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<p>This study aimed to create innovative transfersomes (TRFs) consisting of a lipid blend and a chemical permeation enhancer for efficient transdermal delivery of leflunomide (LFN). Leflunomide, a dihydroorotate dehydrogenase inhibitor, is mainly used to manage rheumatoid arthritis (RA). Oral consumption of LFN for RA can lead to adverse systemic effects; hence, local application is advisable. To develop topical dosage form of LFN, transfersomes with improved skin permeation capabilities were fabricated. The vesicle diameter of LFN-TRF was determined to be 181.2 ± 2.17&#xa0;nm, zeta potential of − 29.2 ± 0.06&#xa0;mV, PDI of 0.259 ± 0.006, and encapsulation percentage (EE) of 86.5 ± 3.45%. Notably, the developed formulation exhibited slow and sustained release of up to 78.87% of LFN over 24&#xa0;h. The drug permeation from the nanocarriers was found to be around 67% for the LFN-TRF-gel and 55.33% for the LFN-gel. Skin irritation assessments indicated no signs of irritation, inflammation, or toxicity, affirming the formulation’s nontoxic and biocompatible characteristics. In vivo studies demonstrated higher anti-inflammatory and anti-arthritic activity than conventional gel. In summary, this study presents a viable alternative for formulating effective topical LFN preparation using transfersomes.</p> Graphical Abstract <p></p>

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QbD-enabled leflunomide-transfersomal gel for topical treatment of rheumatoid arthritis

  • 期刊论文

  • 发表日期：

    2026年5月1日

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  • Kailas Moravkar,
  • Rutuja Thakare,
  • Vivek Kumawat,
  • Sandip Sapkal,
  • Shailesh Chalikwar,
  • Pradip Nirbhavane

摘要

This study aimed to create innovative transfersomes (TRFs) consisting of a lipid blend and a chemical permeation enhancer for efficient transdermal delivery of leflunomide (LFN). Leflunomide, a dihydroorotate dehydrogenase inhibitor, is mainly used to manage rheumatoid arthritis (RA). Oral consumption of LFN for RA can lead to adverse systemic effects; hence, local application is advisable. To develop topical dosage form of LFN, transfersomes with improved skin permeation capabilities were fabricated. The vesicle diameter of LFN-TRF was determined to be 181.2 ± 2.17 nm, zeta potential of − 29.2 ± 0.06 mV, PDI of 0.259 ± 0.006, and encapsulation percentage (EE) of 86.5 ± 3.45%. Notably, the developed formulation exhibited slow and sustained release of up to 78.87% of LFN over 24 h. The drug permeation from the nanocarriers was found to be around 67% for the LFN-TRF-gel and 55.33% for the LFN-gel. Skin irritation assessments indicated no signs of irritation, inflammation, or toxicity, affirming the formulation’s nontoxic and biocompatible characteristics. In vivo studies demonstrated higher anti-inflammatory and anti-arthritic activity than conventional gel. In summary, this study presents a viable alternative for formulating effective topical LFN preparation using transfersomes.

Graphical Abstract