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

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Urban, Amanda Migliorini ; Morikava, Francine Sumie ; Schoeffel, Amanda Cristina ; Novatski, Andressa ; Moraes, Gustavo Simao ; Cachoeira, Victoria Schlumberger ; Matioli, Graciette ; Ito, Carmen Antonia Sanches ; Ferrari, Priscileila Colerato ; Neppelenbroek, Karin Hermana ; Urban, Vanessa Migliorini ; Farago, Paulo Vitor

• Document type: Journal article
• Source: CURRENT DRUG DELIVERY; v. 20, n. 10, p. 14-pg., 2023-01-01.

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:& beta;-cyclodextrin (Nys:& beta;CD) 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:& beta;CD 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:& beta;CD 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. (AU)

• FAPESP's process: 17/07314-1 - Clinical evaluation of antifungal addition to temporary soft liner in the treatment of denture stomatitis
• Grantee: Karin Hermana Neppelenbroek
• Support Opportunities: Regular Research Grants