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<p>The current research developed a novel transdermal patch of methotrexate (MTX) using a polymeric blend of ethyl cellulose and hydroxypropyl methylcellulose (EC: HPMC, 1:5) to address the major key limitations of existing oral and topical preparations, namely low bioavailability, systemic toxicity, and inadequate skin penetration. In this study, four types of penetration enhancers (Eucalyptus Oil, N-methyl-2-pyrrolidone, Tween 80, and Oleic Acid) are compared at different concentrations in the selected EC: HPMC matrix. Among all the formulations, the patch containing 10% Oleic Acid (F5 OA 10%) demonstrated the most favorable performance. In Ex vivo experiments, the formulation F5 OA 10% disrupted the stratum corneum lipids, resulting in a 13.5&#xa0;°C reduction in lipid melting transition temperature, which meant that oleic acid was 9.8 times more permeable than control formulation F5 (EC: HPMC, 1:5). The formulation (F5 OA 10%) showed a significantly improved pharmacokinetic profile in the in vivo assessment, with a C<sub>max</sub> 183.29 ng/mL and a half-life of 22.19&#xa0;h which was 44% longer than the control formulation (15.37&#xa0;h, <i>p</i> &lt; 0.001). Furthermore, the formulation also achieved a higher cumulative drug exposure (AUC = 3123.68 ng·h/mL) and mean residence time (26.73&#xa0;h), signifying sustained release and enhanced bioavailability. Overall, the optimized formulation (F5 OA 10%) provided a stable, targeted transdermal delivery system that demonstrated significantly enhanced skin permeation, drug retention, and significantly improved pharmacokinetic performance, positioning it as a suitable candidate for psoriasis therapy with the potential for reduced systemic side effects.</p>

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Methotrexate Loaded Polymeric Patches with Penetration Enhancers for Transdermal Delivery: in vitro, Ex Vivo, and in Vivo Characterization

  • 期刊论文

  • 发表日期：

    2026年3月19日

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  • Muhammad Shahid Latif,
  • Asif Nawaz,
  • Muhammad Khurshid Alam Shah,
  • Muhammad Fareed,
  • Muhammad Waseem Khan,
  • Muhammad Luqman Nordin,
  • Omar Awad Alsaidan,
  • Sami I. Alzarea

摘要

The current research developed a novel transdermal patch of methotrexate (MTX) using a polymeric blend of ethyl cellulose and hydroxypropyl methylcellulose (EC: HPMC, 1:5) to address the major key limitations of existing oral and topical preparations, namely low bioavailability, systemic toxicity, and inadequate skin penetration. In this study, four types of penetration enhancers (Eucalyptus Oil, N-methyl-2-pyrrolidone, Tween 80, and Oleic Acid) are compared at different concentrations in the selected EC: HPMC matrix. Among all the formulations, the patch containing 10% Oleic Acid (F5 OA 10%) demonstrated the most favorable performance. In Ex vivo experiments, the formulation F5 OA 10% disrupted the stratum corneum lipids, resulting in a 13.5 °C reduction in lipid melting transition temperature, which meant that oleic acid was 9.8 times more permeable than control formulation F5 (EC: HPMC, 1:5). The formulation (F5 OA 10%) showed a significantly improved pharmacokinetic profile in the in vivo assessment, with a Cmax 183.29 ng/mL and a half-life of 22.19 h which was 44% longer than the control formulation (15.37 h, p < 0.001). Furthermore, the formulation also achieved a higher cumulative drug exposure (AUC = 3123.68 ng·h/mL) and mean residence time (26.73 h), signifying sustained release and enhanced bioavailability. Overall, the optimized formulation (F5 OA 10%) provided a stable, targeted transdermal delivery system that demonstrated significantly enhanced skin permeation, drug retention, and significantly improved pharmacokinetic performance, positioning it as a suitable candidate for psoriasis therapy with the potential for reduced systemic side effects.