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<p>In this study, phenylpropanoid/monoterpene alcohols (eugenol, cinnamyl alcohol, α-terpenol, l-menthol, geraniol and citronellol) and their fatty acid ester derivatives were systematically evaluated as penetration enhancers both in vitro and in vivo on blonanserin and ropinirole. In addition, the mechanisms of penetration enhancement and structure-activity relationship were thoroughly discussed. The permeability promotion effects of the amphiphilic enhancers on two alkaline drugs were investigated across full-thickness rabbit skin in vitro. Skin irritation was evaluated through histological analysis. Finally, the mechanism was elucidated by in vitro release experiments, molecular simulations, attenuated total reflection-Fourier transform infrared spectroscopy, confocal laser microscopy and solid-state nuclear magnetic resonance. Myristate esters had positive promoting effects on the model drugs. Transdermal mechanism studies revealed that penetration enhancers could disturb the spatial arrangement of the side chains of lipids in the stratum corneum, alter the secondary structure of keratin, and enhance the lipid mobility without inducing skin irritation. Chain monoterpenoid myristate esters found to effectively improve the transdermal permeation of the model drugs while avoiding cellular damage.</p>

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Penetration effect and structure-activity relationship of phenylpropanoid/monoterpene alcohols and esters as enhancers on buonserin and ropinirole

  • 期刊论文

  • 发表日期：

    2026年3月13日

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  • Jinwei Zhang,
  • Yan Li,
  • Heping Wang,
  • Mengdi Liu,
  • Runchuang Liu,
  • XinYu Hao,
  • Luyuan Zhang,
  • Ligang Zhao

摘要

In this study, phenylpropanoid/monoterpene alcohols (eugenol, cinnamyl alcohol, α-terpenol, l-menthol, geraniol and citronellol) and their fatty acid ester derivatives were systematically evaluated as penetration enhancers both in vitro and in vivo on blonanserin and ropinirole. In addition, the mechanisms of penetration enhancement and structure-activity relationship were thoroughly discussed. The permeability promotion effects of the amphiphilic enhancers on two alkaline drugs were investigated across full-thickness rabbit skin in vitro. Skin irritation was evaluated through histological analysis. Finally, the mechanism was elucidated by in vitro release experiments, molecular simulations, attenuated total reflection-Fourier transform infrared spectroscopy, confocal laser microscopy and solid-state nuclear magnetic resonance. Myristate esters had positive promoting effects on the model drugs. Transdermal mechanism studies revealed that penetration enhancers could disturb the spatial arrangement of the side chains of lipids in the stratum corneum, alter the secondary structure of keratin, and enhance the lipid mobility without inducing skin irritation. Chain monoterpenoid myristate esters found to effectively improve the transdermal permeation of the model drugs while avoiding cellular damage.