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Newfangled Topical Film-Forming Solution for Facilitated Antifungal Therapy: Design, Development, Characterization, and In Vitro Evaluation
Luliconazole is a broad-spectrum topical antifungal agent that acts by altering the synthesis of fungi cell membranes. Literature suggests that the recurrence of fungal infection can be avoided by altering the pH of the site of infection. Studies have also suggested that fungi thrive by altering ski...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9961451/ https://www.ncbi.nlm.nih.gov/pubmed/36850286 http://dx.doi.org/10.3390/polym15041003 |
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author | Dhimmar, Bhakti Pokale, Rahul Rahamathulla, Mohamed Hani, Umme Alshahrani, Mohammad Y. Alshehri, Sultan Shakeel, Faiyaz Alam, Prawez Osmani, Riyaz Ali M. Patil, Amit B. |
author_facet | Dhimmar, Bhakti Pokale, Rahul Rahamathulla, Mohamed Hani, Umme Alshahrani, Mohammad Y. Alshehri, Sultan Shakeel, Faiyaz Alam, Prawez Osmani, Riyaz Ali M. Patil, Amit B. |
author_sort | Dhimmar, Bhakti |
collection | PubMed |
description | Luliconazole is a broad-spectrum topical antifungal agent that acts by altering the synthesis of fungi cell membranes. Literature suggests that the recurrence of fungal infection can be avoided by altering the pH of the site of infection. Studies have also suggested that fungi thrive by altering skin pH to be slightly acidic, i.e., pH 3–5. The current study is aimed to design, develop, characterize, and evaluate an alkaline pH-based antifungal spray solution for antifungal effects. Luliconazole was used as an antifungal agent and an alkaline spray was formulated for topical application by using Eudragit RS 100, propylene glycol (PG), water, sodium bicarbonate, and ethanol via solubilization method. Herein, sodium bicarbonate was used as an alkalizing agent. Based on DSC, FTIR, PXRD, scanning electron microscopy (SEM), and rheological analysis outcomes, the drug (luliconazole) and polymer were found to be compatible. F-14 formulation containing 22% Eudragit RS 100 (ERS), 1.5% PG, and 0.25% sodium bicarbonate was optimized by adopting the quality by design approach by using design of experiment software. The viscosity, pH, drying time, volume of solution post spraying, and spray angle were, 14.99 ± 0.21 cp, 8 pH, 60 s, 0.25 mL ± 0.05 mL, and 80 ± 2, respectively. In vitro drug diffusion studies and in vitro antifungal trials against Candida albicans revealed 98.0 ± 0.2% drug diffusion with a zone of inhibition of 9 ± 0.12 mm. The findings of the optimized luliconazole topical film-forming solution were satisfactory, it was compatible with human skin, and depicted sustained drug release that suggests promising applicability in facilitated topical antifungal treatments. |
format | Online Article Text |
id | pubmed-9961451 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-99614512023-02-26 Newfangled Topical Film-Forming Solution for Facilitated Antifungal Therapy: Design, Development, Characterization, and In Vitro Evaluation Dhimmar, Bhakti Pokale, Rahul Rahamathulla, Mohamed Hani, Umme Alshahrani, Mohammad Y. Alshehri, Sultan Shakeel, Faiyaz Alam, Prawez Osmani, Riyaz Ali M. Patil, Amit B. Polymers (Basel) Article Luliconazole is a broad-spectrum topical antifungal agent that acts by altering the synthesis of fungi cell membranes. Literature suggests that the recurrence of fungal infection can be avoided by altering the pH of the site of infection. Studies have also suggested that fungi thrive by altering skin pH to be slightly acidic, i.e., pH 3–5. The current study is aimed to design, develop, characterize, and evaluate an alkaline pH-based antifungal spray solution for antifungal effects. Luliconazole was used as an antifungal agent and an alkaline spray was formulated for topical application by using Eudragit RS 100, propylene glycol (PG), water, sodium bicarbonate, and ethanol via solubilization method. Herein, sodium bicarbonate was used as an alkalizing agent. Based on DSC, FTIR, PXRD, scanning electron microscopy (SEM), and rheological analysis outcomes, the drug (luliconazole) and polymer were found to be compatible. F-14 formulation containing 22% Eudragit RS 100 (ERS), 1.5% PG, and 0.25% sodium bicarbonate was optimized by adopting the quality by design approach by using design of experiment software. The viscosity, pH, drying time, volume of solution post spraying, and spray angle were, 14.99 ± 0.21 cp, 8 pH, 60 s, 0.25 mL ± 0.05 mL, and 80 ± 2, respectively. In vitro drug diffusion studies and in vitro antifungal trials against Candida albicans revealed 98.0 ± 0.2% drug diffusion with a zone of inhibition of 9 ± 0.12 mm. The findings of the optimized luliconazole topical film-forming solution were satisfactory, it was compatible with human skin, and depicted sustained drug release that suggests promising applicability in facilitated topical antifungal treatments. MDPI 2023-02-17 /pmc/articles/PMC9961451/ /pubmed/36850286 http://dx.doi.org/10.3390/polym15041003 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Dhimmar, Bhakti Pokale, Rahul Rahamathulla, Mohamed Hani, Umme Alshahrani, Mohammad Y. Alshehri, Sultan Shakeel, Faiyaz Alam, Prawez Osmani, Riyaz Ali M. Patil, Amit B. Newfangled Topical Film-Forming Solution for Facilitated Antifungal Therapy: Design, Development, Characterization, and In Vitro Evaluation |
title | Newfangled Topical Film-Forming Solution for Facilitated Antifungal Therapy: Design, Development, Characterization, and In Vitro Evaluation |
title_full | Newfangled Topical Film-Forming Solution for Facilitated Antifungal Therapy: Design, Development, Characterization, and In Vitro Evaluation |
title_fullStr | Newfangled Topical Film-Forming Solution for Facilitated Antifungal Therapy: Design, Development, Characterization, and In Vitro Evaluation |
title_full_unstemmed | Newfangled Topical Film-Forming Solution for Facilitated Antifungal Therapy: Design, Development, Characterization, and In Vitro Evaluation |
title_short | Newfangled Topical Film-Forming Solution for Facilitated Antifungal Therapy: Design, Development, Characterization, and In Vitro Evaluation |
title_sort | newfangled topical film-forming solution for facilitated antifungal therapy: design, development, characterization, and in vitro evaluation |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9961451/ https://www.ncbi.nlm.nih.gov/pubmed/36850286 http://dx.doi.org/10.3390/polym15041003 |
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