Preparation of topical itraconazole with enhanced skin/nail permeability and in vivo antifungal efficacy against superficial mycosis
- Authors
- Subedi, L.; Song, S.-Y.; Jha, S.K.; Lee, S.-H.; Pangeni, R.; Koo, K.-T.; Kim, B.J.; Cho, S.-S.; Park, J.W.
- Issue Date
- May-2021
- Publisher
- MDPI AG
- Keywords
- Antifungal activity; Itraconazole; Nail infiltration; Skin penetration; Superficial mycosis; Topical solution
- Citation
- Pharmaceutics, v.13, no.5, pp 1 - 16
- Pages
- 16
- Journal Title
- Pharmaceutics
- Volume
- 13
- Number
- 5
- Start Page
- 1
- End Page
- 16
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/48001
- DOI
- 10.3390/pharmaceutics13050622
- ISSN
- 1999-4923
1999-4923
- Abstract
- In this study, a stable and highly skin-permeable topical delivery system for itraconazole (ITZ) was designed to provide effective treatment against superficial mycosis. Herein, ITZ was incorporated into a solution composed of ethanol, benzyl alcohol, hydrochloric acid, Transcutol P, and cyclomethicone as a delivery vehicle, solubilizer, protonating agent, permeation enhancer, and spreading agent, respectively. At 72 h, the optimal topical ITZ formulation (ITZ–TF#11) exhibited 135% enhanced skin permeability, which led to increases in drug deposition in the stratum corneum, epidermis, and dermis of 479%, 739%, and 2024%, respectively, compared with the deposition of 1% ITZ in ethanol (control). Moreover, on day 7, ITZ–TF#11 demonstrated 2.09-and 2.30-fold enhanced nail flux and drug deposition, compared with the control. At a dose of 40 mg/kg/day, ITZ–TF#11 showed 323% greater lesion recovery, a 165% lower mean erythema severity score, and a 37% lower mean logarithm of viable fungal cells in skin in the treated area, compared with mice that received oral ITZ at the same dose. Overall, the findings imply that ITZ–TF#11 is a superior alternative to oral ITZ for treatment of superficial mycosis. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.
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