IADR Abstract Archives
Cytocompatibility and Antifungal Effectiveness of a Mucoadhesive Formulation Containing Nystatin Complexed With β-Cyclodextrin
Objectives: To evaluate the biocompatibility and antifungal effects of mucoadhesive gels containing raw nystatin or nystatin complexed with β-cyclodextrin (βCD).
Methods: The mucoadhesive formulation was developed with chitosan and hydroxyethylcellulose, incorporating nystatin at 16.1 mg/g (Nys 16.1 group), 32 mg/g (Nys 32 group) or complexed with βCD 36 mg/g (equivalent to 16.1 mg/g of Nys) (Nys:βCD group). Groups using mucoadhesive gel without drug incorporation (Gel group) and 2% miconazole oral gel (Daktarin®; Dk group) were also evaluated. Gel leachates were diluted at selected concentrations. Cell viability (MTT assay, using L929 murine fibroblasts) and antifungal potential (EUCAST broth microdilution method and metabolic activity of Candida albicans ATCC 10231 by resazurin assay) were assessed at distinct leachate’s concentrations. Results were expressed in percentages, and gel leachates with cell viability >75% were considered non-cytotoxic. Statistical analysis of resazurin assay was performed using 2-way ANOVA, followed by Dunnett's test (α=0.05).
Results: The Gel, Nys 16.1, and Nys 32 groups exhibited slight or moderate cytotoxicity at 100% leachate concentration, reaching maximum viability with 25% and 12.5%. The Nys:βCD group showed no cytotoxicity at any concentration, while the Dk group exhibited cytotoxicity at concentrations above 1%. Similarly to the control group ATCC10231, the Gel group demonstrated no antifungal activity with high metabolic activity of C. albicans (p>0.05). Dk group exhibited low inhibition values (0-30%) without differences from the control (p>0.05). Nystatin-containing groups (Nys 16.1, Nys 32, and Nys:βCD) showed high fungal inhibition capacity (>90%) and low metabolic activity of C. albicans, even at low concentrations (p<0.05).
Conclusions: Mucoadhesives containing nystatin showed therapeutic potential for oral candidiasis in terms of cytocompatibility and antifungal activity. Nonetheless, the association of nystatin-βCD resulted in improved cytocompatibility performance and similar antifungal activity, suggesting potential therapeutical benefits in efficiency.
Methods: The mucoadhesive formulation was developed with chitosan and hydroxyethylcellulose, incorporating nystatin at 16.1 mg/g (Nys 16.1 group), 32 mg/g (Nys 32 group) or complexed with βCD 36 mg/g (equivalent to 16.1 mg/g of Nys) (Nys:βCD group). Groups using mucoadhesive gel without drug incorporation (Gel group) and 2% miconazole oral gel (Daktarin®; Dk group) were also evaluated. Gel leachates were diluted at selected concentrations. Cell viability (MTT assay, using L929 murine fibroblasts) and antifungal potential (EUCAST broth microdilution method and metabolic activity of Candida albicans ATCC 10231 by resazurin assay) were assessed at distinct leachate’s concentrations. Results were expressed in percentages, and gel leachates with cell viability >75% were considered non-cytotoxic. Statistical analysis of resazurin assay was performed using 2-way ANOVA, followed by Dunnett's test (α=0.05).
Results: The Gel, Nys 16.1, and Nys 32 groups exhibited slight or moderate cytotoxicity at 100% leachate concentration, reaching maximum viability with 25% and 12.5%. The Nys:βCD group showed no cytotoxicity at any concentration, while the Dk group exhibited cytotoxicity at concentrations above 1%. Similarly to the control group ATCC10231, the Gel group demonstrated no antifungal activity with high metabolic activity of C. albicans (p>0.05). Dk group exhibited low inhibition values (0-30%) without differences from the control (p>0.05). Nystatin-containing groups (Nys 16.1, Nys 32, and Nys:βCD) showed high fungal inhibition capacity (>90%) and low metabolic activity of C. albicans, even at low concentrations (p<0.05).
Conclusions: Mucoadhesives containing nystatin showed therapeutic potential for oral candidiasis in terms of cytocompatibility and antifungal activity. Nonetheless, the association of nystatin-βCD resulted in improved cytocompatibility performance and similar antifungal activity, suggesting potential therapeutical benefits in efficiency.