Ghogare,
  • Someshwar Mankar

摘要

Objective

To develop and optimize tapinarof-loaded proniosome gel for enhanced topical therapy for plaque psoriasis.

Methods

Tapinarof-loaded proniosomes were prepared via the coacervation phase separation method and optimized via the Box–Behnken design, with the surfactant concentration (Span 60: 900–1800 mg), membrane stabilizer content (cholesterol: 200–300 mg), and phospholipid amount (soyubicin: 800–900 mg) as independent variables. The optimized proniosomal formulation was incorporated into different gel bases (Carbopol 934, HPMC K15M, their combination, and sodium alginate). The physicochemical properties, ex vivo permeation, stability, and in vivo antipsoriatic efficacy of the formulations were characterized in an imiquimod-induced psoriasis model.

Results

The optimized proniosomal formulation (Span 60: 1350 mg, cholesterol: 250 mg, soya lecithin: 850 mg) exhibited excellent entrapment efficiency (90.93%), drug release (96.98%), and vesicle size (118.56 nm) with minimal prediction error (0.066–2.166%). Among the gel formulations, NG3 (Carbopol 934-HPMC K15M combination) demonstrated superior properties, with an optimal pH (6.53), spreadability (15.74 g·cm/sec), and drug content (97.92%). Ex vivo studies revealed significantly greater steady-state fluxes (28.37 µg/cm²/h) and permeability coefficients (5.67 × 10⁻³ cm/h) for NG3 than for the other formulations. The formulation-maintained stability under accelerated conditions, with a statistically insignificant 5.9% reduction in drug content after 3 months (p > 0.05). Compared with the marketed formulation, NG3 had significantly greater antipsoriatic efficacy in vivo, with lower PASI scores (1.75 vs. 2.86), reduced skin thickness (0.89 mm vs. 1.14 mm), and decreased inflammatory cytokine levels (TNF-α: 36.25 vs. 54.37 pg/mg).

Conclusion

The developed proniosomal gel significantly enhances the therapeutic efficacy of tapinarof for plaque psoriasis treatment through improved skin penetration and targeted delivery, offering potential for reduced application frequency and enhanced patient compliance in clinical settings.

Graphical Abstract