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Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol(®) Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study
The present research was aimed to develop a terbinafin hydrochloride (TH)-encapsulated solid lipid nanoparticles (SLNs) hydrogel for improved antifungal efficacy. TH-loaded SLNs were obtained from glyceryl monostearate (lipid) and Pluronic(®) F68 (surfactant) employing high-pressure homogenization....
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9320640/ https://www.ncbi.nlm.nih.gov/pubmed/35890289 http://dx.doi.org/10.3390/pharmaceutics14071393 |
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author | Rarokar, Nilesh R. Menghani, Sunil S. Kerzare, Deweshri R. Khedekar, Pramod B. Bharne, Ashish P. Alamri, Abdulhakeem S. Alsanie, Walaa F. Alhomrani, Majid Sreeharsha, Nagaraja Asdaq, Syed Mohammed Basheeruddin |
author_facet | Rarokar, Nilesh R. Menghani, Sunil S. Kerzare, Deweshri R. Khedekar, Pramod B. Bharne, Ashish P. Alamri, Abdulhakeem S. Alsanie, Walaa F. Alhomrani, Majid Sreeharsha, Nagaraja Asdaq, Syed Mohammed Basheeruddin |
author_sort | Rarokar, Nilesh R. |
collection | PubMed |
description | The present research was aimed to develop a terbinafin hydrochloride (TH)-encapsulated solid lipid nanoparticles (SLNs) hydrogel for improved antifungal efficacy. TH-loaded SLNs were obtained from glyceryl monostearate (lipid) and Pluronic(®) F68 (surfactant) employing high-pressure homogenization. The ratio of drug with respect to lipid was optimized, considering factors such as desired particle size and highest percent encapsulation efficiency. Lyophilized SLNs were then incorporated in the hydrogel prepared from 0.2–1.0% w/v carbopol 934P and further evaluated for rheological parameters. The z-average, zeta potential and polydispersity index were found to be 241.3 nm, −15.2 mV and 0.415, respectively. The SLNs show a higher entrapment efficiency of about 98.36%, with 2.12 to 6.3602% drug loading. SEM images, XRD and the results of the DSC, FTIR show successful preparation of SLNs after freeze drying. The TH-loaded SLNs hydrogel showed sustained drug release (95.47 ± 1.45%) over a period of 24 h. The results reported in this study show a significant effect on the zone of inhibition than the marketed formulation and pure drug in Candida albicans cultures, with better physical stability at cooler temperatures. It helped to enhance skin deposition inthe ex vivostudy and improved, in vitro and in vivo, the antifungal activity. |
format | Online Article Text |
id | pubmed-9320640 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-93206402022-07-27 Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol(®) Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study Rarokar, Nilesh R. Menghani, Sunil S. Kerzare, Deweshri R. Khedekar, Pramod B. Bharne, Ashish P. Alamri, Abdulhakeem S. Alsanie, Walaa F. Alhomrani, Majid Sreeharsha, Nagaraja Asdaq, Syed Mohammed Basheeruddin Pharmaceutics Article The present research was aimed to develop a terbinafin hydrochloride (TH)-encapsulated solid lipid nanoparticles (SLNs) hydrogel for improved antifungal efficacy. TH-loaded SLNs were obtained from glyceryl monostearate (lipid) and Pluronic(®) F68 (surfactant) employing high-pressure homogenization. The ratio of drug with respect to lipid was optimized, considering factors such as desired particle size and highest percent encapsulation efficiency. Lyophilized SLNs were then incorporated in the hydrogel prepared from 0.2–1.0% w/v carbopol 934P and further evaluated for rheological parameters. The z-average, zeta potential and polydispersity index were found to be 241.3 nm, −15.2 mV and 0.415, respectively. The SLNs show a higher entrapment efficiency of about 98.36%, with 2.12 to 6.3602% drug loading. SEM images, XRD and the results of the DSC, FTIR show successful preparation of SLNs after freeze drying. The TH-loaded SLNs hydrogel showed sustained drug release (95.47 ± 1.45%) over a period of 24 h. The results reported in this study show a significant effect on the zone of inhibition than the marketed formulation and pure drug in Candida albicans cultures, with better physical stability at cooler temperatures. It helped to enhance skin deposition inthe ex vivostudy and improved, in vitro and in vivo, the antifungal activity. MDPI 2022-06-30 /pmc/articles/PMC9320640/ /pubmed/35890289 http://dx.doi.org/10.3390/pharmaceutics14071393 Text en © 2022 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 Rarokar, Nilesh R. Menghani, Sunil S. Kerzare, Deweshri R. Khedekar, Pramod B. Bharne, Ashish P. Alamri, Abdulhakeem S. Alsanie, Walaa F. Alhomrani, Majid Sreeharsha, Nagaraja Asdaq, Syed Mohammed Basheeruddin Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol(®) Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study |
title | Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol(®) Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study |
title_full | Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol(®) Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study |
title_fullStr | Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol(®) Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study |
title_full_unstemmed | Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol(®) Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study |
title_short | Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol(®) Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study |
title_sort | preparation of terbinafin-encapsulated solid lipid nanoparticles containing antifungal carbopol(®) hydrogel with improved efficacy: in vitro, ex vivo and in vivo study |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9320640/ https://www.ncbi.nlm.nih.gov/pubmed/35890289 http://dx.doi.org/10.3390/pharmaceutics14071393 |
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