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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....

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
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.
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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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