Monocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains

Abstract The development of biomaterials able to act against a wide range of bacteria, including antibiotic resistant bacteria, is of great importance since bacterial colonization is one of the main causes of implant failure. In this work, we explored the possibility to functionalize hydroxyapatite...

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Autores principales:	Daria Giacomini, Paola Torricelli, Giovanna Angela Gentilomi, Elisa Boanini, Massimo Gazzano, Francesca Bonvicini, Emanuele Benetti, Roberto Soldati, Giulia Martelli, Katia Rubini, Adriana Bigi
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2017
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/1a1a7c8ec64f41fcbdcd139851583df5
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spelling	oai:doaj.org-article:1a1a7c8ec64f41fcbdcd139851583df52021-12-02T15:05:23ZMonocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains10.1038/s41598-017-02943-22045-2322https://doaj.org/article/1a1a7c8ec64f41fcbdcd139851583df52017-06-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-02943-2https://doaj.org/toc/2045-2322Abstract The development of biomaterials able to act against a wide range of bacteria, including antibiotic resistant bacteria, is of great importance since bacterial colonization is one of the main causes of implant failure. In this work, we explored the possibility to functionalize hydroxyapatite (HA) nanocrystals with some monocyclic N-thio-substituted β-lactams. To this aim, a series of non-polar azetidinones have been synthesized and characterized. The amount of azetidinones loaded on HA could be properly controlled on changing the polarity of the loading solution and it can reach values up to 17 wt%. Data on cumulative release in aqueous solution show different trends which can be related to the lipophilicity of the molecules and can be modulated by suitable groups on the azetidinone. The examined β-lactams-HA composites display good antibacterial activity against reference Gram-positive and Gram-negative bacteria. However, the results of citotoxicity and antibacterial tests indicate that HA loaded with 4-acetoxy-1-(methylthio)-azetidin-2-one displays the best performance. In fact, this material strongly inhibited the bacterial growth of both methicillin resistant and methicillin susceptible clinical isolates of S. aureus from surgical bone biopsies, showing to be a very good candidate as a new functional biomaterial with enhanced antibacterial activity.Daria GiacominiPaola TorricelliGiovanna Angela GentilomiElisa BoaniniMassimo GazzanoFrancesca BonviciniEmanuele BenettiRoberto SoldatiGiulia MartelliKatia RubiniAdriana BigiNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-12 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Daria Giacomini Paola Torricelli Giovanna Angela Gentilomi Elisa Boanini Massimo Gazzano Francesca Bonvicini Emanuele Benetti Roberto Soldati Giulia Martelli Katia Rubini Adriana Bigi Monocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains
description	Abstract The development of biomaterials able to act against a wide range of bacteria, including antibiotic resistant bacteria, is of great importance since bacterial colonization is one of the main causes of implant failure. In this work, we explored the possibility to functionalize hydroxyapatite (HA) nanocrystals with some monocyclic N-thio-substituted β-lactams. To this aim, a series of non-polar azetidinones have been synthesized and characterized. The amount of azetidinones loaded on HA could be properly controlled on changing the polarity of the loading solution and it can reach values up to 17 wt%. Data on cumulative release in aqueous solution show different trends which can be related to the lipophilicity of the molecules and can be modulated by suitable groups on the azetidinone. The examined β-lactams-HA composites display good antibacterial activity against reference Gram-positive and Gram-negative bacteria. However, the results of citotoxicity and antibacterial tests indicate that HA loaded with 4-acetoxy-1-(methylthio)-azetidin-2-one displays the best performance. In fact, this material strongly inhibited the bacterial growth of both methicillin resistant and methicillin susceptible clinical isolates of S. aureus from surgical bone biopsies, showing to be a very good candidate as a new functional biomaterial with enhanced antibacterial activity.
format	article
author	Daria Giacomini Paola Torricelli Giovanna Angela Gentilomi Elisa Boanini Massimo Gazzano Francesca Bonvicini Emanuele Benetti Roberto Soldati Giulia Martelli Katia Rubini Adriana Bigi
author_facet	Daria Giacomini Paola Torricelli Giovanna Angela Gentilomi Elisa Boanini Massimo Gazzano Francesca Bonvicini Emanuele Benetti Roberto Soldati Giulia Martelli Katia Rubini Adriana Bigi
author_sort	Daria Giacomini
title	Monocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains
title_short	Monocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains
title_full	Monocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains
title_fullStr	Monocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains
title_full_unstemmed	Monocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains
title_sort	monocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains
publisher	Nature Portfolio
publishDate	2017
url	https://doaj.org/article/1a1a7c8ec64f41fcbdcd139851583df5
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Monocyclic β-lactams loaded on hydroxyapatite: new biomaterials with enhanced antibacterial activity against resistant strains

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