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 (LUVfuso VAN), and cationic (LUVcat 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 LUVfuso VAN, LUVcat 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 LUVfuso 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.
Highlights
Staphylococcus aureus (S. aureus) is a Gram-positive microorganism responsible for the majority of nosocomial and community-acquired infections
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
Vancomycin encapsulated in fusogenic liposomes demonstrated enhanced antimicrobial activity against mature S. aureus biofilms
Summary
Staphylococcus aureus (S. aureus) is a Gram-positive microorganism responsible for the majority of nosocomial and community-acquired infections. Over 90% of S. aureus strains are found to be resistant to methicillin (methicillin resistant S. aureus—MRSA), penicillin, aminoglycosides, macrolides, lincosamides, and other beta-lactams (Chakraborty et al, 2012; Muppidi et al, 2012; Sande et al, 2012; Elkhodairy et al, 2014; Shi et al, 2014) In this scenario of microbial resistance, vancomycin (VAN) is considered a first-choice antibiotic for the treatment of methicillin-resistant S. aureus (MRSA) infections (Pumerantz et al, 2011; Honary et al, 2013; Holland et al, 2014; Men et al, 2016; Gudiol et al, 2017). VAN systemic side effects are another limiting factor, which include severe watery diarrhea, kidney failure (Pumerantz et al, 2011; Rose et al, 2012; Honary et al, 2013), ototoxicity, neutropenia, fever, anaphylaxis, thrombocytopenia, and phlebitis (McAuley, 2012)
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
