Polymer-Antimicrobial Peptide Constructs with Tailored Drug-Release Behavior Article Swipe
Robert Pola
,
Matěj Vícha
,
Jiří Trousil
,
Eliška Grosmanová
,
Michal Pechar
,
Anna Rumlerová
,
Martin Studenovský
,
Emilie Kučerová
,
Pavel Ulbrich
,
Barbora Vokatá
,
Tomáš Etrych
·
YOU?
·
· 2023
· Open Access
·
· DOI: https://doi.org/10.3390/pharmaceutics15020406
YOU?
·
· 2023
· Open Access
·
· DOI: https://doi.org/10.3390/pharmaceutics15020406
Microbial resistance is one of the main problems of modern medicine. Recently, antimicrobial peptides have been recognized as a novel approach to overcome the microbial resistance issue, nevertheless, their low stability, toxicity, and potential immunogenic response in biological systems have limited their clinical application. Herein, we present the design, synthesis, and preliminary biological evaluation of polymer-antibacterial peptide constructs. The antimicrobial GKWMKLLKKILK-NH2 oligopeptide (PEP) derived from halictine, honey bee venom, was bound to a polymer carrier via various biodegradable spacers employing the pH-sensitive or enzymatically-driven release and reactivation of the PEP’s antimicrobial activity. The antibacterial properties of the polymer-PEP constructs were assessed by a determination of the minimum inhibitory concentrations, followed by fluorescence and transmission electron microscopy. The PEP exerted antibacterial activity against both, gram-positive and negative bacteria, via disruption of the bacterial cell wall mechanism. Importantly, PEP partly retained its antibacterial efficacy against Staphylococcus epidermidis, Escherichia coli, and Acinetobacter baumanii even though it was bound to the polymer carrier. Indeed, to observe antibacterial activity similar to the free PEP, the peptide has to be released from the polymer carrier in response to a pH decrease. Enzymatically-driven release and reactivation of the PEP antimicrobial activity were recognized as less effective when compared to the pH-sensitive release of PEP.
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Metadata
- Type
- article
- Language
- en
- Landing Page
- https://doi.org/10.3390/pharmaceutics15020406
- https://www.mdpi.com/1999-4923/15/2/406/pdf?version=1675331714
- OA Status
- gold
- Cited By
- 11
- References
- 32
- Related Works
- 10
- OpenAlex ID
- https://openalex.org/W4318052980
All OpenAlex metadata
Raw OpenAlex JSON
- OpenAlex ID
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https://openalex.org/W4318052980Canonical identifier for this work in OpenAlex
- DOI
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https://doi.org/10.3390/pharmaceutics15020406Digital Object Identifier
- Title
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Polymer-Antimicrobial Peptide Constructs with Tailored Drug-Release BehaviorWork title
- Type
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articleOpenAlex work type
- Language
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enPrimary language
- Publication year
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2023Year of publication
- Publication date
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2023-01-25Full publication date if available
- Authors
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Robert Pola, Matěj Vícha, Jiří Trousil, Eliška Grosmanová, Michal Pechar, Anna Rumlerová, Martin Studenovský, Emilie Kučerová, Pavel Ulbrich, Barbora Vokatá, Tomáš EtrychList of authors in order
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https://doi.org/10.3390/pharmaceutics15020406Publisher landing page
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https://www.mdpi.com/1999-4923/15/2/406/pdf?version=1675331714Direct link to full text PDF
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YesWhether a free full text is available
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goldOpen access status per OpenAlex
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https://www.mdpi.com/1999-4923/15/2/406/pdf?version=1675331714Direct OA link when available
- Concepts
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Antimicrobial, Drug, Peptide, Antimicrobial drug, Polymer, Chemistry, Nanotechnology, Pharmacology, Materials science, Medicine, Biochemistry, Organic chemistryTop concepts (fields/topics) attached by OpenAlex
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11Total citation count in OpenAlex
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2025: 7, 2024: 2, 2023: 2Per-year citation counts (last 5 years)
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32Number of works referenced by this work
- Related works (count)
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10Other works algorithmically related by OpenAlex
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