Cargando…
Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity
The present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation...
Autores principales: | , , , , , , , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8872403/ https://www.ncbi.nlm.nih.gov/pubmed/35200513 http://dx.doi.org/10.3390/gels8020133 |
_version_ | 1784657230757363712 |
---|---|
author | Zafar, Ameeduzzafar Imam, Syed Sarim Alruwaili, Nabil K. Yasir, Mohd Alsaidan, Omar Awad Alshehri, Sultan Ghoneim, Mohammed M. Khalid, Mohammad Alquraini, Ali Alharthi, Salman S. |
author_facet | Zafar, Ameeduzzafar Imam, Syed Sarim Alruwaili, Nabil K. Yasir, Mohd Alsaidan, Omar Awad Alshehri, Sultan Ghoneim, Mohammed M. Khalid, Mohammad Alquraini, Ali Alharthi, Salman S. |
author_sort | Zafar, Ameeduzzafar |
collection | PubMed |
description | The present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation across the skin. BSs were prepared by the thin-film hydration method and optimized by the Box–Behnken design (BBD) using lipid (A), span 60 (B), and sodium deoxycholate (C) as independent variables. The selected formulation (BN-BSo) was converted into the gel using Carbopol 940 as a gelling agent. The prepared optimized gel (BN-BS-og) was further evaluated for the gel characterization, drug release, drug permeation, irritation, and anti-fungal study. The optimized bilosomes (BN-BSo) showed a mean vesicle size of 215 ± 6.5 nm and an entrapment efficiency of 89.2 ± 1.5%. The DSC study showed that BN was completely encapsulated in the BS lipid matrix. BN-BSog showed good viscosity, consistency, spreadability, and pH. A significantly (p < 0.05) high release (81.09 ± 4.01%) was achieved from BN-BSo compared to BN-BSog (65.85 ± 4.87%) and pure BN (17.54 ± 1.37 %). The permeation study results revealed that BN-BSo, BN-BSog, and pure BN exhibited 56.2 ± 2.7%, 39.2 ± 2.9%, and 16.6 ± 2.3%. The enhancement ratio of permeation flux was found to be 1.4-fold and 3.4-fold for the BN-BS-og and pure BN dispersion. The HET-CAM study showed that BN-BSog was found to be nonirritant as the score was found within the limit. The antifungal study revealed a significant (p < 0.05) enhanced antifungal activity against C. albicans and A. niger. The findings of the study revealed that BS is an important drug delivery system for transdermal delivery. |
format | Online Article Text |
id | pubmed-8872403 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-88724032022-02-25 Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity Zafar, Ameeduzzafar Imam, Syed Sarim Alruwaili, Nabil K. Yasir, Mohd Alsaidan, Omar Awad Alshehri, Sultan Ghoneim, Mohammed M. Khalid, Mohammad Alquraini, Ali Alharthi, Salman S. Gels Article The present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation across the skin. BSs were prepared by the thin-film hydration method and optimized by the Box–Behnken design (BBD) using lipid (A), span 60 (B), and sodium deoxycholate (C) as independent variables. The selected formulation (BN-BSo) was converted into the gel using Carbopol 940 as a gelling agent. The prepared optimized gel (BN-BS-og) was further evaluated for the gel characterization, drug release, drug permeation, irritation, and anti-fungal study. The optimized bilosomes (BN-BSo) showed a mean vesicle size of 215 ± 6.5 nm and an entrapment efficiency of 89.2 ± 1.5%. The DSC study showed that BN was completely encapsulated in the BS lipid matrix. BN-BSog showed good viscosity, consistency, spreadability, and pH. A significantly (p < 0.05) high release (81.09 ± 4.01%) was achieved from BN-BSo compared to BN-BSog (65.85 ± 4.87%) and pure BN (17.54 ± 1.37 %). The permeation study results revealed that BN-BSo, BN-BSog, and pure BN exhibited 56.2 ± 2.7%, 39.2 ± 2.9%, and 16.6 ± 2.3%. The enhancement ratio of permeation flux was found to be 1.4-fold and 3.4-fold for the BN-BS-og and pure BN dispersion. The HET-CAM study showed that BN-BSog was found to be nonirritant as the score was found within the limit. The antifungal study revealed a significant (p < 0.05) enhanced antifungal activity against C. albicans and A. niger. The findings of the study revealed that BS is an important drug delivery system for transdermal delivery. MDPI 2022-02-18 /pmc/articles/PMC8872403/ /pubmed/35200513 http://dx.doi.org/10.3390/gels8020133 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 Zafar, Ameeduzzafar Imam, Syed Sarim Alruwaili, Nabil K. Yasir, Mohd Alsaidan, Omar Awad Alshehri, Sultan Ghoneim, Mohammed M. Khalid, Mohammad Alquraini, Ali Alharthi, Salman S. Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
title | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
title_full | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
title_fullStr | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
title_full_unstemmed | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
title_short | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
title_sort | formulation and evaluation of topical nano-lipid-based delivery of butenafine: in vitro characterization and antifungal activity |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8872403/ https://www.ncbi.nlm.nih.gov/pubmed/35200513 http://dx.doi.org/10.3390/gels8020133 |
work_keys_str_mv | AT zafarameeduzzafar formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity AT imamsyedsarim formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity AT alruwailinabilk formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity AT yasirmohd formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity AT alsaidanomarawad formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity AT alshehrisultan formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity AT ghoneimmohammedm formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity AT khalidmohammad formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity AT alqurainiali formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity AT alharthisalmans formulationandevaluationoftopicalnanolipidbaseddeliveryofbutenafineinvitrocharacterizationandantifungalactivity |