Abstract
Efficient topical delivery of antifungal drugs, such as lanoconazole (LCZ), is challenging due to the limited water solubility and required prolonged duration of treatment. In this study, LCZ-loaded emulsions stabilized with cellulose nanocrystals grafted with polyphosphoesters (LCZ-loaded CP-PEs) were developed to enhance the anti-inflammatory efficacy of LCZ on skin. A high drug-loading efficiency (>80%) of LCZ in CP-PEs with a small mean droplet size of 1.0–1.5 μm was achieved. The sustained release of LCZ and superior skin permeation of the LCZ-loaded CP-PEs, likely due to the excellent stability and rigidity of oil droplets, assured prolonged local action. In addition, the excellent anti-inflammatory efficacy of the LCZ-loaded CP-PEs was clarified using a mouse ear model of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation. Treatment with the LCZ-loaded CP-PEs significantly reduced auricular thickness compared to treatments with a commercial ointment and control solution containing LCZ. These results suggest that LCZ-loaded CP-PEs are a promising alternative for the treatment of inflammatory skin diseases, such as tinea pedis.
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Acknowledgements
This study was financially supported by grants from JSPS KAKENHI (grant no. 19H04474) and the MEXT Private University Research Branding Project.
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S.H., methodology, investigation, and writing - original draft; A.O., methodology; S.F., methodology and resources; Y.I., conceptualization, supervision, writing - review & editing, and funding acquisition.
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Hiranphinyophat, S., Otaka, A., Fujii, S. et al. Lanoconazole-loaded emulsion stabilized with cellulose nanocrystals decorated with polyphosphoesters reduced inflammatory edema in a mouse model. Polym J 53, 1493–1498 (2021). https://doi.org/10.1038/s41428-021-00548-1
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DOI: https://doi.org/10.1038/s41428-021-00548-1