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Purpose <p>Oxyresveratrol, a polyphenolic compound, is a major constituent of several medicinal plants, particularly <i>Artocarpus lakoocha</i>. It has demonstrated various systemic and topical pharmacological activities, including anti-HIV, anti-herpes simplex virus, and anti-tyrosinase effects. However, its low oral bioavailability limits therapeutic application, making transdermal drug delivery a promising alternative. This study aimed to investigate the skin permeation behavior of oxyresveratrol and evaluate the impact of permeation enhancers on its transdermal delivery and skin retention using full-thickness porcine ear skin in a side-by-side diffusion cell system.</p> Methods <p>Binary solvent systems with different ratios of ethanol/phosphate-buffered saline pH 7.4 (PBS) and propylene glycol/PBS were assessed. Subsequently, the effects of polysorbate 20, diethylene glycol monoethyl ether (DEGEE), and N-methyl-2-pyrrolidone (NMP) in the optimized binary solvent system were examined.</p> Results <p>The results indicated that a 3:7 ethanol/PBS ratio provided the highest solubility, permeation coefficient, flux, and skin accumulation. The incorporation of 10% DEGEE into this system significantly enhanced oxyresveratrol permeation, while NMP at 3–5% notably increased skin retention.</p> Conclusion <p>These findings provide valuable insights into the transdermal permeation profile of oxyresveratrol and the role of permeation enhancers, supporting its potential development in transdermal and topical pharmaceutical formulations.</p>

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Enhancing Transdermal Delivery of Oxyresveratrol: Skin Permeation and Retention Using Permeation Enhancers in a Porcine Skin Model

  • 期刊论文

  • 发表日期：

    2025年10月17日

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  • Bunleu Sungthong,
  • Sarunya Tuntiyasawasdikul,
  • Warut Panyatee,
  • Benyapa Sakdanupong,
  • Wanida Caichompoo,
  • Catheleeya Mekjaruskul

摘要

Purpose

Oxyresveratrol, a polyphenolic compound, is a major constituent of several medicinal plants, particularly Artocarpus lakoocha. It has demonstrated various systemic and topical pharmacological activities, including anti-HIV, anti-herpes simplex virus, and anti-tyrosinase effects. However, its low oral bioavailability limits therapeutic application, making transdermal drug delivery a promising alternative. This study aimed to investigate the skin permeation behavior of oxyresveratrol and evaluate the impact of permeation enhancers on its transdermal delivery and skin retention using full-thickness porcine ear skin in a side-by-side diffusion cell system.

Methods

Binary solvent systems with different ratios of ethanol/phosphate-buffered saline pH 7.4 (PBS) and propylene glycol/PBS were assessed. Subsequently, the effects of polysorbate 20, diethylene glycol monoethyl ether (DEGEE), and N-methyl-2-pyrrolidone (NMP) in the optimized binary solvent system were examined.

Results

The results indicated that a 3:7 ethanol/PBS ratio provided the highest solubility, permeation coefficient, flux, and skin accumulation. The incorporation of 10% DEGEE into this system significantly enhanced oxyresveratrol permeation, while NMP at 3–5% notably increased skin retention.

Conclusion

These findings provide valuable insights into the transdermal permeation profile of oxyresveratrol and the role of permeation enhancers, supporting its potential development in transdermal and topical pharmaceutical formulations.