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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Main Authors: Mayank Phagna, Reena Badhwar, Manvi Singh, Abdulsalam Alhalmi, Rahmuddin Khan, Omar M. Noman, Ahmad Alahdab
Format: Article
Language:English
Published: MDPI AG 2023-11-01
Series:Gels
Subjects:
Online Access:https://www.mdpi.com/2310-2861/9/11/894
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author Mayank Phagna
Reena Badhwar
Manvi Singh
Abdulsalam Alhalmi
Rahmuddin Khan
Omar M. Noman
Ahmad Alahdab
author_facet Mayank Phagna
Reena Badhwar
Manvi Singh
Abdulsalam Alhalmi
Rahmuddin Khan
Omar M. Noman
Ahmad Alahdab
author_sort Mayank Phagna
collection DOAJ
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 doaj.art-df55b83cc1724b068f22ada34cfba8432023-11-24T14:43:25ZengMDPI AGGels2310-28612023-11-0191189410.3390/gels9110894Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of DermatophytosisMayank Phagna0Reena Badhwar1Manvi Singh2Abdulsalam Alhalmi3Rahmuddin Khan4Omar M. Noman5Ahmad Alahdab6Department of Pharmaceutics, SGT College of Pharmacy, SGT University, Gurugram 122001, IndiaDepartment of Pharmaceutics, SGT College of Pharmacy, SGT University, Gurugram 122001, IndiaDepartment of Pharmaceutics, SGT College of Pharmacy, SGT University, Gurugram 122001, IndiaDepartment of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, IndiaDepartment of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, IndiaDepartment of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaInstitute of Pharmacy, Clinical Pharmacy, University of Greifswald, Friedrich-Ludwig-Jahn-Str. 17, 17489 Greifswald, GermanyDermatophytosis, 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.https://www.mdpi.com/2310-2861/9/11/894terbinafine hydrochloridedermatophytosisnanoemulgelnanoemulsiontexture analysis
spellingShingle Mayank Phagna
Reena Badhwar
Manvi Singh
Abdulsalam Alhalmi
Rahmuddin Khan
Omar M. Noman
Ahmad Alahdab
Development and Characterization of Terbinafine-Loaded Nanoemulgel for Effective Management of Dermatophytosis
Gels
terbinafine hydrochloride
dermatophytosis
nanoemulgel
nanoemulsion
texture analysis
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 terbinafine hydrochloride
dermatophytosis
nanoemulgel
nanoemulsion
texture analysis
url https://www.mdpi.com/2310-2861/9/11/894
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