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Lanoconazole-loaded emulsion stabilized with cellulose nanocrystals decorated with polyphosphoesters reduced inflammatory edema in a mouse model

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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Correspondence to Yasuhiko Iwasaki.

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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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