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Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application—Development, Initial Assessment, and Pilot Release Studies

Vaginal candidiasis (VC) is an emerging global hardly treated health issue affecting millions of women worldwide. In this study, the nanoemulsion consisting of clotrimazole (CLT), rapeseed oil, Pluronic F-68, Span 80, PEG 200, and lactic acid was prepared using high-speed and high-pressure homogeniz...

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Autores principales: Smoleński, Michał, Muschert, Susanne, Haznar-Garbacz, Dorota, Małolepsza-Jarmołowska, Katarzyna
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10224398/
https://www.ncbi.nlm.nih.gov/pubmed/37242679
http://dx.doi.org/10.3390/pharmaceutics15051437
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author Smoleński, Michał
Muschert, Susanne
Haznar-Garbacz, Dorota
Małolepsza-Jarmołowska, Katarzyna
author_facet Smoleński, Michał
Muschert, Susanne
Haznar-Garbacz, Dorota
Małolepsza-Jarmołowska, Katarzyna
author_sort Smoleński, Michał
collection PubMed
description Vaginal candidiasis (VC) is an emerging global hardly treated health issue affecting millions of women worldwide. In this study, the nanoemulsion consisting of clotrimazole (CLT), rapeseed oil, Pluronic F-68, Span 80, PEG 200, and lactic acid was prepared using high-speed and high-pressure homogenization. Yielded formulations were characterized by an average droplet size of 52–56 nm, homogenous size distribution by volume, and a polydispersity index (PDI) < 0.2. The osmolality of nanoemulsions (NEs) fulfilled the recommendations of the WHO advisory note. NEs were stable throughout 28 weeks of storage. The stationary and dynamic (USP apparatus IV) pilot study of the changes of free CLT over time for NEs, as well as market cream and CLT suspension as references, were conducted. Test results of the changes in the amount of free CLT released from the encapsulated form were not coherent; in the stationary method, NEs yielded up to 27% of the released CLT dose within 5 h, while in the USP apparatus IV method, NEs released up to 10% of the CLT dose. NEs are promising carriers for vaginal drug delivery in the treatment of VC; however, further development of the final dosage form and harmonized release or dissolution testing protocols are needed.
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spelling pubmed-102243982023-05-28 Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application—Development, Initial Assessment, and Pilot Release Studies Smoleński, Michał Muschert, Susanne Haznar-Garbacz, Dorota Małolepsza-Jarmołowska, Katarzyna Pharmaceutics Article Vaginal candidiasis (VC) is an emerging global hardly treated health issue affecting millions of women worldwide. In this study, the nanoemulsion consisting of clotrimazole (CLT), rapeseed oil, Pluronic F-68, Span 80, PEG 200, and lactic acid was prepared using high-speed and high-pressure homogenization. Yielded formulations were characterized by an average droplet size of 52–56 nm, homogenous size distribution by volume, and a polydispersity index (PDI) < 0.2. The osmolality of nanoemulsions (NEs) fulfilled the recommendations of the WHO advisory note. NEs were stable throughout 28 weeks of storage. The stationary and dynamic (USP apparatus IV) pilot study of the changes of free CLT over time for NEs, as well as market cream and CLT suspension as references, were conducted. Test results of the changes in the amount of free CLT released from the encapsulated form were not coherent; in the stationary method, NEs yielded up to 27% of the released CLT dose within 5 h, while in the USP apparatus IV method, NEs released up to 10% of the CLT dose. NEs are promising carriers for vaginal drug delivery in the treatment of VC; however, further development of the final dosage form and harmonized release or dissolution testing protocols are needed. MDPI 2023-05-08 /pmc/articles/PMC10224398/ /pubmed/37242679 http://dx.doi.org/10.3390/pharmaceutics15051437 Text en © 2023 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
Smoleński, Michał
Muschert, Susanne
Haznar-Garbacz, Dorota
Małolepsza-Jarmołowska, Katarzyna
Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application—Development, Initial Assessment, and Pilot Release Studies
title Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application—Development, Initial Assessment, and Pilot Release Studies
title_full Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application—Development, Initial Assessment, and Pilot Release Studies
title_fullStr Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application—Development, Initial Assessment, and Pilot Release Studies
title_full_unstemmed Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application—Development, Initial Assessment, and Pilot Release Studies
title_short Nanoemulsion Loaded with Clotrimazole Based on Rapeseed Oil for Potential Vaginal Application—Development, Initial Assessment, and Pilot Release Studies
title_sort nanoemulsion loaded with clotrimazole based on rapeseed oil for potential vaginal application—development, initial assessment, and pilot release studies
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10224398/
https://www.ncbi.nlm.nih.gov/pubmed/37242679
http://dx.doi.org/10.3390/pharmaceutics15051437
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