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Interaction between Different Pharmaceutical Excipients in Liquid Dosage Forms—Assessment of Cytotoxicity and Antimicrobial Activity

Nowadays, the safety of parabens as pharmaceutical preservatives is debated. Recent studies investigated their interference with the oestrogen receptors, nevertheless their carcinogenic activity was also proved. That was the reason why the re-evaluation of the biocompatibility and antimicrobial acti...

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Autores principales: Nemes, Dániel, Kovács, Renátó, Nagy, Fruzsina, Mező, Mirtill, Poczok, Nikolett, Ujhelyi, Zoltán, Pető, Ágota, Fehér, Pálma, Fenyvesi, Ferenc, Váradi, Judit, Vecsernyés, Miklós, Bácskay, Ildikó
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6100184/
https://www.ncbi.nlm.nih.gov/pubmed/30041418
http://dx.doi.org/10.3390/molecules23071827
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author Nemes, Dániel
Kovács, Renátó
Nagy, Fruzsina
Mező, Mirtill
Poczok, Nikolett
Ujhelyi, Zoltán
Pető, Ágota
Fehér, Pálma
Fenyvesi, Ferenc
Váradi, Judit
Vecsernyés, Miklós
Bácskay, Ildikó
author_facet Nemes, Dániel
Kovács, Renátó
Nagy, Fruzsina
Mező, Mirtill
Poczok, Nikolett
Ujhelyi, Zoltán
Pető, Ágota
Fehér, Pálma
Fenyvesi, Ferenc
Váradi, Judit
Vecsernyés, Miklós
Bácskay, Ildikó
author_sort Nemes, Dániel
collection PubMed
description Nowadays, the safety of parabens as pharmaceutical preservatives is debated. Recent studies investigated their interference with the oestrogen receptors, nevertheless their carcinogenic activity was also proved. That was the reason why the re-evaluation of the biocompatibility and antimicrobial activity of parabens is required using modern investigation methods. We aimed to test the cytotoxic, antifungal and antibacterial effect of parabens on Caco-2 cells, C. albicans, C. parapsilosis, C. glabrata, E. coli, P. aeruginosa and S. aureus. Two complex systems (glycerol—Polysorbate 20; ethanol—Capryol PGMC™) were formulated to study—with the MTT-assay and microdilution method, respectively—how other excipients may modify the biocompatibility and antimicrobial effect of parabens. In the case of cytotoxicity, the toxicity of these two systems was highly influenced by co-solvents and surfactants. The fungi and bacteria had significantly different resistance in the formulations and in some cases the excipients could highly modify the effectiveness of parabens both in an agonistic and in a counteractive way. These results indicate that with appropriate selection, non-preservative excipients can contribute to the antimicrobial safety of the products, thus they may decrease the required preservative concentration.
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spelling pubmed-61001842018-11-13 Interaction between Different Pharmaceutical Excipients in Liquid Dosage Forms—Assessment of Cytotoxicity and Antimicrobial Activity Nemes, Dániel Kovács, Renátó Nagy, Fruzsina Mező, Mirtill Poczok, Nikolett Ujhelyi, Zoltán Pető, Ágota Fehér, Pálma Fenyvesi, Ferenc Váradi, Judit Vecsernyés, Miklós Bácskay, Ildikó Molecules Article Nowadays, the safety of parabens as pharmaceutical preservatives is debated. Recent studies investigated their interference with the oestrogen receptors, nevertheless their carcinogenic activity was also proved. That was the reason why the re-evaluation of the biocompatibility and antimicrobial activity of parabens is required using modern investigation methods. We aimed to test the cytotoxic, antifungal and antibacterial effect of parabens on Caco-2 cells, C. albicans, C. parapsilosis, C. glabrata, E. coli, P. aeruginosa and S. aureus. Two complex systems (glycerol—Polysorbate 20; ethanol—Capryol PGMC™) were formulated to study—with the MTT-assay and microdilution method, respectively—how other excipients may modify the biocompatibility and antimicrobial effect of parabens. In the case of cytotoxicity, the toxicity of these two systems was highly influenced by co-solvents and surfactants. The fungi and bacteria had significantly different resistance in the formulations and in some cases the excipients could highly modify the effectiveness of parabens both in an agonistic and in a counteractive way. These results indicate that with appropriate selection, non-preservative excipients can contribute to the antimicrobial safety of the products, thus they may decrease the required preservative concentration. MDPI 2018-07-23 /pmc/articles/PMC6100184/ /pubmed/30041418 http://dx.doi.org/10.3390/molecules23071827 Text en © 2018 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Nemes, Dániel
Kovács, Renátó
Nagy, Fruzsina
Mező, Mirtill
Poczok, Nikolett
Ujhelyi, Zoltán
Pető, Ágota
Fehér, Pálma
Fenyvesi, Ferenc
Váradi, Judit
Vecsernyés, Miklós
Bácskay, Ildikó
Interaction between Different Pharmaceutical Excipients in Liquid Dosage Forms—Assessment of Cytotoxicity and Antimicrobial Activity
title Interaction between Different Pharmaceutical Excipients in Liquid Dosage Forms—Assessment of Cytotoxicity and Antimicrobial Activity
title_full Interaction between Different Pharmaceutical Excipients in Liquid Dosage Forms—Assessment of Cytotoxicity and Antimicrobial Activity
title_fullStr Interaction between Different Pharmaceutical Excipients in Liquid Dosage Forms—Assessment of Cytotoxicity and Antimicrobial Activity
title_full_unstemmed Interaction between Different Pharmaceutical Excipients in Liquid Dosage Forms—Assessment of Cytotoxicity and Antimicrobial Activity
title_short Interaction between Different Pharmaceutical Excipients in Liquid Dosage Forms—Assessment of Cytotoxicity and Antimicrobial Activity
title_sort interaction between different pharmaceutical excipients in liquid dosage forms—assessment of cytotoxicity and antimicrobial activity
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6100184/
https://www.ncbi.nlm.nih.gov/pubmed/30041418
http://dx.doi.org/10.3390/molecules23071827
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