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Purpose <p>This study aims to develop and assess an ethosomal-based transdermal delivery system for tofacitinib (TFA) to enhance its therapeutic efficacy in treating rheumatoid arthritis (RA).</p> Methods <p>Ethosomal formulations (ET1–ET13) were developed through the cold sonication method and optimized using Central Composite Design (CCD). CCD was selected to efficiently evaluate linear, quadratic, and interaction effects with reduced experimental runs and predictive response surface models. The evaluation encompassed key formulation parameters such as particle size, entrapment efficiency (%EE), and drug loading (%DL). The optimized formulation (ET14) was integrated into a Carbopol 934 gel to enhance topical applicability and stability.</p> Results <p>ET14 showed a particle size of 257.9&#xa0;nm, %EE of 78.24 ± 1.5%, and %DL of 29.46 ± 0.87%. The ethosomal gel exhibited favorable physicochemical properties: pH of 6.0 ± 0.2, spreadability of 12.09 ± 0.36&#xa0;g·cm/s, and drug content of 89.56 ± 0.42%. Compared with the conventional TFA gel, the ethosomal gel demonstrated a 3.6-fold increase in in vitro drug release and a 2-fold enhancement in ex vivo skin permeation. The in vivo efficacy using a Complete Freund’s Adjuvant-induced RA rat model demonstrated that TFA-ETH gel significantly decreased paw edema, arthritis scores, reducing the arthritic index by ~ 68% (vs. DG), while FT gel showed ~ 35% reduction. The treatment also improved body weight compared to the disease group (<i>P</i> &lt; 0.001).</p> Conclusion <p>Ethosomal encapsulation significantly enhances the dermal bioavailability and therapeutic index of TFA. This delivery platform presents a non-invasive and patient-compliant method for targeted and sustained RA therapy.</p>

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Development and Evaluation of Tofacitinib-Loaded Ethosomal Gel for Transdermal Management of Rheumatoid Arthritis

  • 期刊论文

  • 发表日期：

    2026年2月26日

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  • Pavani Chowdary,
  • Vishnu Pulavarthy,
  • V. V. S. Rajendra Prasad,
  • Jyothi Golagana,
  • V Balchander,
  • Sadhana Noothi

摘要

Purpose

This study aims to develop and assess an ethosomal-based transdermal delivery system for tofacitinib (TFA) to enhance its therapeutic efficacy in treating rheumatoid arthritis (RA).

Methods

Ethosomal formulations (ET1–ET13) were developed through the cold sonication method and optimized using Central Composite Design (CCD). CCD was selected to efficiently evaluate linear, quadratic, and interaction effects with reduced experimental runs and predictive response surface models. The evaluation encompassed key formulation parameters such as particle size, entrapment efficiency (%EE), and drug loading (%DL). The optimized formulation (ET14) was integrated into a Carbopol 934 gel to enhance topical applicability and stability.

Results

ET14 showed a particle size of 257.9 nm, %EE of 78.24 ± 1.5%, and %DL of 29.46 ± 0.87%. The ethosomal gel exhibited favorable physicochemical properties: pH of 6.0 ± 0.2, spreadability of 12.09 ± 0.36 g·cm/s, and drug content of 89.56 ± 0.42%. Compared with the conventional TFA gel, the ethosomal gel demonstrated a 3.6-fold increase in in vitro drug release and a 2-fold enhancement in ex vivo skin permeation. The in vivo efficacy using a Complete Freund’s Adjuvant-induced RA rat model demonstrated that TFA-ETH gel significantly decreased paw edema, arthritis scores, reducing the arthritic index by ~ 68% (vs. DG), while FT gel showed ~ 35% reduction. The treatment also improved body weight compared to the disease group (P < 0.001).

Conclusion

Ethosomal encapsulation significantly enhances the dermal bioavailability and therapeutic index of TFA. This delivery platform presents a non-invasive and patient-compliant method for targeted and sustained RA therapy.