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

Montefusco-Pereira, Carlos Victor; Formicola, Beatrice; Goes, Adriely; Marrano, Claudia Adriana; Mantegazza, Francesco; Carvalho-Wodarz, Cristiane de Souza; Fuhrmann, Gregor; Caneva, Enrico; Nicotra, Francesco; Lehr, Claus‐Michael; Russo, Laura

doi:10.1016/j.ejpb.2020.01.013

Cited by 21 publications

(14 citation statements)

References 29 publications

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“…Epithelial cells are widely used for biomedical research as constitute primary tissues throughout the body and several reports have used them to study the toxicity of antimicrobial liposome formulations. [ 45–48 ] In this work, because the intended application of L‐GraS is for dermal tissues, it was relevant to evaluate its biocompatibility with epithelial cells.…”

Section: Resultsmentioning

confidence: 99%

Nanodelivery of the Gramicidin Peptide for Enhancing Antimicrobial Activity

Antezana

Municoy

Bellino

et al. 2021

Euro J Lipid Sci & Tech

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Gramicidin S (GraS) is an amphiphilic peptide that has emerged as an effective alternative antibiotic. However, its applicability is restricted for clinical uses due to its effect on eukaryotic cells and low aqueous solubility. In this work, a novel water‐soluble peptide formulation with bactericidal activity is developed by the incorporation of Gramicidin S in the lipid bilayer of liposomes (L‐GraS). As a result, GraS included in the lipid vesicles is stabilized in aqueous medium and showed antimicrobial activity against Staphylococcus aureus. In addition, L‐GraS reveals enhanced biocompatibility with mammalian cells in comparison with the free peptide. Molecular dynamics simulations shed light on the collective behavior between GraS peptides and liposomes from a molecular approach. The molecular dynamic simulations are in agreement with experimental results and further confirm the effective incorporation of GraS in the liposomes, letting understand the best formulation procedure of the vesicles. Therefore, the L‐GraS nanosystem presented here is an interesting alternative to conventional antibiotics, with less restrictions and promising features to improve current therapies. Practical Applications: Incorporation of GraS in liposomes is an interesting approach to increase the solubility of the peptide, thus expanding its therapeutic horizon as a promising alternative to combat bacterial colonization especially in wound infections.

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Section: Resultsmentioning

confidence: 99%

Nanodelivery of the Gramicidin Peptide for Enhancing Antimicrobial Activity

Antezana

Municoy

Bellino

et al. 2021

Euro J Lipid Sci & Tech

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“…This novel nanocarrier platform rests on a rational combination of different approaches to fighting bacteria biofilms, involving the use of liposomes, a composition based on cationic lipids or surfactants [45], the delivery of QSI instead of antibiotics [16], and the functionalization for targeting [42,46], all converging in a successful system that had not yet been investigated.…”

Section: Discussionmentioning

confidence: 99%

Mannosyl, glucosyl or galactosyl liposomes to improve resveratrol efficacy against Methicillin Resistant Staphylococcus aureus biofilm

Aiello

Pagano

Ceccacci

et al. 2021

Colloids and Surfaces A: Physicochemical and Engineering Aspect

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Novel cationic glycoliposomes, composed of 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), cholesterol (Chol) and glycoamphiphiles featuring a galactosyl, mannosyl or glucosyl moiety have been investigated for the targeted delivery of trans-resveratrol (RSV), a Quorum Sensing Inhibitor (QSI), to Methicillin Resistant Staphylococcus Aureus (MRSA) biofilms.All the glycosylated formulations show a 10-20 % reduction of their hydrodynamic size and a high positive increase in ζ-potential (20÷27mV), with respect to the almost neutral DOPC/Chol liposomes (-3.7 mV). RSV is entrapped in liposomes with high Entrapment Efficiency (EE%), the formulations containing glycosylated amphiphiles showing higher values of EE% (79-90 %) than those containing DOPC/CHOL (65 %). In all the liposomal formulations, the inclusion of RSV causes a decrease in ζ-potential, which is particularly evident in the negative value of DOPC/Chol liposomes (-14.8 mV). This is probably due to the ionization of a small percentage of RSV molecules that point towards the lipid/water interface, as reported in the literature.Greater antioxidant activity is found when RSV is embedded in glycosylated liposomes, rather than DOPC/ CHOL liposomes. This finding suggests a different RSV distribution in the lipid membrane enclosing the glycosylated amphiphiles, which favor an external exposure of RSV.Biological assays carried out to monitor the demolition effect of RSV-loaded liposomes on mature biofilm of MRSA show that the presence of cationic glycoamphiphiles is essential for a demolition effect to take place on the biofilm matrix. In particular, RSV-galactosylated liposomes are the most effective in destroying MRSA biofilm even at a RSV concentration (0.019 mM) sixty times lower than the MIC (1.2 mM). This work demonstrates, for the first time, how the functionalization of liposomes with cationic glycosydic residues can enhance liposome performances as QSI nanocarriers for the treatment of biofilm associated infections.

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“…Alternatively, the synthesis of liposomes covalently modified with a quaternary ammonium compound for combination therapy against bacterial infection has been given in [63]. The quaternary ammonium compound ((11-mercaptoundecyl)-N,N,N-trimethylammonium bromide (MTAB)) has been attached to maleimide-functionalized liposomes via a thiol linker.…”

Section: Lipid Nanocarriers Modified With Amphiphilic Moleculesmentioning

confidence: 99%

Nanocarriers for Biomedicine: From Lipid Formulations to Inorganic and Hybrid Nanoparticles

Kashapov

Ibragimova

Pavlov

et al. 2021

IJMS

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Encapsulation of cargoes in nanocontainers is widely used in different fields to solve the problems of their solubility, homogeneity, stability, protection from unwanted chemical and biological destructive effects, and functional activity improvement. This approach is of special importance in biomedicine, since this makes it possible to reduce the limitations of drug delivery related to the toxicity and side effects of therapeutics, their low bioavailability and biocompatibility. This review highlights current progress in the use of lipid systems to deliver active substances to the human body. Various lipid compositions modified with amphiphilic open-chain and macrocyclic compounds, peptide molecules and alternative target ligands are discussed. Liposome modification also evolves by creating new hybrid structures consisting of organic and inorganic parts. Such nanohybrid platforms include cerasomes, which are considered as alternative nanocarriers allowing to reduce inherent limitations of lipid nanoparticles. Compositions based on mesoporous silica are beginning to acquire no less relevance due to their unique features, such as advanced porous properties, well-proven drug delivery efficiency and their versatility for creating highly efficient nanomaterials. The types of silica nanoparticles, their efficacy in biomedical applications and hybrid inorganic-polymer platforms are the subject of discussion in this review, with current challenges emphasized.

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

Cited by 21 publications

References 29 publications

Nanodelivery of the Gramicidin Peptide for Enhancing Antimicrobial Activity

Nanodelivery of the Gramicidin Peptide for Enhancing Antimicrobial Activity

Mannosyl, glucosyl or galactosyl liposomes to improve resveratrol efficacy against Methicillin Resistant Staphylococcus aureus biofilm

Nanocarriers for Biomedicine: From Lipid Formulations to Inorganic and Hybrid Nanoparticles

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