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Ternary cyclodextrin systems of terbinafine hydrochloride inclusion complexes: Solventless preparation, solid-state, and in vitro characterization
Cyclodextrins (CD) are used extensively in the pharmaceutical industry to improve the water solubility and bioavailability of drugs. Preparing ternary systems by applying a third component can enhance these beneficial effects. The complexation methods of these ternary systems are the same as those o...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10663756/ https://www.ncbi.nlm.nih.gov/pubmed/38027871 http://dx.doi.org/10.1016/j.heliyon.2023.e21416 |
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author | Kondoros, Balázs Attila Kókai, Dávid Burián, Katalin Sorrenti, Milena Catenacci, Laura Csóka, Ildikó Ambrus, Rita |
author_facet | Kondoros, Balázs Attila Kókai, Dávid Burián, Katalin Sorrenti, Milena Catenacci, Laura Csóka, Ildikó Ambrus, Rita |
author_sort | Kondoros, Balázs Attila |
collection | PubMed |
description | Cyclodextrins (CD) are used extensively in the pharmaceutical industry to improve the water solubility and bioavailability of drugs. Preparing ternary systems by applying a third component can enhance these beneficial effects. The complexation methods of these ternary systems are the same as those of two-component complexes. These methods are solvent (co-evaporation, co-precipitation, etc.) or solventless “green” techniques (co-grinding, microwave irradiation, etc.). Using solvent-free methods is considered to be an economically and environmentally desirable technology. This study aimed to prepare ternary systems by the co-grinding method and evaluate the effect of a third component by comparing it to products obtained by solvent methods, binary systems, and marketed products. For that, we used terbinafine hydrochloride as a model drug, sulfobutyl-ether-beta-cyclodextrin as a complexation agent and 5 or 15 w/w% of polyvinylpyrrolidone K-90 (PVP) or hydroxypropyl methylcellulose (HPMC) as auxiliary components. Physicochemical evaluation (X-Ray Diffractometry, Differential Scanning Calorimetry, Thermogravimetry) showed that new solid phases were formed, while Scanning Electron Microscopy was performed to study morphological aspects of the products. Fourier transform infrared spectroscopic measurements suggested different intermolecular interactions depending on the type of polymer. In vitro dissolution studies showed beneficial effects of CD and further improvement with the applied polymers. Products showed less cell toxicity with one exception. Both polymers enhanced the physicochemical and in vitro properties, suggesting a greater bioavailability of the model drug. However, the percentage of polymers applied did not appear to be an influencing factor for these properties. |
format | Online Article Text |
id | pubmed-10663756 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-106637562023-10-21 Ternary cyclodextrin systems of terbinafine hydrochloride inclusion complexes: Solventless preparation, solid-state, and in vitro characterization Kondoros, Balázs Attila Kókai, Dávid Burián, Katalin Sorrenti, Milena Catenacci, Laura Csóka, Ildikó Ambrus, Rita Heliyon Research Article Cyclodextrins (CD) are used extensively in the pharmaceutical industry to improve the water solubility and bioavailability of drugs. Preparing ternary systems by applying a third component can enhance these beneficial effects. The complexation methods of these ternary systems are the same as those of two-component complexes. These methods are solvent (co-evaporation, co-precipitation, etc.) or solventless “green” techniques (co-grinding, microwave irradiation, etc.). Using solvent-free methods is considered to be an economically and environmentally desirable technology. This study aimed to prepare ternary systems by the co-grinding method and evaluate the effect of a third component by comparing it to products obtained by solvent methods, binary systems, and marketed products. For that, we used terbinafine hydrochloride as a model drug, sulfobutyl-ether-beta-cyclodextrin as a complexation agent and 5 or 15 w/w% of polyvinylpyrrolidone K-90 (PVP) or hydroxypropyl methylcellulose (HPMC) as auxiliary components. Physicochemical evaluation (X-Ray Diffractometry, Differential Scanning Calorimetry, Thermogravimetry) showed that new solid phases were formed, while Scanning Electron Microscopy was performed to study morphological aspects of the products. Fourier transform infrared spectroscopic measurements suggested different intermolecular interactions depending on the type of polymer. In vitro dissolution studies showed beneficial effects of CD and further improvement with the applied polymers. Products showed less cell toxicity with one exception. Both polymers enhanced the physicochemical and in vitro properties, suggesting a greater bioavailability of the model drug. However, the percentage of polymers applied did not appear to be an influencing factor for these properties. Elsevier 2023-10-21 /pmc/articles/PMC10663756/ /pubmed/38027871 http://dx.doi.org/10.1016/j.heliyon.2023.e21416 Text en © 2023 The Authors https://creativecommons.org/licenses/by/4.0/This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Research Article Kondoros, Balázs Attila Kókai, Dávid Burián, Katalin Sorrenti, Milena Catenacci, Laura Csóka, Ildikó Ambrus, Rita Ternary cyclodextrin systems of terbinafine hydrochloride inclusion complexes: Solventless preparation, solid-state, and in vitro characterization |
title | Ternary cyclodextrin systems of terbinafine hydrochloride inclusion complexes: Solventless preparation, solid-state, and in vitro characterization |
title_full | Ternary cyclodextrin systems of terbinafine hydrochloride inclusion complexes: Solventless preparation, solid-state, and in vitro characterization |
title_fullStr | Ternary cyclodextrin systems of terbinafine hydrochloride inclusion complexes: Solventless preparation, solid-state, and in vitro characterization |
title_full_unstemmed | Ternary cyclodextrin systems of terbinafine hydrochloride inclusion complexes: Solventless preparation, solid-state, and in vitro characterization |
title_short | Ternary cyclodextrin systems of terbinafine hydrochloride inclusion complexes: Solventless preparation, solid-state, and in vitro characterization |
title_sort | ternary cyclodextrin systems of terbinafine hydrochloride inclusion complexes: solventless preparation, solid-state, and in vitro characterization |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10663756/ https://www.ncbi.nlm.nih.gov/pubmed/38027871 http://dx.doi.org/10.1016/j.heliyon.2023.e21416 |
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