New Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes

Poor solubility of new antifungal of 1,2,4-triazole class (S-119)—a structural analogue of fluconazole in aqueous media was estimated. The solubility improvement using different excipients: biopolymers (PEGs, PVP), surfactants (Brij S20, pluronic F-127) and cyclodextrins (α-CD, β-CD, 2-HP-β-CD, 6-O-...

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Autores principales:	Tatyana V. Volkova, Olga R. Simonova, German L. Perlovich
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	solubility permeability solubilization micellization complexation Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/f10d35e7aaaf45ebab4fa33de8a0b1a5
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spelling	oai:doaj.org-article:f10d35e7aaaf45ebab4fa33de8a0b1a52021-11-25T18:41:16ZNew Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes10.3390/pharmaceutics131118651999-4923https://doaj.org/article/f10d35e7aaaf45ebab4fa33de8a0b1a52021-11-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1865https://doaj.org/toc/1999-4923Poor solubility of new antifungal of 1,2,4-triazole class (S-119)—a structural analogue of fluconazole in aqueous media was estimated. The solubility improvement using different excipients: biopolymers (PEGs, PVP), surfactants (Brij S20, pluronic F-127) and cyclodextrins (α-CD, β-CD, 2-HP-β-CD, 6-O-Maltosyl-β-CD) was assessed in buffer solutions pH 2.0 and pH 7.4. Additionally, 2-HP-β-CD and 6-O-Maltosyl-β-CD were proposed as promising solubilizers for S-119. According to the solubilization capacity and micelle/water partition coefficients in buffer pH 7.4 pluronic F-127 was shown to improve S-119 solubility better than Brij S20. Among biopolymers, the greatest increase in solubility was shown in PVP solutions (pH 7.4) at concentrations above 4 <i>w</i>/<i>v</i>%. Complex analysis of the driving forces of solubilization, micellization and complexation processes matched the solubility results and suggested pluronic F-127 and 6-O-Maltosyl-β-CD as the most effective solubilizing agents for S-119. The comparison of S-119 diffusion through the cellulose membrane and lipophilic PermeaPad barrier revealed a considerable effect of the lipid layer on the decrease in the permeability coefficient. According to the PermeaPad, S-119 was classified as a highly permeated substance. The addition of 1.5 <i>w</i>/<i>v</i>% CDs in donor solution moves it to low-medium permeability class.Tatyana V. VolkovaOlga R. SimonovaGerman L. PerlovichMDPI AGarticlesolubilitypermeabilitysolubilizationmicellizationcomplexationPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1865, p 1865 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	solubility permeability solubilization micellization complexation Pharmacy and materia medica RS1-441
spellingShingle	solubility permeability solubilization micellization complexation Pharmacy and materia medica RS1-441 Tatyana V. Volkova Olga R. Simonova German L. Perlovich New Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes
description	Poor solubility of new antifungal of 1,2,4-triazole class (S-119)—a structural analogue of fluconazole in aqueous media was estimated. The solubility improvement using different excipients: biopolymers (PEGs, PVP), surfactants (Brij S20, pluronic F-127) and cyclodextrins (α-CD, β-CD, 2-HP-β-CD, 6-O-Maltosyl-β-CD) was assessed in buffer solutions pH 2.0 and pH 7.4. Additionally, 2-HP-β-CD and 6-O-Maltosyl-β-CD were proposed as promising solubilizers for S-119. According to the solubilization capacity and micelle/water partition coefficients in buffer pH 7.4 pluronic F-127 was shown to improve S-119 solubility better than Brij S20. Among biopolymers, the greatest increase in solubility was shown in PVP solutions (pH 7.4) at concentrations above 4 <i>w</i>/<i>v</i>%. Complex analysis of the driving forces of solubilization, micellization and complexation processes matched the solubility results and suggested pluronic F-127 and 6-O-Maltosyl-β-CD as the most effective solubilizing agents for S-119. The comparison of S-119 diffusion through the cellulose membrane and lipophilic PermeaPad barrier revealed a considerable effect of the lipid layer on the decrease in the permeability coefficient. According to the PermeaPad, S-119 was classified as a highly permeated substance. The addition of 1.5 <i>w</i>/<i>v</i>% CDs in donor solution moves it to low-medium permeability class.
format	article
author	Tatyana V. Volkova Olga R. Simonova German L. Perlovich
author_facet	Tatyana V. Volkova Olga R. Simonova German L. Perlovich
author_sort	Tatyana V. Volkova
title	New Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes
title_short	New Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes
title_full	New Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes
title_fullStr	New Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes
title_full_unstemmed	New Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes
title_sort	new antifungal compound: impact of cosolvency, micellization and complexation on solubility and permeability processes
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/f10d35e7aaaf45ebab4fa33de8a0b1a5
work_keys_str_mv	AT tatyanavvolkova newantifungalcompoundimpactofcosolvencymicellizationandcomplexationonsolubilityandpermeabilityprocesses AT olgarsimonova newantifungalcompoundimpactofcosolvencymicellizationandcomplexationonsolubilityandpermeabilityprocesses AT germanlperlovich newantifungalcompoundimpactofcosolvencymicellizationandcomplexationonsolubilityandpermeabilityprocesses
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New Antifungal Compound: Impact of Cosolvency, Micellization and Complexation on Solubility and Permeability Processes

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