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Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis

Dermatophytosis, the most prevalent fungal infection, is witnessing a rising incidence annually. To address this challenge, we developed a terbinafine-loaded oil-in-water nanoemulsion (TH-NE) through the aqueous microtitration method. The formulation comprised olive oil (oil phase), Span 80 (surfact...

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Autores principales: Phagna, Mayank, Badhwar, Reena, Singh, Manvi, Alhalmi, Abdulsalam, Khan, Rahmuddin, Noman, Omar M., Alahdab, Ahmad
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10670648/
https://www.ncbi.nlm.nih.gov/pubmed/37998984
http://dx.doi.org/10.3390/gels9110894
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author Phagna, Mayank
Badhwar, Reena
Singh, Manvi
Alhalmi, Abdulsalam
Khan, Rahmuddin
Noman, Omar M.
Alahdab, Ahmad
author_facet Phagna, Mayank
Badhwar, Reena
Singh, Manvi
Alhalmi, Abdulsalam
Khan, Rahmuddin
Noman, Omar M.
Alahdab, Ahmad
author_sort Phagna, Mayank
collection PubMed
description Dermatophytosis, the most prevalent fungal infection, is witnessing a rising incidence annually. To address this challenge, we developed a terbinafine-loaded oil-in-water nanoemulsion (TH-NE) through the aqueous microtitration method. The formulation comprised olive oil (oil phase), Span 80 (surfactant), and propylene glycol (co-surfactant). Pseudo-phase ternary diagrams and thermodynamic studies underscored the stability of TH-NE. Employing the Box–Behnken design (BBD), we optimized TH-NE, which resulted in a remarkable particle size of 28.07 nm ± 0.5, a low polydispersity index (PDI) of 0.1922 ± 0.1, and a substantial negative zeta potential of −41.87 mV ± 1. Subsequently, TH-NE was integrated into a 1.5% carbopol matrix, yielding a nanoemulgel (TH-NEG). Texture analysis of TH-NEG demonstrated a firmness of 168.00 g, a consistency of 229.81 g/s, negative cohesiveness (−83.36 g), and a work of cohesion at −107.02 g/s. In vitro drug release studies revealed an initial burst effect followed by sustained release, with TH-NEG achieving an impressive 88% release over 48 h, outperforming TH-NE (74%) and the marketed formulation (66%). Ex vivo release studies mirrored these results, with TH-NEG (86%) and TH-NE (71%) showcasing sustained drug release in comparison to the marketed formulation (67%). Confocal microscopy illustrated that TH-NEG and TH-NE penetrated to depths of 30 µm and 25 µm, respectively, into the epidermal layer. Furthermore, dermatokinetic studies highlighted the enhanced drug penetration of TH-NEG compared to TH-NE through mouse skin. In summary, our study establishes TH-NEG as a promising carrier for terbinafine in treating dermatophytosis, offering improved drug delivery and sustained release potential.
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spelling pubmed-106706482023-11-12 Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis Phagna, Mayank Badhwar, Reena Singh, Manvi Alhalmi, Abdulsalam Khan, Rahmuddin Noman, Omar M. Alahdab, Ahmad Gels Article Dermatophytosis, the most prevalent fungal infection, is witnessing a rising incidence annually. To address this challenge, we developed a terbinafine-loaded oil-in-water nanoemulsion (TH-NE) through the aqueous microtitration method. The formulation comprised olive oil (oil phase), Span 80 (surfactant), and propylene glycol (co-surfactant). Pseudo-phase ternary diagrams and thermodynamic studies underscored the stability of TH-NE. Employing the Box–Behnken design (BBD), we optimized TH-NE, which resulted in a remarkable particle size of 28.07 nm ± 0.5, a low polydispersity index (PDI) of 0.1922 ± 0.1, and a substantial negative zeta potential of −41.87 mV ± 1. Subsequently, TH-NE was integrated into a 1.5% carbopol matrix, yielding a nanoemulgel (TH-NEG). Texture analysis of TH-NEG demonstrated a firmness of 168.00 g, a consistency of 229.81 g/s, negative cohesiveness (−83.36 g), and a work of cohesion at −107.02 g/s. In vitro drug release studies revealed an initial burst effect followed by sustained release, with TH-NEG achieving an impressive 88% release over 48 h, outperforming TH-NE (74%) and the marketed formulation (66%). Ex vivo release studies mirrored these results, with TH-NEG (86%) and TH-NE (71%) showcasing sustained drug release in comparison to the marketed formulation (67%). Confocal microscopy illustrated that TH-NEG and TH-NE penetrated to depths of 30 µm and 25 µm, respectively, into the epidermal layer. Furthermore, dermatokinetic studies highlighted the enhanced drug penetration of TH-NEG compared to TH-NE through mouse skin. In summary, our study establishes TH-NEG as a promising carrier for terbinafine in treating dermatophytosis, offering improved drug delivery and sustained release potential. MDPI 2023-11-12 /pmc/articles/PMC10670648/ /pubmed/37998984 http://dx.doi.org/10.3390/gels9110894 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
Phagna, Mayank
Badhwar, Reena
Singh, Manvi
Alhalmi, Abdulsalam
Khan, Rahmuddin
Noman, Omar M.
Alahdab, Ahmad
Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis
title Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis
title_full Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis
title_fullStr Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis
title_full_unstemmed Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis
title_short Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis
title_sort development and characterization of terbinafine-loaded nanoemulgel for effective management of dermatophytosis
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10670648/
https://www.ncbi.nlm.nih.gov/pubmed/37998984
http://dx.doi.org/10.3390/gels9110894
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