Antimicrobial activity of β-lapachone encapsulated into liposomes against meticillin-resistant Staphylococcus aureus and Cryptococcus neoformans clinical strains

• Published in: Journal of global antimicrobial resistance. 2015-06, Vol.3 (2), p.103-108
• Main Authors: Cavalcanti, I.M.F., Pontes-Neto, J.G., Kocerginsky, P.O., Bezerra-Neto, A.M., Lima, J.L.C., Lira-Nogueira, M.C.B., Maciel, M.A.V., Neves, R.P., Pimentel, M.F., Santos-Magalhães, N.S.
• Format: Article
• Language: English
• Subjects: Antimicrobial activity; Cryptococcus neoformans; Liposomes; Meticillin-resistant; MRSA; Staphylococcus aureus; β-Lapachone
• ISSN: 2213-7165; 2213-7173
• DOI: 10.1016/j.jgar.2015.03.007

•In vitro antimicrobial activity of β-lapachone (β-lap) encapsulated into liposomes was established.•Bactericidal and fungicidal activity of free and encapsulated β-lap was found against MRSA and Cryptococcus neoformans clinical strains, respectively.•Liposomal formulations do not interfere significantly with the β-lap antibacterial activity against MRSA and improve its antifungal properties against C. neoformans. The aim of this study was to determine whether encapsulation of β-lapachone (β-lap) into liposomes interferes with its in vitro antimicrobial activity against meticillin-resistant Staphylococcus aureus (MRSA) and Cryptococcus neoformans clinical strains. Liposomes (β-lap:lipo or β-lap:HPβ-CD-lipo) were prepared using the hydration of thin lipid film method followed by sonication. The in vitro antimicrobial activities of β-lap-loaded liposomes against MRSA and C. neoformans were evaluated using the microdilution method according to the Clinical and Laboratory Standards Institute (CLSI). The liposomes presented a mean particle size ranging from 88.7±1.5nm to 112.4±1.9nm with a polydispersity index ranging from 0.255 to 0.340, zeta potential from −0.26±0.01mV to +0.25±0.05mV and drug encapsulation efficiency from 97.4±0.3% to 98.9±0.4%. β-Lap and β-lap:HPβ-CD had minimum inhibitory concentrations (MICs) ranging from 2mg/L to 4mg/L, whereas the MICs of β-lap-lipo or β-lap:HPβ-CD-lipo ranged from 4mg/L to 16mg/L for the MRSA strains tested. β-Lap and β-lap:HPβ-CD were able to inhibit fungal growth [MIC=2–8mg/L and minimum fungicidal concentration (MFC)=4–8mg/L]. However, β-lap-lipo and β-lap:HPβ-CD-lipo were more efficient, with MICs and MFCs of