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Assessment of Antimicrobic, Antivirotic and Cytotoxic Potential of Alginate Beads Cross-Linked by Bivalent Ions for Vaginal Administration

Antimicrobial agent abuse poses a serious threat for future pharmacotherapy, including vaginal administration. The solution can be found in simple polymeric systems with inherent antimicrobial properties without the need to incorporate drugs, for instance alginate beads cross-linked by bivalent ions...

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Autores principales: Pavelková, Miroslava, Vysloužil, Jakub, Kubová, Kateřina, Pavloková, Sylvie, Molinková, Dobromila, Celer, Vladimír, Pechová, Alena, Mašek, Josef, Vetchý, David
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7910877/
https://www.ncbi.nlm.nih.gov/pubmed/33513747
http://dx.doi.org/10.3390/pharmaceutics13020165
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author Pavelková, Miroslava
Vysloužil, Jakub
Kubová, Kateřina
Pavloková, Sylvie
Molinková, Dobromila
Celer, Vladimír
Pechová, Alena
Mašek, Josef
Vetchý, David
author_facet Pavelková, Miroslava
Vysloužil, Jakub
Kubová, Kateřina
Pavloková, Sylvie
Molinková, Dobromila
Celer, Vladimír
Pechová, Alena
Mašek, Josef
Vetchý, David
author_sort Pavelková, Miroslava
collection PubMed
description Antimicrobial agent abuse poses a serious threat for future pharmacotherapy, including vaginal administration. The solution can be found in simple polymeric systems with inherent antimicrobial properties without the need to incorporate drugs, for instance alginate beads cross-linked by bivalent ions. The main goal of the presented study was to provide improvement on the well-documented cytotoxicity of Cu(2+) cross-linked alginate. Alginate beads were prepared by external ionotropic gelation by cross-linking with Cu(2+), Ca(2+) and Zn(2+) ions, separately and in mixtures. Morphological properties, swelling capacity, ion release and efficacy against the most common vaginal pathogens (C. albicans, E. coli, E. faecalis and virus strain—human herpesvirus type 1) were evaluated. The prepared particles (particle size 1455.68 ± 18.71–1756.31 ± 16.58 µm) had very good sphericity (0.86 ± 0.04–0.97 ± 0.06). In mixture samples, Cu(2+) hampered second ion loading, and was also released incompletely (18.75–44.8%) compared to the single ion Cu(2+) sample (71.4%). Efficacy against the selected pathogens was confirmed in almost all samples. Although anticipating otherwise, ion mixture samples did not show betterment over a Cu(2+) cross-linked sample in cytotoxicity–pathogen efficacy relation. However, the desired improvement was found in a single ion Zn(2+) sample whose minimal inhibition concentrations against the pathogens (0.6–6.12 mM) were close to, or in the same mathematical order as, its toxic concentration of 50 (1.891 mM). In summary, these findings combined with alginate’s biocompatibility and biodegradability give the combination solid potential in antimicrobial use.
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spelling pubmed-79108772021-02-28 Assessment of Antimicrobic, Antivirotic and Cytotoxic Potential of Alginate Beads Cross-Linked by Bivalent Ions for Vaginal Administration Pavelková, Miroslava Vysloužil, Jakub Kubová, Kateřina Pavloková, Sylvie Molinková, Dobromila Celer, Vladimír Pechová, Alena Mašek, Josef Vetchý, David Pharmaceutics Article Antimicrobial agent abuse poses a serious threat for future pharmacotherapy, including vaginal administration. The solution can be found in simple polymeric systems with inherent antimicrobial properties without the need to incorporate drugs, for instance alginate beads cross-linked by bivalent ions. The main goal of the presented study was to provide improvement on the well-documented cytotoxicity of Cu(2+) cross-linked alginate. Alginate beads were prepared by external ionotropic gelation by cross-linking with Cu(2+), Ca(2+) and Zn(2+) ions, separately and in mixtures. Morphological properties, swelling capacity, ion release and efficacy against the most common vaginal pathogens (C. albicans, E. coli, E. faecalis and virus strain—human herpesvirus type 1) were evaluated. The prepared particles (particle size 1455.68 ± 18.71–1756.31 ± 16.58 µm) had very good sphericity (0.86 ± 0.04–0.97 ± 0.06). In mixture samples, Cu(2+) hampered second ion loading, and was also released incompletely (18.75–44.8%) compared to the single ion Cu(2+) sample (71.4%). Efficacy against the selected pathogens was confirmed in almost all samples. Although anticipating otherwise, ion mixture samples did not show betterment over a Cu(2+) cross-linked sample in cytotoxicity–pathogen efficacy relation. However, the desired improvement was found in a single ion Zn(2+) sample whose minimal inhibition concentrations against the pathogens (0.6–6.12 mM) were close to, or in the same mathematical order as, its toxic concentration of 50 (1.891 mM). In summary, these findings combined with alginate’s biocompatibility and biodegradability give the combination solid potential in antimicrobial use. MDPI 2021-01-27 /pmc/articles/PMC7910877/ /pubmed/33513747 http://dx.doi.org/10.3390/pharmaceutics13020165 Text en © 2021 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
Pavelková, Miroslava
Vysloužil, Jakub
Kubová, Kateřina
Pavloková, Sylvie
Molinková, Dobromila
Celer, Vladimír
Pechová, Alena
Mašek, Josef
Vetchý, David
Assessment of Antimicrobic, Antivirotic and Cytotoxic Potential of Alginate Beads Cross-Linked by Bivalent Ions for Vaginal Administration
title Assessment of Antimicrobic, Antivirotic and Cytotoxic Potential of Alginate Beads Cross-Linked by Bivalent Ions for Vaginal Administration
title_full Assessment of Antimicrobic, Antivirotic and Cytotoxic Potential of Alginate Beads Cross-Linked by Bivalent Ions for Vaginal Administration
title_fullStr Assessment of Antimicrobic, Antivirotic and Cytotoxic Potential of Alginate Beads Cross-Linked by Bivalent Ions for Vaginal Administration
title_full_unstemmed Assessment of Antimicrobic, Antivirotic and Cytotoxic Potential of Alginate Beads Cross-Linked by Bivalent Ions for Vaginal Administration
title_short Assessment of Antimicrobic, Antivirotic and Cytotoxic Potential of Alginate Beads Cross-Linked by Bivalent Ions for Vaginal Administration
title_sort assessment of antimicrobic, antivirotic and cytotoxic potential of alginate beads cross-linked by bivalent ions for vaginal administration
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7910877/
https://www.ncbi.nlm.nih.gov/pubmed/33513747
http://dx.doi.org/10.3390/pharmaceutics13020165
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