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Article

Effect of Penetration Enhancers on Toenail Delivery of Efinaconazole from Hydroalcoholic Preparations

1
Colledge of Pharmacy, Dankook University, Dongnam-gu, Cheonan 330-714, Chungnam, Korea
2
Dong-A Pharmaceutical Co. Ltd., Giheung-gu, Yongin 446-905, Gyeonggi, Korea
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Luigi A. Agrofoglio
Molecules 2021, 26(6), 1650; https://doi.org/10.3390/molecules26061650
Received: 17 December 2020 / Revised: 23 February 2021 / Accepted: 9 March 2021 / Published: 16 March 2021
(This article belongs to the Section Medicinal Chemistry)
The incorporation of permeation enhancers in topical preparations has been recognized as a simple and valuable approach to improve the penetration of antifungal agents into toenails. In this study, to improve the toenail delivery of efinaconazole (EFN), a triazole derivative for onychomycosis treatment, topical solutions containing different penetration enhancers were designed, and the permeation profiles were evaluated using bovine hoof models. In an in vitro permeation study in a Franz diffusion cell, hydroalcoholic solutions (HSs) containing lipophilic enhancers, particularly prepared with propylene glycol dicaprylocaprate (Labrafac PG), had 41% higher penetration than the HS base. Moreover, the combination of hydroxypropyl-β-cyclodextrin with Labrafac PG further facilitated the penetration of EFN across the hoof membrane. In addition, this novel topical solution prepared with both lipophilic and hydrophilic enhancers was physicochemically stable, with no drug degradation under ambient conditions (25 °C, for 10 months). Therefore, this HS system can be a promising tool for enhancing the toenail permeability and therapeutic efficacy of EFN. View Full-Text
Keywords: efinaconazole; transungual drug delivery; hydroalcoholic solution; permeation enhancer; bovine hoof; onychomycosis; propylene glycol dicaprylocaprate; hydroxypropyl-β-cyclodextrin efinaconazole; transungual drug delivery; hydroalcoholic solution; permeation enhancer; bovine hoof; onychomycosis; propylene glycol dicaprylocaprate; hydroxypropyl-β-cyclodextrin
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MDPI and ACS Style

Park, J.S.; Kim, J.S.; Ho, M.J.; Park, D.W.; Kim, E.A.; Choi, Y.S.; Jang, S.W.; Kang, M.J. Effect of Penetration Enhancers on Toenail Delivery of Efinaconazole from Hydroalcoholic Preparations. Molecules 2021, 26, 1650. https://doi.org/10.3390/molecules26061650

AMA Style

Park JS, Kim JS, Ho MJ, Park DW, Kim EA, Choi YS, Jang SW, Kang MJ. Effect of Penetration Enhancers on Toenail Delivery of Efinaconazole from Hydroalcoholic Preparations. Molecules. 2021; 26(6):1650. https://doi.org/10.3390/molecules26061650

Chicago/Turabian Style

Park, Jun S., Jeong S. Kim, Myoung J. Ho, Dong W. Park, Eun A. Kim, Yong S. Choi, Sun W. Jang, and Myung J. Kang 2021. "Effect of Penetration Enhancers on Toenail Delivery of Efinaconazole from Hydroalcoholic Preparations" Molecules 26, no. 6: 1650. https://doi.org/10.3390/molecules26061650

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