Transdermal Delivery of Low-Molecular-Weight Drugs and New Modality of Drugs: Recent Innovation to Penetration Enhancement Techniques

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: 20 April 2025 | Viewed by 764

Special Issue Editors


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Guest Editor
1. Department of Medical Pharmacy, Graduate School of Pharmaceutical Sciences, Josai International University, 1 Gumyo Togane, Chiba 283-0002, Japan
2. Faculty of Pharmaceutical Sciences, Josai International University, 1 Gumyo Togane, Chiba 283-0002, Japan
3. Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, 1-1 Keyakidai Sakado, Saitama 350-0295, Japan
Interests: pharmaceutical technology; drug delivery; skin permeation
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Guest Editor
Department of Medical Pharmacy, Graduate School of Pharmaceutical Sciences, Josai International University, 1 Gumyo Togane, Chiba 283-0002, Japan
Interests: pharmaceutical technology; drug delivery; skin permeation

Special Issue Information

Dear Colleagues,

The current diversification of drug discovery methods has sparked a revolution in technologies for seeking active pharmaceutical ingredients. Simultaneously, the developments in drug administration methods form new modalities and low-molecular-weight drugs. Consequently, there is a growing need to establish methodologies that facilitate easy administration, particularly for children and patients with dementia. If sufficient quantities of drugs, including medium-sized molecules, can be effectively administered through the skin, it could significantly advance overall drug therapy. For this Special Issue, we encourage scientists worldwide to propose innovations in penetration enhancement techniques that enable transdermal delivery not only for small molecules, but also for medium-sized drugs.

Prof. Dr. Kenji Sugibayashi
Dr. Takeshi Oshizaka
Guest Editors

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Keywords

  • transdermal delivery
  • enhanced skin permeation
  • penetration enhancer
  • microneedle
  • iontophoresis
  • new modality
  • easy administration
  • skin barrier

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Published Papers (1 paper)

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Research

12 pages, 1677 KiB  
Article
Enhanced Drug Skin Permeation by Azone-Mimicking Ionic Liquids: Effects of Fatty Acids Forming Ionic Liquids
by Takeshi Oshizaka, Shunsuke Kodera, Rika Kawakubo, Issei Takeuchi, Kenji Mori and Kenji Sugibayashi
Pharmaceutics 2025, 17(1), 41; https://doi.org/10.3390/pharmaceutics17010041 - 30 Dec 2024
Viewed by 401
Abstract
Background/Objectives: Laurocapram (Azone) attracted attention 40 years ago as a compound with the highest skin-penetration-enhancing effect at that time; however, its development was shelved due to strong skin irritation. We had already prepared and tested an ante-enhancer (IL-Azone), an ionic liquid (IL) [...] Read more.
Background/Objectives: Laurocapram (Azone) attracted attention 40 years ago as a compound with the highest skin-penetration-enhancing effect at that time; however, its development was shelved due to strong skin irritation. We had already prepared and tested an ante-enhancer (IL-Azone), an ionic liquid (IL) with a similar structure to Azone, consisting of ε-caprolactam and myristic acid, as an enhancer candidate that maintains the high skin-penetration-enhancing effect of Azone with low skin irritation. In the present study, fatty acids with different carbon numbers (caprylic acid: C8, capric acid: C10, lauric acid: C12, myristic acid: C14, and oleic acid: C18:1) were selected and used with ε-caprolactam to prepare various IL-Azones in the search for a more effective IL-Azone. Methods: Excised porcine skin was pretreated with each IL-Azone to assess the in vitro skin permeability of antipyrine (ANP) as a model penetrant. In addition, 1,3-butanediol was selected for the skin permeation test to confirm whether the effect of IL-Azone was due to fatty acids and if this effect differed depending on the concentration of IL-Azone applied. Results: The results obtained showed that C12 IL-Azone exerted the highest skin-penetration-enhancing effect, which was higher than Azone. On the other hand, many of the IL-Azones tested had a lower skin-penetration-enhancing effect. Conclusions: These results suggest the potential of C12 IL-Azone as a strong and useful penetration enhancer. Full article
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