Coupling quaternary ammonium surfactants to the surface of liposomes improves both antibacterial efficacy and host cell biocompatibility

Montefusco-Pereira, CV; Formicola, B; Goes, A; Re, F; Marrano, CA; Mantegazza, F; Carvalho-Wodarz, C; Fuhrmann, G; Caneva, E; Nicotra, F; Lehr, CM; Russo, L

Abstract

By functionalizing the surface of PEG-liposomes with linkers bearing quaternary ammonium compounds (QACs), we generated novel bacteria disruptors with anti-adhesive properties and reduced cytotoxicity compared to free QACs. Furthermore, QAC-functionalized liposomes are a promising platform for future drug encapsulation. The QAC (11-mercaptoundecyl)-N,N,N-trimethylammonium bromide (MTAB) was attached to maleimide-functionalized liposomes (DSPE-PEG) via thiol linker. The MTAB-functionalized liposomes were physicochemically characterized and their biological activity, in terms of anti-adherence activity and biofilm prevention in Escherichia coli were assessed. The results showed that MTAB-functionalized liposomes inhibit bacterial adherence and biofilm formation while reducing MTAB toxicity.

Keywords: Anti-adherence nanoparticles; Liposomes; Bacterial biofilm; Quarternary ammonium functionalization

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Liposome System

Coupling quaternary ammonium surfactants to the surface of liposomes is an innovative strategy in drug delivery and medical treatment. Liposomes, which are small spherical vesicles made of lipid bilayers, are widely used to encapsulate drugs, ensuring their stability and controlled release within the body. By modifying the surface of liposomes with quaternary ammonium surfactants, scientists aim to enhance their effectiveness and broaden their range of applications. Quaternary ammonium surfactants are positively charged molecules known for their antimicrobial properties and ability to interact with biological membranes. When these surfactants are attached to the surface of liposomes, they confer several beneficial attributes. Firstly, the positive charge can improve the stability of liposomes by preventing aggregation and enhancing their dispersion in biological fluids. Secondly, the antimicrobial properties of quaternary ammonium surfactants can help protect the encapsulated drugs from microbial degradation, ensuring their potency until they reach their target. Moreover, these surfactant-modified liposomes can interact more effectively with negatively charged cellular membranes, improving the delivery of drugs to specific cells or tissues. This targeted delivery system increases the therapeutic efficacy while minimizing side effects, making it particularly valuable for treating infections, cancers, and other diseases.