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Current Drug Delivery

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ISSN (Print): 1567-2018
ISSN (Online): 1875-5704

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Research Article

Characterization, Antifungal Evaluation against Candida spp. Strains and Application of Nystatin: β-cyclodextrin Inclusion Complexes

Author(s): Amanda Migliorini Urban, Francine Sumie Morikava, Amanda Cristina Schoeffel, Andressa Novatski, Gustavo Simão Moraes, Victoria Schlumberger Cachoeira, Graciette Matioli, Carmen Antonia Sanches Ito, Priscileila Colerato Ferrari, Karin Hermana Neppelenbroek, Vanessa Migliorini Urban* and Paulo Vitor Farago

Volume 20, Issue 10, 2023

Published on: 03 November, 2022

Page: [1533 - 1546] Pages: 14

DOI: 10.2174/1567201820666221017103119

Price: $65

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Abstract

Background: Nystatin (Nys) is a fungicidal drug commonly prescribed for candidiasis disease in several administration routes. However, Nys is a class IV drug, according to the Biopharmaceutical Classification System, that possesses limited bioavailability and is used for local activity.

Objective: This study developed and characterized nystatin:β-cyclodextrin (Nys:βCD) inclusion complexes and evaluated their activity against Candida spp.

Methods: Complexes were characterized by physicochemical techniques and drug dissolution profiles. The susceptibility of C. albicans, C. krusei, C. parapsilosis, C. glabrata, C. guilliermondii, C. tropicalis, and C. auris was assessed using the broth microdilution method. The applicability of Nys:βCD inclusion complex was evaluated by incorporating it into a temporary soft material for denture stomatitis treatment.

Results: Nys was better complexed in a 1:1 molar ratio by freeze-drying and spray-drying methods. The inclusion complexes show bi-exponential release, an initial burst release followed by a sustained manner, presenting higher dissolution efficiency than raw Nys. The 1:1 freeze-drying Nys: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 Nys.

Conclusion: 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.

Keywords: Nystatin, beta-cyclodextrins, freeze-drying, spray-drying, Candida spp., denture stomatitis, DSC.

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