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Effects of Temperature and Humidity on the Skin Permeation of Hydrophilic and Hydrophobic Drugs

  • Research Article
  • Theme: Advances in Topical Delivery of Drugs
  • Published:
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Abstract

The humidity was a well-known method to hydrate the skin; however, the published data were varied, and systemic experiments in the previous papers were few. Therefore, the in vitro permeation of excised porcine ear skin by drugs with different polarities [aminopyrine (AMP), antipyrine (ANP), methylparaben (MP), and ibuprofen (IP)] was analyzed under a constant skin surface temperature with different temperatures and humidities to reveal the effects of temperature and humidity on the skin permeation enhancement effects. Applied formulations were prepared by mixing the drug and a hydrophilic vehicle containing glycerin. The disposition-distance profiles of water and the humectant glycerin in the stratum corneum were also investigated using confocal Raman microscopy. High absolute humidity (AH) significantly contributed to the high skin penetration of the hydrophilic penetrants AMP, ANP, and MP but not the hydrophobic penetrant IP. An increase in the partition parameter and a decrease in the diffusivity parameter occurred with an increase in AH, independent of drug polarity. Moreover, we found that dew condensation induced by high AH on temperature-controlled skin surface may effectively increase water content and may provide higher glycerin distribution in the skin barrier, the stratum corneum. Increasing the amount of water and hydrophilic vehicles such as glycerin in the stratum corneum may enhance the permeation of hydrophilic penetrants AMP, ANP, and MP. These data suggested a dew condensation on the skin surface induced by high AH at a constant skin surface temperature would be important to enhance hydrophilic penetrants.

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Authors and Affiliations

  1. R&D–Development Research, Kao Corporation, 2-1-3 Bunka, Sumida-ku, Tokyo, 131-8501, Japan

    Hiroaki Iikura, Koji Uchida, Satoru Naitou, Masaru Hosokawa & Takashi Uchida

  2. Biological Science Laboratories, Kao Corporation, 2606 Akabane, Ichikai-machi, Haga-gun, Tochigi, 321-3497, Japan

    Chie Ogawa-Fuse

  3. Analytical Science Research Laboratories, Kao Corporation, 2606 Akabane, Ichikai-machi, Haga-gun, Tochigi, 321-3497, Japan

    Kotatsu Bito

  4. Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama, 350-0295, Japan

    Takashi Uchida, Hiroaki Todo & Kenji Sugibayashi

  5. Faculty of Life and Environmental Sciences, Teikyo University of Science, 2-2-1 Senju Sakuragi, Adachi-ku, Tokyo, 120-0045, Japan

    Tomohiko Sano

Authors
  1. Hiroaki Iikura
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  2. Koji Uchida
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  5. Satoru Naitou
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  6. Masaru Hosokawa
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  7. Takashi Uchida
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  8. Tomohiko Sano
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  9. Hiroaki Todo
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  10. Kenji Sugibayashi
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Correspondence to Tomohiko Sano or Kenji Sugibayashi.

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Guest Editor: S. Narasimha Murthy

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Iikura, H., Uchida, K., Ogawa-Fuse, C. et al. Effects of Temperature and Humidity on the Skin Permeation of Hydrophilic and Hydrophobic Drugs. AAPS PharmSciTech 20, 264 (2019). https://doi.org/10.1208/s12249-019-1481-1

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  • DOI: https://doi.org/10.1208/s12249-019-1481-1

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