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Pharmaceutics
Special Issues
Antimicrobial Peptide-Polymer Conjugates
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Antimicrobial Peptide-Polymer Conjugates

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Biologics and Biosimilars".

Deadline for manuscript submissions: closed (30 September 2021) | Viewed by 21121

Special Issue Editors

Dr. Claudia Monteiro

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Guest Editor
Instituto de Investigação e Inovação em Saúde, Universidade do Porto, 4050-313 Porto, Portugal
Interests: antimicrobial peptides; antimicrobial compounds; biofilms; biomaterials
Special Issues, Collections and Topics in MDPI journals
Dr. Viorica Patrulea

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Guest Editor
Department of Engineering Science, Institute of Biomedical Engineering, University of Oxford, Old Road Campus Research Building, Headington, Oxford OX3 7DQ, UK
Interests: wound healing; chronic wounds; hard-to-heal wounds; antimicrobial resistance; wound infection; antimicrobial agents; nanocomplexes; biopolymers
Special Issues, Collections and Topics in MDPI journals
Dr. Martijn Riool

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Guest Editor
Medical Microbiology, Amsterdam UMC (location AMC), 1105 AZ Amsterdam, The Netherlands
Interests: biomaterial-associated infections; antimicrobial peptides (AMPs); biofilms; strategies for infection prevention and control; antimicrobial resistance; antimicrobial coatings; Staphylococcus aureus; Candida albicans

Special Issue Information

Dear Colleagues,

The rapid spread of antibiotic-resistant bacteria is a worrying public health problem, and the World Health Organization (WHO) considers it to be one of the greatest threats to global health.

Antimicrobial peptides (AMPs) have been drawing attention as a very promising alternative to conventional antibiotics. AMPs have a broad spectrum of action and are able to break down bacterial membranes with a very low propensity to induce resistance.

Novel AMP delivery systems, namely polymeric systems, are currently being developed to improve the bioactivity of AMPs while reducing possible side effects.

This Special Issue aims to cover different aspects of the development of AMP–polymer conjugates designed to control AMP delivery in different forms, namely nano and microparticles, films/coatings, scaffolds, hydrogels, fibers, and printed systems. Papers describing the design, preparation, and physico-chemical and biological characterization of these systems are most welcome.

Authors are invited to submit original research articles and reviews in this important and exciting research field.

Dr. Claudia Monteiro
Dr. Viorica Patrulea
Dr. Martijn Riool
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • AMP delivery systems
  • polymers
  • biomaterials
  • nanoparticles
  • fibers
  • scaffolds
  • films/coatings
  • hydrogels
  • printed systems
  • antibacterial/antimicrobial activity
  • efficacy and safety

Published Papers (6 papers)

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Editorial

Jump to: Research, Review

3 pages, 203 KiB  
Editorial
Antimicrobial Peptide–Polymer Conjugates
by Martijn Riool, Viorica Patrulea and Cláudia Monteiro
Pharmaceutics 2022, 14(10), 2171; https://doi.org/10.3390/pharmaceutics14102171 - 12 Oct 2022
Cited by 3 | Viewed by 1202
Abstract
The global health threat imposed by the fast spread of antibiotic-resistant bacteria is directing research not only towards the discovery of new antibacterial molecules but also to the repurposing of old drugs, while improving their efficiency and safety [...] Full article
(This article belongs to the Special Issue Antimicrobial Peptide-Polymer Conjugates)

Research

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16 pages, 5079 KiB  
Article
Antibacterial Activity of T22, a Specific Peptidic Ligand of the Tumoral Marker CXCR4
by Naroa Serna, José Vicente Carratalá, Oscar Conchillo-Solé, Carlos Martínez-Torró, Ugutz Unzueta, Ramón Mangues, Neus Ferrer-Miralles, Xavier Daura, Esther Vázquez and Antonio Villaverde
Pharmaceutics 2021, 13(11), 1922; https://doi.org/10.3390/pharmaceutics13111922 - 13 Nov 2021
Cited by 5 | Viewed by 2568
Abstract
CXCR4 is a cytokine receptor used by HIV during cell attachment and infection. Overexpressed in the cancer stem cells of more than 20 human neoplasias, CXCR4 is a convenient antitumoral drug target. T22 is a polyphemusin-derived peptide and an effective CXCR4 ligand. Its [...] Read more.
CXCR4 is a cytokine receptor used by HIV during cell attachment and infection. Overexpressed in the cancer stem cells of more than 20 human neoplasias, CXCR4 is a convenient antitumoral drug target. T22 is a polyphemusin-derived peptide and an effective CXCR4 ligand. Its highly selective CXCR4 binding can be exploited as an agent for the cell-targeted delivery and internalization of associated antitumor drugs. Sharing chemical and structural traits with antimicrobial peptides (AMPs), the capability of T22 as an antibacterial agent remains unexplored. Here, we have detected T22-associated antimicrobial activity and biofilm formation inhibition over Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, in a spectrum broader than the reference AMP GWH1. In contrast to GWH1, T22 shows neither cytotoxicity over mammalian cells nor hemolytic activity and is active when displayed on protein-only nanoparticles through genetic fusion. Under the pushing need for novel antimicrobial agents, the discovery of T22 as an AMP is particularly appealing, not only as its mere addition to the expanding catalogue of antibacterial drugs. The recognized clinical uses of T22 might allow its combined and multivalent application in complex clinical conditions, such as colorectal cancer, that might benefit from the synchronous destruction of cancer stem cells and local bacterial biofilms. Full article
(This article belongs to the Special Issue Antimicrobial Peptide-Polymer Conjugates)
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Review

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20 pages, 4378 KiB  
Review
Polymer Conjugates of Antimicrobial Peptides (AMPs) with d-Amino Acids (d-aa): State of the Art and Future Opportunities
by Ottavia Bellotto, Sabrina Semeraro, Antonella Bandiera, Federica Tramer, Nicola Pavan and Silvia Marchesan
Pharmaceutics 2022, 14(2), 446; https://doi.org/10.3390/pharmaceutics14020446 - 19 Feb 2022
Cited by 20 | Viewed by 4925
Abstract
In recent years, antimicrobial peptides (AMPs) have enjoyed a renaissance, as the world is currently facing an emergency in terms of severe infections that evade antibiotics’ treatment. This is due to the increasing emergence and spread of resistance mechanisms. Covalent conjugation with polymers [...] Read more.
In recent years, antimicrobial peptides (AMPs) have enjoyed a renaissance, as the world is currently facing an emergency in terms of severe infections that evade antibiotics’ treatment. This is due to the increasing emergence and spread of resistance mechanisms. Covalent conjugation with polymers is an interesting strategy to modulate the pharmacokinetic profile of AMPs and enhance their biocompatibility profile. It can also be an effective approach to develop active coatings for medical implants and devices, and to avoid biofilm formation on their surface. In this concise review, we focus on the last 5 years’ progress in this area, pertaining in particular to AMPs that contain d-amino acids, as well as their role, and the advantages that may arise from their introduction into AMPs. Full article
(This article belongs to the Special Issue Antimicrobial Peptide-Polymer Conjugates)
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25 pages, 2608 KiB  
Review
Antimicrobial Peptides in the Battle against Orthopedic Implant-Related Infections: A Review
by Bruna Costa, Guillermo Martínez-de-Tejada, Paula A. C. Gomes, M. Cristina L. Martins and Fabíola Costa
Pharmaceutics 2021, 13(11), 1918; https://doi.org/10.3390/pharmaceutics13111918 - 12 Nov 2021
Cited by 20 | Viewed by 3452
Abstract
Prevention of orthopedic implant-related infections is a major medical challenge, particularly due to the involvement of biofilm-encased and multidrug-resistant bacteria. Current therapies, based on antibiotic administration, have proven to be insufficient, and infection prevalence may rise due to the dissemination of antibiotic resistance. [...] Read more.
Prevention of orthopedic implant-related infections is a major medical challenge, particularly due to the involvement of biofilm-encased and multidrug-resistant bacteria. Current therapies, based on antibiotic administration, have proven to be insufficient, and infection prevalence may rise due to the dissemination of antibiotic resistance. Antimicrobial peptides (AMPs) have attracted attention as promising substitutes of conventional antibiotics, owing to their broad-spectrum of activity, high efficacy at very low concentrations, and, importantly, low propensity for inducing resistance. The aim of this review is to offer an updated perspective of the development of AMPs-based preventive strategies for orthopedic and dental implant-related infections. In this regard, two major research strategies are herein addressed, namely (i) AMP-releasing systems from titanium-modified surfaces and from bone cements or beads; and (ii) AMP immobilization strategies used to graft AMPs onto titanium or other model surfaces with potential translation as coatings. In overview, releasing strategies have evolved to guarantee higher loadings, prolonged and targeted delivery periods upon infection. In addition, avant-garde self-assembling strategies or polymer brushes allowed higher immobilized peptide surface densities, overcoming bioavailability issues. Future research efforts should focus on the regulatory demands for pre-clinical and clinical validation towards clinical translation. Full article
(This article belongs to the Special Issue Antimicrobial Peptide-Polymer Conjugates)
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39 pages, 2732 KiB  
Review
Current Advances in Lipid and Polymeric Antimicrobial Peptide Delivery Systems and Coatings for the Prevention and Treatment of Bacterial Infections
by Miriam E. van Gent, Muhanad Ali, Peter H. Nibbering and Sylvia N. Kłodzińska
Pharmaceutics 2021, 13(11), 1840; https://doi.org/10.3390/pharmaceutics13111840 - 02 Nov 2021
Cited by 37 | Viewed by 5064
Abstract
Bacterial infections constitute a threat to public health as antibiotics are becoming less effective due to the emergence of antimicrobial resistant strains and biofilm and persister formation. Antimicrobial peptides (AMPs) are considered excellent alternatives to antibiotics; however, they suffer from limitations related to [...] Read more.
Bacterial infections constitute a threat to public health as antibiotics are becoming less effective due to the emergence of antimicrobial resistant strains and biofilm and persister formation. Antimicrobial peptides (AMPs) are considered excellent alternatives to antibiotics; however, they suffer from limitations related to their peptidic nature and possible toxicity. The present review critically evaluates the chemical characteristics and antibacterial effects of lipid and polymeric AMP delivery systems and coatings that offer the promise of enhancing the efficacy of AMPs, reducing their limitations and prolonging their half-life. Unfortunately, the antibacterial activities of these systems and coatings have mainly been evaluated in vitro against planktonic bacteria in less biologically relevant conditions, with only some studies focusing on the antibiofilm activities of the formulated AMPs and on the antibacterial effects in animal models. Further improvements of lipid and polymeric AMP delivery systems and coatings may involve the functionalization of these systems to better target the infections and an analysis of the antibacterial activities in biologically relevant environments. Based on the available data we proposed which polymeric AMP delivery system or coatings could be profitable for the treatment of the different hard-to-treat infections, such as bloodstream infections and catheter- or implant-related infections. Full article
(This article belongs to the Special Issue Antimicrobial Peptide-Polymer Conjugates)
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24 pages, 2667 KiB  
Review
Host Defense Peptide-Mimicking Polymers and Polymeric-Brush-Tethered Host Defense Peptides: Recent Developments, Limitations, and Potential Success
by Hashem Etayash and Robert E. W. Hancock
Pharmaceutics 2021, 13(11), 1820; https://doi.org/10.3390/pharmaceutics13111820 - 01 Nov 2021
Cited by 16 | Viewed by 2773
Abstract
Amphiphilic antimicrobial polymers have attracted considerable interest as structural mimics of host defense peptides (HDPs) that provide a broad spectrum of activity and do not induce bacterial-drug resistance. Likewise, surface engineered polymeric-brush-tethered HDP is considered a promising coating strategy that prevents infections and [...] Read more.
Amphiphilic antimicrobial polymers have attracted considerable interest as structural mimics of host defense peptides (HDPs) that provide a broad spectrum of activity and do not induce bacterial-drug resistance. Likewise, surface engineered polymeric-brush-tethered HDP is considered a promising coating strategy that prevents infections and endows implantable materials and medical devices with antifouling and antibacterial properties. While each strategy takes a different approach, both aim to circumvent limitations of HDPs, enhance physicochemical properties, therapeutic performance, and enable solutions to unmet therapeutic needs. In this review, we discuss the recent advances in each approach, spotlight the fundamental principles, describe current developments with examples, discuss benefits and limitations, and highlight potential success. The review intends to summarize our knowledge in this research area and stimulate further work on antimicrobial polymers and functionalized polymeric biomaterials as strategies to fight infectious diseases. Full article
(This article belongs to the Special Issue Antimicrobial Peptide-Polymer Conjugates)
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