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Design of nanosystems for the delivery of quorum sensing inhibitors: A preliminary study

DOI: 10.3390/molecules25235655 DOI Help

Authors: Supandeep Singh Hallan (University of Ferrara; Malmö University) , Paolo Marchetti (University of Ferrara) , Daria Bortolotti (University of Ferrara) , Maddalena Sguizzato (University of Ferrara) , Elisabetta Esposito (University of Ferrara) , Paolo Mariani (Polytechnic University of Marche) , Claudio Trapella (University of Ferrara) , Roberta Rizzo (University of Ferrara) , Rita Cortesi (University of Ferrara)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Molecules , VOL 25

State: Published (Approved)
Published: November 2020
Diamond Proposal Number(s): 21035

Open Access Open Access

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.

Journal Keywords: nanotechnological systems; liposomes; QS inhibitors; drug delivery; biofilm; MTT test

Subject Areas: Biology and Bio-materials

Instruments: B21-High Throughput SAXS