Structure–activity relationship of drug conjugated polymeric materials against uropathogenic bacteria colonization under <i>in vitro</i> and <i>in vivo</i> settings

Sarkar, Sourav; Moitra, Parikshit; Bhattacharya, Santanu

doi:10.1039/d3tb01841e

J. Mater. Chem. B

2024

DOI: 10.1039/d3tb01841e

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Structure–activity relationship of drug conjugated polymeric materials against uropathogenic bacteria colonization under in vitro and in vivo settings

Sourav Sarkar,

Parikshit Moitra,

Santanu Bhattacharya

Abstract: Schematic representation of the drug conjugated polyethyleneimine and its application in inhibiting the bacterial biofilm formation on inanimate surfaces as well as on mouse skin abrasion model.

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Unlocking the Potential: PEGylation and Molecular Weight Reduction of Ionenes for Enhanced Antifungal Activity and Biocompatibility

Kurzyna,

Kopiasz,

Paul

et al. 2024

Macromolecular Bioscience

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Numerous synthetic polymers, imitating natural antimicrobial peptides, have demonstrated potent antimicrobial activity, positioning them as potential candidates for new antimicrobial drugs. However, the high activity of these molecules often comes at the cost of elevated toxicity against eukaryotic organisms. In this study, a series of cationic ionenes with varying molecular weights to assess the influence of polymer chain length on ionene activity is investigated. To enhance polymer antimicrobial activity and limit toxicity a PEG side chain is introduced into the repeating unit. The resulting molecules consistently exhibited high activity against three model organisms: E. coli, S. aureus and C. albicans. The incorporation of side PEG chain improves antifungal properties and biocompatibility, regardless of molecular weight. The most important finding of this work is that the reduction of polymer molecular mass led to increased antifungal activity and reduced cytotoxicity against HMF and MRC‐5 cell lines simultaneously. As a result, the best‐performing molecules reported herein displayed minimal inhibitory concentrations (MIC) as low as 2 and 0.0625 µg mL1 for C. albicans and C. tropicalis respectively, demonstrating exceptional selectivity. It is plausible that some of described herein molecules can serve as potential lead candidates for new antifungal drugs.

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Unlocking the Potential: PEGylation and Molecular Weight Reduction of Ionenes for Enhanced Antifungal Activity and Biocompatibility

Kurzyna,

Kopiasz,

Paul

et al. 2024

Macromolecular Bioscience

View full text Add to dashboard Cite

show abstract

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Structure–activity relationship of drug conjugated polymeric materials against uropathogenic bacteria colonization under in vitro and in vivo settings

Abstract: Schematic representation of the drug conjugated polyethyleneimine and its application in inhibiting the bacterial biofilm formation on inanimate surfaces as well as on mouse skin abrasion model.

Cited by 1 publication

References 89 publications

Unlocking the Potential: PEGylation and Molecular Weight Reduction of Ionenes for Enhanced Antifungal Activity and Biocompatibility

Unlocking the Potential: PEGylation and Molecular Weight Reduction of Ionenes for Enhanced Antifungal Activity and Biocompatibility

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