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<p>Leflunomide (LEF) is a disease-modifying anti-rheumatic drug (DMARD) widely used in the management of rheumatoid arthritis (RA), but its oral administration is associated with systemic adverse effects and variable bioavailability. Topical delivery of the drug via nanocarrier systems provides potential opportunities to enhance local drug concentration in inflamed joints while reducing systemic exposure. This study aimed to develop oil-in-water nanoemulsions (NEs) of leflunomide (LEF) to enhance its topical permeation. Preliminary screening studies were conducted wherein Capmul MCM EP/NF, Tween 20, and Transcutol P were selected as oil, surfactant, and co-surfactant. A 3:1 S<sub>mix</sub> ratio showed the largest NE region. LEF-NEs were prepared by the spontaneous emulsification method and optimized using an I-optimal mixture design, wherein the optimized LEF-NEs achieved a size of 88.4 ± 12.6&#xa0;nm, a PDI &lt; 0.3, 92.1 ± 1.9% Solubilisation efficiency, and 99 ± 0.25% transmittance. Stability tests showed no phase separation, globule size changes, or coalescence. Carbopol ETD 2020 converted LEF-NEs into gels, which exhibited a pH of 5.8 ± 0.2, 92.4 ± 3.2% drug content, and a viscosity of 345 ± 4.2 cps. Approximately 70.3 ± 2.1% drug release and 51 ± 1.47% skin permeation with a steady flux of 40&#xa0;µg/cm<sup>2</sup>/min were achieved over 48&#xa0;h. Overall, the results support the potential of LEF-NE gels for localized treatment of RA, showing improved solubility, stability, and skin permeation, thereby reducing the systemic side effects associated with oral therapy.</p>

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Topical Nanoemulsion of Leflunomide for Rheumatoid Arthritis: Formulation, Optimization and Ex Vivo Assessment

  • 期刊论文

  • 发表日期：

    2026年4月16日

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  • Amruta Parmar,
  • S. Brijesh

摘要

Leflunomide (LEF) is a disease-modifying anti-rheumatic drug (DMARD) widely used in the management of rheumatoid arthritis (RA), but its oral administration is associated with systemic adverse effects and variable bioavailability. Topical delivery of the drug via nanocarrier systems provides potential opportunities to enhance local drug concentration in inflamed joints while reducing systemic exposure. This study aimed to develop oil-in-water nanoemulsions (NEs) of leflunomide (LEF) to enhance its topical permeation. Preliminary screening studies were conducted wherein Capmul MCM EP/NF, Tween 20, and Transcutol P were selected as oil, surfactant, and co-surfactant. A 3:1 Smix ratio showed the largest NE region. LEF-NEs were prepared by the spontaneous emulsification method and optimized using an I-optimal mixture design, wherein the optimized LEF-NEs achieved a size of 88.4 ± 12.6 nm, a PDI < 0.3, 92.1 ± 1.9% Solubilisation efficiency, and 99 ± 0.25% transmittance. Stability tests showed no phase separation, globule size changes, or coalescence. Carbopol ETD 2020 converted LEF-NEs into gels, which exhibited a pH of 5.8 ± 0.2, 92.4 ± 3.2% drug content, and a viscosity of 345 ± 4.2 cps. Approximately 70.3 ± 2.1% drug release and 51 ± 1.47% skin permeation with a steady flux of 40 µg/cm2/min were achieved over 48 h. Overall, the results support the potential of LEF-NE gels for localized treatment of RA, showing improved solubility, stability, and skin permeation, thereby reducing the systemic side effects associated with oral therapy.