AUTHOR=Scriboni Andreia Borges , Couto Verônica Muniz , Ribeiro Lígia Nunes de Morais , Freires Irlan Almeida , Groppo Francisco Carlos , de Paula Eneida , Franz-Montan Michelle , Cogo-Müller Karina TITLE=Fusogenic Liposomes Increase the Antimicrobial Activity of Vancomycin Against Staphylococcus aureus Biofilm JOURNAL=Frontiers in Pharmacology VOLUME=10 YEAR=2019 URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2019.01401 DOI=10.3389/fphar.2019.01401 ISSN=1663-9812 ABSTRACT=

Objective: The aim of the present study was to encapsulate vancomycin in different liposomal formulations and compare the in vitro antimicrobial activity against Staphylococcus aureus biofilms.

Methods: Large unilamellar vesicles of conventional (LUV VAN), fusogenic (LUV_fuso VAN), and cationic (LUV_cat VAN) liposomes encapsulating VAN were characterized in terms of size, polydispersity index, zeta potential, morphology, encapsulation efficiency (%EE) and in vitro release kinetics. The formulations were tested for their Minimum Inhibitory Concentration (MIC) and inhibitory activity on biofilm formation and viability, using methicillin-susceptible S. aureus ATCC 29213 and methicillin-resistant S. aureus ATCC 43300 strains.

Key Findings: LUV VAN showed better %EE (32.5%) and sustained release than LUV_fuso VAN, LUV_cat VAN, and free VAN. The formulations were stable over 180 days at 4°C, except for LUV VAN, which was stable up to 120 days. The MIC values for liposomal formulations and free VAN ranged from 0.78 to 1.56 µg/ml against both tested strains, with no difference in the inhibition of biofilm formation as compared to free VAN. However, when treating mature biofilm, encapsulated LUV_fuso VAN increased the antimicrobial efficacy as compared to the other liposomal formulations and to free VAN, demonstrating a better ability to penetrate the biofilm.

Conclusion: Vancomycin encapsulated in fusogenic liposomes demonstrated enhanced antimicrobial activity against mature S. aureus biofilms.