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<p>Methotrexate is widely used in the management of rheumatoid arthritis; however, its clinical utility is limited by poor oral bioavailability, gastrointestinal toxicity, and frequent dosing requirements. The present study aimed to develop and optimize a dissolving transdermal microneedle patch of methotrexate to achieve sustained drug delivery and improved therapeutic performance. Methotrexate-loaded microneedles were fabricated using a blend of polyvinyl alcohol and poly (lactic-co-glycolic acid) employing a micromolding technique. Preformulation studies confirmed drug purity and compatibility with excipients. A Quality by Design approach using central composite design was applied to optimize polymer concentrations, with in-vitro dissolution time and moisture uptake as critical quality attributes. The optimized formulation demonstrated adequate mechanical strength (axial fracture force ≈ 0.52&#xa0;N), uniform needle geometry, controlled moisture uptake (&lt; 10%), and sustained dissolution over approximately 7 days. In-vitro and ex-vivo studies revealed significantly enhanced drug release, permeation, and skin deposition compared to conventional transdermal patches. In vivo pharmacokinetic evaluation showed a 3.02-fold increase in relative bioavailability over oral administration, with prolonged mean residence time. Overall, the developed methotrexate-loaded microneedle patch represents a promising, patient-friendly transdermal system capable of improving bioavailability, reducing dosing frequency, and minimizing systemic side effects in rheumatoid arthritis therapy.</p>

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Design, Optimization, and Evaluation of Methotrexate-Loaded Transdermal Microneedles for Targeted Rheumatoid Arthritis Therapy

  • 期刊论文

  • 发表日期：

    2026年5月28日

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  • Priya Patel,
  • Dhwani Bhatt,
  • Bijal Prajapati,
  • Bhupendra G Prajapati,
  • Devesh U Kapoor

摘要

Methotrexate is widely used in the management of rheumatoid arthritis; however, its clinical utility is limited by poor oral bioavailability, gastrointestinal toxicity, and frequent dosing requirements. The present study aimed to develop and optimize a dissolving transdermal microneedle patch of methotrexate to achieve sustained drug delivery and improved therapeutic performance. Methotrexate-loaded microneedles were fabricated using a blend of polyvinyl alcohol and poly (lactic-co-glycolic acid) employing a micromolding technique. Preformulation studies confirmed drug purity and compatibility with excipients. A Quality by Design approach using central composite design was applied to optimize polymer concentrations, with in-vitro dissolution time and moisture uptake as critical quality attributes. The optimized formulation demonstrated adequate mechanical strength (axial fracture force ≈ 0.52 N), uniform needle geometry, controlled moisture uptake (< 10%), and sustained dissolution over approximately 7 days. In-vitro and ex-vivo studies revealed significantly enhanced drug release, permeation, and skin deposition compared to conventional transdermal patches. In vivo pharmacokinetic evaluation showed a 3.02-fold increase in relative bioavailability over oral administration, with prolonged mean residence time. Overall, the developed methotrexate-loaded microneedle patch represents a promising, patient-friendly transdermal system capable of improving bioavailability, reducing dosing frequency, and minimizing systemic side effects in rheumatoid arthritis therapy.