Nystatin:β-cyclodextrin inclusion complexes – revisited

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The Nystatin/CD complexes appeared in the literature in 1990 with so far 210 publications mentioning both nystatin and cyclodextrin (SCOPUS). Still there is no CD-enabled Nystatin formulation on the market.

In this work, Nystatin was complexed in a 1:1 molar ratio by freeze-drying and spray-drying methods. The inclusion complexes showed bi-exponential release, an initial burst release followed by a sustained manner, presenting higher dissolution efficiency than raw Nystatin. The 1:1 freeze-dried Nystatin:βCD complex presents antifungal activity against all evaluated Candida strains, showing the maintenance of the drug effectiveness. The inclusion complex incorporated into a tissue conditioner material for denture stomatitis treatment effectively inhibited more than 90% of C. albicans biofilm growth during 7 and 14 days, in a half dose compared to raw Nystatin.

This work represents a significant contribution to treating a wide variety of diseases caused by the Candida species, optimizing the drug bioavailability and compliance to the treatment due to improved drug solubility, dissolution, and sustained delivery.

Urban AM, Morikava FS, Schoeffel AC, Novatski A, Moraes GS, Cachoeira VS, Matioli G, Sanches Ito CA, Ferrari PC, Neppelenbroek KH, Urban VM, Farago PV. Characterization, antifungal evaluation against Candida spp. strains, and application of nystatin:β-cyclodextrin inclusion complexes. Curr Drug Deliv. 2022 Oct 17. doi: 10.2174/1567201820666221017103119. Epub ahead of print. PMID: 36263476.

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