Scholarlink

<p>Efficient transdermal delivery of hydrophobic small-molecule drugs remains a persistent challenge in dermatological therapeutics due to the limited solubility of active materials, stability of formulation, and the physical barrier posed by the stratum corneum. Here, we report a one-step emulsification strategy that enables the formation of water-in-oil-in-water (W/O/W) double emulsions and water-in-oil (W/O) single emulsions using silica nanoparticles as the sole stabilizer. A hydrophobic usnic acid derivative active material, usnic acid-cinnamic acid (UA-CA), was solubilized in aqueous solvents by the precise control of the polarity by addition of organic solvents. The aqueous phase was then incorporated into emulsions through a vortexing step with oil phase without the use of surfactants or multi-step emulsification processes. By tuning the polarity and volume fraction, phase behavior was correlated with emulsion morphology, demonstrating phase-inversion-driven enclosure of the inner dispersed phase to form double emulsions. While stable double emulsions and single emulsions with high UA-CA concentrations were successfully fabricated, ex vivo porcine skin permeation experiments revealed negligible transdermal transport efficacy (<i>C</i><sub>permeate</sub>/<i>C</i><sub>feed</sub> &lt; 10<sup>–5</sup>) of the drug. These results highlights trade-off relationship between the emulsion stability and skin permeability, providing design principles for next-generation topical formulations.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

One-Step Emulsification Enables High Loading of Hydrophobic Drugs, But Not Transdermal Delivery: Phase-Inversion-Driven Double and Single Emulsions Stabilized by Silica Nanoparticles

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2026年4月1日

查看全文
  • Jaehong Lee,
  • Hyun Seo Shim,
  • Seong-Bae Min,
  • Chan-Yeong Heo,
  • Siyoung Q. Choi

摘要

Efficient transdermal delivery of hydrophobic small-molecule drugs remains a persistent challenge in dermatological therapeutics due to the limited solubility of active materials, stability of formulation, and the physical barrier posed by the stratum corneum. Here, we report a one-step emulsification strategy that enables the formation of water-in-oil-in-water (W/O/W) double emulsions and water-in-oil (W/O) single emulsions using silica nanoparticles as the sole stabilizer. A hydrophobic usnic acid derivative active material, usnic acid-cinnamic acid (UA-CA), was solubilized in aqueous solvents by the precise control of the polarity by addition of organic solvents. The aqueous phase was then incorporated into emulsions through a vortexing step with oil phase without the use of surfactants or multi-step emulsification processes. By tuning the polarity and volume fraction, phase behavior was correlated with emulsion morphology, demonstrating phase-inversion-driven enclosure of the inner dispersed phase to form double emulsions. While stable double emulsions and single emulsions with high UA-CA concentrations were successfully fabricated, ex vivo porcine skin permeation experiments revealed negligible transdermal transport efficacy (Cpermeate/Cfeed < 10–5) of the drug. These results highlights trade-off relationship between the emulsion stability and skin permeability, providing design principles for next-generation topical formulations.