Design of Nanosystems for the Delivery of Quorum Sensing Inhibitors: A Preliminary Study.

Supandeep Singh Hallan,Rita Cortesi,Maddalena Sguizzato,Claudio Trapella,Paolo Marchetti,Elisabetta Esposito,Roberta Rizzo,Paolo Mariani,Daria Bortolotti

doi:10.3390/molecules25235655

Supandeep Singh Hallan, Rita Cortesi + Show 7 more

Open Access

https://doi.org/10.3390/molecules25235655

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Abstract

Biofilm production is regulated by the Quorum Sensing system. Nowadays, Quorum Sensing represents an appealing target to design new compounds to increase antibiotics effects and avoid development of antibiotics multiresistance. In this research the use of liposomes to target two novel synthetic biofilm inhibitors is presented, focusing on a preformulation study to select a liposome composition for in vitro test. Five different liposome (LP) formulations, composed of phosphatidyl choline, cholesterol and charged surfactant (2:1:1, molar ratio) have been prepared by direct hydration and extrusion. As charged surfactants dicetyl phosphate didecyldimethylammonium chloride, di isobutyl phenoxy ethyl dimethyl benzyl ammonium chloride and stearylamine (SA) and have been used. Liposome charge, size and morphology were investigated by zeta potential, photon correlation spectroscopy, small angle x-ray spectroscopy and electron microscopy. LP-SA was selected for the loading of biofilm inhibitors and subjected to high performance liquid chromatography for entrapment capacity evaluation. LP-SA loaded inhibitors showed a higher diameter (223.6 nm) as compared to unloaded ones (205.7 nm) and a dose-dependent anti-biofilm effect mainly after 48 h of treatment, while free biofilm inhibitors loose activity. In conclusion, our data supported the use of liposomes as a strategy to enhance biofilm inhibitors effect.

Highlights

IntroductionBiofilms can be described as a dispersion of immobilized microbial colonies within a self-produced matrix of hydrophilic extracellular polymers such as polysaccharides, proteins and nucleic acids
Biofilms can be described as a dispersion of immobilized microbial colonies within a self-produced matrix of hydrophilic extracellular polymers such as polysaccharides, proteins and nucleic acids.Many factors such as surface properties, nutrient availability and the presence of microbial constituents are able to influence the structure and composition of biofilms [1]
100 μL of acetic acid 33% was added to each well to solubilize crystal violet and the absorbance read at 570 nm. This preliminary study was finalized to evaluate the possible employment of liposomes as carriers for QS inhibitor (QSi)

Summary

Introduction

Biofilms can be described as a dispersion of immobilized microbial colonies within a self-produced matrix of hydrophilic extracellular polymers such as polysaccharides, proteins and nucleic acids Many factors such as surface properties, nutrient availability and the presence of microbial constituents are able to influence the structure and composition of biofilms [1]. Biofilm formation is a very complex process in which some cells, when it reaches maturity, begin to detach and separate from the aggregates repeatedly, leading to a continuous generation of bacteria able to spread and originate new microcolonies [4]. For this reason, bacterial biofilm represents a challenge in Molecules 2020, 25, 5655; doi:10.3390/molecules25235655 www.mdpi.com/journal/molecules. The inhibition of biofilm formation can be considered a suitable target to design new antibacterial therapies

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