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Pharmaceutics
Special Issues
Breakthroughs in Antimicrobial Peptides
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Breakthroughs in Antimicrobial Peptides

A special issue of Pharmaceutics (ISSN 1999-4923).

Deadline for manuscript submissions: closed (31 May 2019) | Viewed by 36488

Special Issue Editor

Prof. Dr. Stefania Galdiero

E-Mail Website1 Website2
Guest Editor
Department of Pharmacy, University of Naples Federico II, Via Mezzocannone 16, 80134 Napoli, Italy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antimicrobial peptides (AMPs) are continuously attracting attention as a challenging opportunity for advanced medical applications. The rapid worldwide development of resistance to conventional antibiotics makes it imperative to allocate efforts to bring AMPs with advanced properties into clinical use. In fact, antibiotic resistance is a priority concern, and the technological development of new materials with antimicrobial properties provides a breakthrough for the discovery of new molecules for therapeutic use.

This Special Issue of Pharmaceutics focuses on new strategies and approaches to AMP-based systems intended for antimicrobial therapies, which could also be combined with anti-cancer therapies. We welcome articles concerning all aspects of AMP-based molecules designed for advanced therapy. Especially, studies on the relationships between biophysical features and activities, new materials, original synthetic approaches, innovative formulation and delivery strategies are welcome for this Special Issue. Articles illustrating current and future trends in the development of AMP therapeutics spanning a multitude of disciplines including chemistry, physics, biology, pharmaceutical materials science, and contributing to the design of highly active molecules are highly encouraged.

Prof. Stefania Galdiero
Guest Editor

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Keywords

  • peptide
  • antimicrobials
  • membranes
  • bacteria
  • biofilm
  • materials

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Published Papers (5 papers)

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Research

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15 pages, 316 KiB  
Article
Influence of Short Cationic Lipopeptides with Fatty Acids of Different Chain Lengths on Bacterial Biofilms Formed on Polystyrene and Hydrogel Surfaces
by Malgorzata Anna Paduszynska, Magdalena Maciejewska, Damian Neubauer, Krzysztof Golacki, Magdalena Szymukowicz, Marta Bauer and Wojciech Kamysz
Pharmaceutics 2019, 11(10), 506; https://doi.org/10.3390/pharmaceutics11100506 - 1 Oct 2019
Cited by 18 | Viewed by 3652
Abstract
Nowadays, biomaterials are applied in many different branches of medicine. They significantly improve the patients’ comfort and quality of life, but also constitute a significant risk factor for biofilm-associated infections. Currently, intensive research on the development of novel materials resistant to microbial colonization [...] Read more.
Nowadays, biomaterials are applied in many different branches of medicine. They significantly improve the patients’ comfort and quality of life, but also constitute a significant risk factor for biofilm-associated infections. Currently, intensive research on the development of novel materials resistant to microbial colonization as well as new compounds that are active against biofilms is being carried out. Within this research, antimicrobial peptides (AMPs) and their analogues are being intensively investigated due to their promising antimicrobial activities. The main goal of this study was to synthesize and evaluate the antimicrobial efficacy of short cationic lipopeptides that were designed to imitate the features of AMPs responsible for antimicrobial activities: positive net charge and amphipacity. The positive charge of the molecules results from the presence of basic amino acid residues: arginine and lysine. Amphipacity is provided by the introduction of decanoic, dodecanoic, tetradecanoic, and hexadecanoic acid chains to the molecules. Lipopeptides (C16-KR-NH2, C16-KKK-NH2, C16-KKC-NH2, C16-KGK-NH2, C14-KR-NH2, C14-KKC-NH2, C12-KR-NH2, C12-KKC-NH2, and (C10)2-KKKK-NH2) were synthesized using a novel solid-phase temperature-assisted methodology. The minimum inhibitory concentrations (MICs), minimum biofilm eradication concentrations (MBECs), and minimum biofilm formation inhibitory concentrations (MBFICs) were determined for the following bacterial strains: Staphylococcus aureus ATCC 25923, Staphylococcus epidermidis ATCC 14990, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 9027, and Proteus mirabilis PCM 543. The biofilms were cultured on two types of surfaces: polystyrene plates (PS) and contact lenses (CL). The lipopeptides exhibited the ability to inhibit the growth of bacteria in a liquid medium as well as on the PS and CL. The compounds also eliminated the bacterial biofilm from the surface of both materials. In general, the activity against gram-positive bacteria was stronger in comparison to that against gram-negative strains. There were certain discrepancies between the activity of compounds against the biofilm cultured on PS and CL. This was especially noticeable for staphylococci—the lipopeptides presented much higher activity against biofilm formed on the PS surface. It is worth noting that the obtained MBEC values for lipopeptides were usually only a few times higher than the MICs. The results of the performed experiments suggest that further studies on lipopeptides and their potential application in the treatment and prophylaxis of biofilm-associated infections should be conducted. Full article
(This article belongs to the Special Issue Breakthroughs in Antimicrobial Peptides)
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Review

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33 pages, 2716 KiB  
Review
Advances in Lipid and Metal Nanoparticles for Antimicrobial Peptide Delivery
by Marcin Makowski, Ítala C. Silva, Constança Pais do Amaral, Sónia Gonçalves and Nuno C. Santos
Pharmaceutics 2019, 11(11), 588; https://doi.org/10.3390/pharmaceutics11110588 - 8 Nov 2019
Cited by 89 | Viewed by 8978
Abstract
Antimicrobial peptides (AMPs) have been described as excellent candidates to overcome antibiotic resistance. Frequently, AMPs exhibit a wide therapeutic window, with low cytotoxicity and broad-spectrum antimicrobial activity against a variety of pathogens. In addition, some AMPs are also able to modulate the immune [...] Read more.
Antimicrobial peptides (AMPs) have been described as excellent candidates to overcome antibiotic resistance. Frequently, AMPs exhibit a wide therapeutic window, with low cytotoxicity and broad-spectrum antimicrobial activity against a variety of pathogens. In addition, some AMPs are also able to modulate the immune response, decreasing potential harmful effects such as sepsis. Despite these benefits, only a few formulations have successfully reached clinics. A common flaw in the druggability of AMPs is their poor pharmacokinetics, common to several peptide drugs, as they may be degraded by a myriad of proteases inside the organism. The combination of AMPs with carrier nanoparticles to improve delivery may enhance their half-life, decreasing the dosage and thus, reducing production costs and eventual toxicity. Here, we present the most recent advances in lipid and metal nanodevices for AMP delivery, with a special focus on metal nanoparticles and liposome formulations. Full article
(This article belongs to the Special Issue Breakthroughs in Antimicrobial Peptides)
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24 pages, 1289 KiB  
Review
Nanosystems as Vehicles for the Delivery of Antimicrobial Peptides (AMPs)
by Ángela Martin-Serrano, Rafael Gómez, Paula Ortega and F. Javier de la Mata
Pharmaceutics 2019, 11(9), 448; https://doi.org/10.3390/pharmaceutics11090448 - 2 Sep 2019
Cited by 97 | Viewed by 8168
Abstract
Recently, antimicrobial peptides (AMPs), also called host defence peptides (HDPs), are attracting great interest, as they are a highly viable alternative in the search of new approaches to the resistance presented by bacteria against antibiotics in infectious diseases. However, due to their nature, [...] Read more.
Recently, antimicrobial peptides (AMPs), also called host defence peptides (HDPs), are attracting great interest, as they are a highly viable alternative in the search of new approaches to the resistance presented by bacteria against antibiotics in infectious diseases. However, due to their nature, they present a series of disadvantages such as low bioavailability, easy degradability by proteases, or low solubility, among others, which limits their use as antimicrobial agents. For all these reasons, the use of vehicles for the delivery of AMPs, such as polymers, nanoparticles, micelles, carbon nanotubes, dendrimers, and other types of systems, allows the use of AMPs as a real alternative to treatment with antibiotics. Full article
(This article belongs to the Special Issue Breakthroughs in Antimicrobial Peptides)
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15 pages, 1388 KiB  
Review
Biofilms: Novel Strategies Based on Antimicrobial Peptides
by Emilia Galdiero, Lucia Lombardi, Annarita Falanga, Giovanni Libralato, Marco Guida and Rosa Carotenuto
Pharmaceutics 2019, 11(7), 322; https://doi.org/10.3390/pharmaceutics11070322 - 10 Jul 2019
Cited by 99 | Viewed by 7560
Abstract
The problem of drug resistance is very worrying and ever increasing. Resistance is due not only to the reckless use of antibiotics but also to the fact that pathogens are able to adapt to different conditions and develop self-defense mechanisms such as living [...] Read more.
The problem of drug resistance is very worrying and ever increasing. Resistance is due not only to the reckless use of antibiotics but also to the fact that pathogens are able to adapt to different conditions and develop self-defense mechanisms such as living in biofilms; altogether these issues make the search for alternative drugs a real challenge. Antimicrobial peptides appear as promising alternatives but they have disadvantages that do not make them easily applicable in the medical field; thus many researches look for solutions to overcome the disadvantages and ensure that the advantages can be exploited. This review describes the biofilm characteristics and identifies the key features that antimicrobial peptides should have. Recalcitrant bacterial infections caused by the most obstinate bacterial species should be treated with a strategy to combine conventional peptides functionalized with nano-tools. This approach could effectively disrupt high density infections caused by biofilms. Moreover, the importance of using in vivo non mammalian models for biofilm studies is described. In particular, here we analyze the use of amphibians as a model to substitute the rodent model. Full article
(This article belongs to the Special Issue Breakthroughs in Antimicrobial Peptides)
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17 pages, 1094 KiB  
Review
A New Hope: Self-Assembling Peptides with Antimicrobial Activity
by Lucia Lombardi, Annarita Falanga, Valentina Del Genio and Stefania Galdiero
Pharmaceutics 2019, 11(4), 166; https://doi.org/10.3390/pharmaceutics11040166 - 4 Apr 2019
Cited by 93 | Viewed by 7289
Abstract
Peptide drugs hold great promise for the treatment of infectious diseases thanks to their novel mechanisms of action, low toxicity, high specificity, and ease of synthesis and modification. Naturally developing self-assembly in nature has inspired remarkable interest in self-assembly of peptides to functional [...] Read more.
Peptide drugs hold great promise for the treatment of infectious diseases thanks to their novel mechanisms of action, low toxicity, high specificity, and ease of synthesis and modification. Naturally developing self-assembly in nature has inspired remarkable interest in self-assembly of peptides to functional nanomaterials. As a matter of fact, their structural, mechanical, and functional advantages, plus their high bio-compatibility and bio-degradability make them excellent candidates for facilitating biomedical applications. This review focuses on the self-assembly of peptides for the fabrication of antibacterial nanomaterials holding great interest for substituting antibiotics, with emphasis on strategies to achieve nano-architectures of self-assembly. The antibacterial activities achieved by these nanomaterials are also described. Full article
(This article belongs to the Special Issue Breakthroughs in Antimicrobial Peptides)
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