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Biomedicines
Volume 10
Issue 6
10.3390/biomedicines10061301
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Article

Novel Retro-Inverso Peptide Antibiotic Efficiently Released by a Responsive Hydrogel-Based System

by
Angela Cesaro
1,2,3,
Rosa Gaglione
4,5,
Marco Chino
4,
Maria De Luca
4,
Rocco Di Girolamo
4,
Angelina Lombardi
4,
Rosanna Filosa
6,7 and
Angela Arciello
4,5,*
1
Machine Biology Group, Departments of Psychiatry and Microbiology, Institute for Biomedical Informatics, Institute for Translational Medicine and Therapeutics, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA
2
Departments of Bioengineering and Chemical and Biomolecular Engineering, School of Engineering and Applied Science, University of Pennsylvania, Philadelphia, PA 19104, USA
3
Penn Institute for Computational Science, University of Pennsylvania, Philadelphia, PA 19104, USA
4
Department of Chemical Sciences, University of Naples Federico II, Via Cintia 21, I-80126 Naples, Italy
5
Istituto Nazionale di Biostrutture e Biosistemi (INBB), I-00136 Rome, Italy
6
AMP Biotec, Research Start-Up, s.s. 7, km 256, I-82030 Apollosa, Italy
7
Department of Sciences and Technology, University of Sannio, Via De Sanctis, I-82100 Benevento, Italy
*
Author to whom correspondence should be addressed.
Biomedicines 2022, 10(6), 1301; https://doi.org/10.3390/biomedicines10061301
Submission received: 4 May 2022 / Revised: 27 May 2022 / Accepted: 29 May 2022 / Published: 2 June 2022
(This article belongs to the Special Issue Antimicrobial Peptides Aka Host Defense Peptides – from Basic Research to Therapy)
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Abstract

Topical antimicrobial treatments are often ineffective on recalcitrant and resistant skin infections. This necessitates the design of antimicrobials that are less susceptible to resistance mechanisms, as well as the development of appropriate delivery systems. These two issues represent a great challenge for researchers in pharmaceutical and drug discovery fields. Here, we defined the therapeutic properties of a novel peptidomimetic inspired by an antimicrobial sequence encrypted in human apolipoprotein B. The peptidomimetic was found to exhibit antimicrobial and anti-biofilm properties at concentration values ranging from 2.5 to 20 µmol L−1, to be biocompatible toward human skin cell lines, and to protect human keratinocytes from bacterial infections being able to induce a reduction of bacterial units by two or even four orders of magnitude with respect to untreated samples. Based on these promising results, a hyaluronic-acid-based hydrogel was devised to encapsulate and to specifically deliver the selected antimicrobial agent to the site of infection. The developed hydrogel-based system represents a promising, effective therapeutic option by combining the mechanical properties of the hyaluronic acid polymer with the anti-infective activity of the antimicrobial peptidomimetic, thus opening novel perspectives in the treatment of skin infections.
Keywords: drug design; antimicrobial peptidomimetic; hydrogel-based system; hyaluronic acid; anti-infective activity; skin infections drug design; antimicrobial peptidomimetic; hydrogel-based system; hyaluronic acid; anti-infective activity; skin infections

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MDPI and ACS Style

Cesaro, A.; Gaglione, R.; Chino, M.; De Luca, M.; Di Girolamo, R.; Lombardi, A.; Filosa, R.; Arciello, A. Novel Retro-Inverso Peptide Antibiotic Efficiently Released by a Responsive Hydrogel-Based System. Biomedicines 2022, 10, 1301. https://doi.org/10.3390/biomedicines10061301

AMA Style

Cesaro A, Gaglione R, Chino M, De Luca M, Di Girolamo R, Lombardi A, Filosa R, Arciello A. Novel Retro-Inverso Peptide Antibiotic Efficiently Released by a Responsive Hydrogel-Based System. Biomedicines. 2022; 10(6):1301. https://doi.org/10.3390/biomedicines10061301

Chicago/Turabian Style

Cesaro, Angela, Rosa Gaglione, Marco Chino, Maria De Luca, Rocco Di Girolamo, Angelina Lombardi, Rosanna Filosa, and Angela Arciello. 2022. "Novel Retro-Inverso Peptide Antibiotic Efficiently Released by a Responsive Hydrogel-Based System" Biomedicines 10, no. 6: 1301. https://doi.org/10.3390/biomedicines10061301

APA Style

Cesaro, A., Gaglione, R., Chino, M., De Luca, M., Di Girolamo, R., Lombardi, A., Filosa, R., & Arciello, A. (2022). Novel Retro-Inverso Peptide Antibiotic Efficiently Released by a Responsive Hydrogel-Based System. Biomedicines, 10(6), 1301. https://doi.org/10.3390/biomedicines10061301

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