Antipathogenic Activity of Betainized Polyethyleneimine Sprays Without Toxicity

<b>Background/Objectives</b>: The design of alternative antipathogenic sprays has recently attracted much attention due to the limitations of existing formulations, such as toxicity and low and narrow efficacy. Polyethyleneimine (PEI) is a great antimicrobial polymer against a wide range...

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Main Authors: Selin S. Suner, Ramesh S. Ayyala, Nurettin Sahiner
Format: Article
Language:English
Published: MDPI AG 2024-10-01
Series:Biomedicines
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Online Access:https://www.mdpi.com/2227-9059/12/11/2462
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author Selin S. Suner
Ramesh S. Ayyala
Nurettin Sahiner
author_facet Selin S. Suner
Ramesh S. Ayyala
Nurettin Sahiner
author_sort Selin S. Suner
collection DOAJ
description <b>Background/Objectives</b>: The design of alternative antipathogenic sprays has recently attracted much attention due to the limitations of existing formulations, such as toxicity and low and narrow efficacy. Polyethyleneimine (PEI) is a great antimicrobial polymer against a wide range of pathogens, but toxicity limits its use. Here, betainized PEI (B-PEI) was synthesized to decrease the toxicity of PEI and protonated with citric acid (CA), boric acid (BA), and HCl to improve antimicrobial activity. <b>Methods</b>: Cytotoxicity of the PEI-based solutions was determined on L929 fibroblast cells. Antibacterial/fungal activity of PEI-based antipathogenic sprays was investigated by microtiter and disc diffusion assays, in addition to bacterial viability and adhesion % of common bacteria and fungi on the PEI-treated masks. Furthermore, the antiviral effect of the PEI-based solutions was determined against SARS-CoV-2 virus. <b>Results</b>: The biosafe concentration of PEI was determined as 1 μg/mL with 75 ± 11% cell viability, but B-PEI and its protonated forms had great biocompatibility even at 1000 μg/mL with more than 85% viability. The antibacterial/fungal effect of non-toxic B-PEI was improved by protonation with BA and HCl with 2.5–10 mg/mL minimum bactericidal/fungicidal concentrations (MBCs/MFCs). Bacterial/fungal viability and adhesion on the mask was almost eliminated by using 50 μL with 5–10 mg/mL of B-PEI-BA. Both protonated bare and betainized PEI show potent antiviral activity against SARS-CoV-2 virus. <b>Conclusions</b>: The toxicity of PEI was overcome by using betainized forms of PEI (B-PEI). Furthermore, the antimicrobial and antiviral efficacy of PEI and B-PEI was improved by protonation with CA, BA, and HCl of amine groups on B-PEI. B-PEI-BA spray solution has great potential as an antipathogenic spray with broad-spectrum antimicrobial potency against harmful bacteria, fungi, and viruses without any toxicity.
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spelling doaj-art-f3f1a94e84a14bd2b2cbf587a55616b02025-08-20T02:28:02ZengMDPI AGBiomedicines2227-90592024-10-011211246210.3390/biomedicines12112462Antipathogenic Activity of Betainized Polyethyleneimine Sprays Without ToxicitySelin S. Suner0Ramesh S. Ayyala1Nurettin Sahiner2Department of Chemistry, Faculty of Sciences, Canakkale Onsekiz Mart University Terzioglu Campus, Canakkale 17100, TurkeyDepartment of Ophthalmology, Morsani College of Medicine, University of South Florida, Tampa, FL 33612, USADepartment of Chemistry, Faculty of Sciences, Canakkale Onsekiz Mart University Terzioglu Campus, Canakkale 17100, Turkey<b>Background/Objectives</b>: The design of alternative antipathogenic sprays has recently attracted much attention due to the limitations of existing formulations, such as toxicity and low and narrow efficacy. Polyethyleneimine (PEI) is a great antimicrobial polymer against a wide range of pathogens, but toxicity limits its use. Here, betainized PEI (B-PEI) was synthesized to decrease the toxicity of PEI and protonated with citric acid (CA), boric acid (BA), and HCl to improve antimicrobial activity. <b>Methods</b>: Cytotoxicity of the PEI-based solutions was determined on L929 fibroblast cells. Antibacterial/fungal activity of PEI-based antipathogenic sprays was investigated by microtiter and disc diffusion assays, in addition to bacterial viability and adhesion % of common bacteria and fungi on the PEI-treated masks. Furthermore, the antiviral effect of the PEI-based solutions was determined against SARS-CoV-2 virus. <b>Results</b>: The biosafe concentration of PEI was determined as 1 μg/mL with 75 ± 11% cell viability, but B-PEI and its protonated forms had great biocompatibility even at 1000 μg/mL with more than 85% viability. The antibacterial/fungal effect of non-toxic B-PEI was improved by protonation with BA and HCl with 2.5–10 mg/mL minimum bactericidal/fungicidal concentrations (MBCs/MFCs). Bacterial/fungal viability and adhesion on the mask was almost eliminated by using 50 μL with 5–10 mg/mL of B-PEI-BA. Both protonated bare and betainized PEI show potent antiviral activity against SARS-CoV-2 virus. <b>Conclusions</b>: The toxicity of PEI was overcome by using betainized forms of PEI (B-PEI). Furthermore, the antimicrobial and antiviral efficacy of PEI and B-PEI was improved by protonation with CA, BA, and HCl of amine groups on B-PEI. B-PEI-BA spray solution has great potential as an antipathogenic spray with broad-spectrum antimicrobial potency against harmful bacteria, fungi, and viruses without any toxicity.https://www.mdpi.com/2227-9059/12/11/2462polyethyleneiminebetainized polyethyleneimineantipathogenic spraysbiocompatibleantimicrobialantiviral
spellingShingle Selin S. Suner
Ramesh S. Ayyala
Nurettin Sahiner
Antipathogenic Activity of Betainized Polyethyleneimine Sprays Without Toxicity
Biomedicines
polyethyleneimine
betainized polyethyleneimine
antipathogenic sprays
biocompatible
antimicrobial
antiviral
title Antipathogenic Activity of Betainized Polyethyleneimine Sprays Without Toxicity
title_full Antipathogenic Activity of Betainized Polyethyleneimine Sprays Without Toxicity
title_fullStr Antipathogenic Activity of Betainized Polyethyleneimine Sprays Without Toxicity
title_full_unstemmed Antipathogenic Activity of Betainized Polyethyleneimine Sprays Without Toxicity
title_short Antipathogenic Activity of Betainized Polyethyleneimine Sprays Without Toxicity
title_sort antipathogenic activity of betainized polyethyleneimine sprays without toxicity
topic polyethyleneimine
betainized polyethyleneimine
antipathogenic sprays
biocompatible
antimicrobial
antiviral
url https://www.mdpi.com/2227-9059/12/11/2462
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AT nurettinsahiner antipathogenicactivityofbetainizedpolyethyleneiminesprayswithouttoxicity