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Background <p>Caffeine possesses therapeutic potential for topical applications such as anti-cellulite and neonatal apnea treatment. However, its hydrophilic nature limits skin penetration. This study aimed to formulate and characterize caffeine-loaded microemulsions specifically designed to enhance transfollicular delivery.</p> Methods <p>Oil-in-water microemulsions were prepared using Tween 80 and Labrasol (surfactants), Capryol 90 (co-surfactant), and an oil phase of oleic acid: Transcutol P (10:1). Formulations were characterized for droplet size, polydispersity, pH, viscosity, surface tension, and physical stability. In vitro drug release and skin permeation kinetics were assessed using Franz diffusion cells across both hairy (abdominal) and non-hairy (ear) guinea pig skin models.</p> Results <p>The microemulsions formed stable, nanoscale droplets (5–15&#xa0;nm) with a skin-compatible pH (~ 5.54) and suitable viscosity (130–176 cps). Phase behavior studies indicated that a higher surfactant/co-surfactant ratio (6:1) expanded the microemulsion region. Formulation MEA-4 exhibited the most favorable drug release profile, achieving 72.4% cumulative release within 24&#xa0;h. Permeation studies demonstrated significantly enhanced caffeine delivery through hairy skin compared to non-hairy skin, confirming the critical role of the transfollicular pathway. Key parameters such as steady-state flux (Jss) and permeability coefficient (Papp) were substantially improved by optimizing the water content and surfactant ratio.</p> Conclusion <p>This study successfully developed an optimized microemulsion system that significantly enhances the transfollicular delivery of caffeine. The formulation’s composition particularly the surfactant/co-surfactant ratio, oil content, and water percentage profoundly influences its physicochemical properties and permeation efficacy. These findings highlight the potential of microemulsions as an effective platform for targeted topical caffeine delivery.</p>

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Transfollicular Delivery of Caffeine via Optimized Microemulsions: Formulation and Skin Kinetics

  • 期刊论文

  • 发表日期：

    2026年3月2日

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  • Anayatollah Salimi,
  • Maryam Lami,
  • Arghavan Salimi,
  • Saeed Mohammad Soleymani

摘要

Background

Caffeine possesses therapeutic potential for topical applications such as anti-cellulite and neonatal apnea treatment. However, its hydrophilic nature limits skin penetration. This study aimed to formulate and characterize caffeine-loaded microemulsions specifically designed to enhance transfollicular delivery.

Methods

Oil-in-water microemulsions were prepared using Tween 80 and Labrasol (surfactants), Capryol 90 (co-surfactant), and an oil phase of oleic acid: Transcutol P (10:1). Formulations were characterized for droplet size, polydispersity, pH, viscosity, surface tension, and physical stability. In vitro drug release and skin permeation kinetics were assessed using Franz diffusion cells across both hairy (abdominal) and non-hairy (ear) guinea pig skin models.

Results

The microemulsions formed stable, nanoscale droplets (5–15 nm) with a skin-compatible pH (~ 5.54) and suitable viscosity (130–176 cps). Phase behavior studies indicated that a higher surfactant/co-surfactant ratio (6:1) expanded the microemulsion region. Formulation MEA-4 exhibited the most favorable drug release profile, achieving 72.4% cumulative release within 24 h. Permeation studies demonstrated significantly enhanced caffeine delivery through hairy skin compared to non-hairy skin, confirming the critical role of the transfollicular pathway. Key parameters such as steady-state flux (Jss) and permeability coefficient (Papp) were substantially improved by optimizing the water content and surfactant ratio.

Conclusion

This study successfully developed an optimized microemulsion system that significantly enhances the transfollicular delivery of caffeine. The formulation’s composition particularly the surfactant/co-surfactant ratio, oil content, and water percentage profoundly influences its physicochemical properties and permeation efficacy. These findings highlight the potential of microemulsions as an effective platform for targeted topical caffeine delivery.