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<p>Gout is a prevalent inflammatory arthritic disorder affecting more than 40 million people worldwide, with incidence increasing due to aging populations, lifestyle factors, and metabolic comorbidities. Febuxostat (FEB), a xanthine oxidase inhibitor used for urate-lowering therapy, often triggers acute gout flares during treatment initiation, necessitating concurrent anti-inflammatory therapy such as aceclofenac (ACE). However, the oral administration of both drugs is associated with poor aqueous solubility, first-pass metabolism, and gastrointestinal adverse effects. The present study aimed to develop and optimize a ufasome-based transdermal gel co-loaded with FEB and ACE to provide controlled and sustained drug release for improved gout management. Ufasomes were prepared using the thin-film hydration method and optimized through a Box–Behnken design. The optimized formulation exhibited nanosized vesicles (199&#xa0;nm for FEB and 365&#xa0;nm for ACE), high entrapment efficiency (&gt; 80%), and stable zeta potential values. The ufasomal gel demonstrated sustained in vitro drug release over 24&#xa0;h compared with plain drug gel, while ex vivo permeation studies indicated controlled diffusion across rat skin, suggesting formation of a drug reservoir within cutaneous layers. The drug release follows 1st order model for FEB and ACE. In vivo pharmacodynamic studies showed significant reductions in serum uric acid levels (<i>p</i> &lt; 0.01) and paw edema volume (<i>p</i> &lt; 0.001). These findings suggest that the FEB–ACE ufasomal transdermal gel offers a sustained delivery platform that may improve therapeutic outcomes and patient compliance in gout therapy. The novelty of this work lies in the dual-drug ufasomal transdermal system integrating urate-lowering and anti-inflammatory therapy in a single formulation, offering a potential alternative to conventional oral treatment for gout management with improved therapeutic convenience.</p>

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Ufasome-based transdermal dual-vesicular gel of febuxostat and aceclofenac for sustained gout therapy: formulation optimization and pharmacodynamic evaluation

  • 期刊论文

  • 发表日期：

    2026年5月2日

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  • Khyati Parekh,
  • Vaishali Thakkar,
  • Devesh Kapoor,
  • Chetan Sojitra,
  • Ankita Desai,
  • Tejal Gandhi

摘要

Gout is a prevalent inflammatory arthritic disorder affecting more than 40 million people worldwide, with incidence increasing due to aging populations, lifestyle factors, and metabolic comorbidities. Febuxostat (FEB), a xanthine oxidase inhibitor used for urate-lowering therapy, often triggers acute gout flares during treatment initiation, necessitating concurrent anti-inflammatory therapy such as aceclofenac (ACE). However, the oral administration of both drugs is associated with poor aqueous solubility, first-pass metabolism, and gastrointestinal adverse effects. The present study aimed to develop and optimize a ufasome-based transdermal gel co-loaded with FEB and ACE to provide controlled and sustained drug release for improved gout management. Ufasomes were prepared using the thin-film hydration method and optimized through a Box–Behnken design. The optimized formulation exhibited nanosized vesicles (199 nm for FEB and 365 nm for ACE), high entrapment efficiency (> 80%), and stable zeta potential values. The ufasomal gel demonstrated sustained in vitro drug release over 24 h compared with plain drug gel, while ex vivo permeation studies indicated controlled diffusion across rat skin, suggesting formation of a drug reservoir within cutaneous layers. The drug release follows 1st order model for FEB and ACE. In vivo pharmacodynamic studies showed significant reductions in serum uric acid levels (p < 0.01) and paw edema volume (p < 0.001). These findings suggest that the FEB–ACE ufasomal transdermal gel offers a sustained delivery platform that may improve therapeutic outcomes and patient compliance in gout therapy. The novelty of this work lies in the dual-drug ufasomal transdermal system integrating urate-lowering and anti-inflammatory therapy in a single formulation, offering a potential alternative to conventional oral treatment for gout management with improved therapeutic convenience.