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Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against Candida albicans

Luliconazole is a new topical imidazole antifungal drug for the treatment of skin infections. It has low solubility and poor skin penetration which limits its therapeutic applications. In order to improve its therapeutic efficacy, spanlastics nanoformulation was developed and optimized using a combi...

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Autores principales: Alhakamy, Nabil A., Al-Rabia, Mohammed W., Md, Shadab, Sirwi, Alaa, Khayat, Selwan Saud, AlOtaibi, Sahar Saad, Hakami, Raghad Abkar, Al Sadoun, Hadeel, Eldakhakhny, Basmah Medhat, Abdulaal, Wesam H., Aldawsari, Hibah M., Badr-Eldin, Shaimaa M., Elfaky, Mahmoud A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8309172/
https://www.ncbi.nlm.nih.gov/pubmed/34203359
http://dx.doi.org/10.3390/pharmaceutics13070977
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author Alhakamy, Nabil A.
Al-Rabia, Mohammed W.
Md, Shadab
Sirwi, Alaa
Khayat, Selwan Saud
AlOtaibi, Sahar Saad
Hakami, Raghad Abkar
Al Sadoun, Hadeel
Eldakhakhny, Basmah Medhat
Abdulaal, Wesam H.
Aldawsari, Hibah M.
Badr-Eldin, Shaimaa M.
Elfaky, Mahmoud A.
author_facet Alhakamy, Nabil A.
Al-Rabia, Mohammed W.
Md, Shadab
Sirwi, Alaa
Khayat, Selwan Saud
AlOtaibi, Sahar Saad
Hakami, Raghad Abkar
Al Sadoun, Hadeel
Eldakhakhny, Basmah Medhat
Abdulaal, Wesam H.
Aldawsari, Hibah M.
Badr-Eldin, Shaimaa M.
Elfaky, Mahmoud A.
author_sort Alhakamy, Nabil A.
collection PubMed
description Luliconazole is a new topical imidazole antifungal drug for the treatment of skin infections. It has low solubility and poor skin penetration which limits its therapeutic applications. In order to improve its therapeutic efficacy, spanlastics nanoformulation was developed and optimized using a combined mixture-process variable design (CMPV). The optimized formulation was converted into a hydrogel formula to enhance skin penetration and increase the efficacy in experimental cutaneous Candida albicans infections in Swiss mice wounds. The optimized formulation was generated at percentages of Span and Tween of 48% and 52%, respectively, and a sonication time of 6.6 min. The software predicted that the proposed formulation would achieve a particle size of 50 nm with a desirability of 0.997. The entrapment of luliconazole within the spanlastics carrier showed significant (p < 0.0001) antifungal efficacy in the immunocompromised Candida-infected Swiss mice without causing any irritation, when compared to the luliconazole treated groups. The microscopic observation showed almost complete removal of the fungal colonies on the skin of the infected animals (0.2 ± 0.05 log CFU), whereas the control animals had 0.2 ± 0.05 log CFU. Therefore, luliconazole spanlastics could be an effective formulation with improved topical delivery for antifungal activity against C. albicans.
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spelling pubmed-83091722021-07-25 Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against Candida albicans Alhakamy, Nabil A. Al-Rabia, Mohammed W. Md, Shadab Sirwi, Alaa Khayat, Selwan Saud AlOtaibi, Sahar Saad Hakami, Raghad Abkar Al Sadoun, Hadeel Eldakhakhny, Basmah Medhat Abdulaal, Wesam H. Aldawsari, Hibah M. Badr-Eldin, Shaimaa M. Elfaky, Mahmoud A. Pharmaceutics Article Luliconazole is a new topical imidazole antifungal drug for the treatment of skin infections. It has low solubility and poor skin penetration which limits its therapeutic applications. In order to improve its therapeutic efficacy, spanlastics nanoformulation was developed and optimized using a combined mixture-process variable design (CMPV). The optimized formulation was converted into a hydrogel formula to enhance skin penetration and increase the efficacy in experimental cutaneous Candida albicans infections in Swiss mice wounds. The optimized formulation was generated at percentages of Span and Tween of 48% and 52%, respectively, and a sonication time of 6.6 min. The software predicted that the proposed formulation would achieve a particle size of 50 nm with a desirability of 0.997. The entrapment of luliconazole within the spanlastics carrier showed significant (p < 0.0001) antifungal efficacy in the immunocompromised Candida-infected Swiss mice without causing any irritation, when compared to the luliconazole treated groups. The microscopic observation showed almost complete removal of the fungal colonies on the skin of the infected animals (0.2 ± 0.05 log CFU), whereas the control animals had 0.2 ± 0.05 log CFU. Therefore, luliconazole spanlastics could be an effective formulation with improved topical delivery for antifungal activity against C. albicans. MDPI 2021-06-28 /pmc/articles/PMC8309172/ /pubmed/34203359 http://dx.doi.org/10.3390/pharmaceutics13070977 Text en © 2021 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
Alhakamy, Nabil A.
Al-Rabia, Mohammed W.
Md, Shadab
Sirwi, Alaa
Khayat, Selwan Saud
AlOtaibi, Sahar Saad
Hakami, Raghad Abkar
Al Sadoun, Hadeel
Eldakhakhny, Basmah Medhat
Abdulaal, Wesam H.
Aldawsari, Hibah M.
Badr-Eldin, Shaimaa M.
Elfaky, Mahmoud A.
Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against Candida albicans
title Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against Candida albicans
title_full Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against Candida albicans
title_fullStr Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against Candida albicans
title_full_unstemmed Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against Candida albicans
title_short Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against Candida albicans
title_sort development and optimization of luliconazole spanlastics to augment the antifungal activity against candida albicans
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8309172/
https://www.ncbi.nlm.nih.gov/pubmed/34203359
http://dx.doi.org/10.3390/pharmaceutics13070977
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