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
Laboratório de Imunopatologia Keizo-Asami (LIKA), Universidade Federal de Pernambuco (UFPE), Av. Prof. Moraes Rego 1235, Cidade Universitária, 50670-901 Recife, PE, Brazil; Centro Acadêmico de Vitória (CAV), UFPE, Vitória de Santo Antão, PE, Brazil.
Laboratório de Imunopatologia Keizo-Asami (LIKA), Universidade Federal de Pernambuco (UFPE), Av. Prof. Moraes Rego 1235, Cidade Universitária, 50670-901 Recife, PE, Brazil.
J Glob Antimicrob Resist. 2015 Jun;3(2):103-108. doi: 10.1016/j.jgar.2015.03.007. Epub 2015 Apr 30.
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 <4mg/L. These findings suggest that the liposomal formulations tested do not interfere significantly with β-lap antibacterial activity against MRSA and improve its antifungal properties against C. neoformans.
本研究的目的是确定将β-拉帕醌(β-lap)包裹于脂质体中是否会干扰其对耐甲氧西林金黄色葡萄球菌(MRSA)和新型隐球菌临床菌株的体外抗菌活性。采用薄膜水化法并经超声处理制备脂质体(β-lap:lipo或β-lap:HPβ-CD-lipo)。根据临床和实验室标准协会(CLSI)的方法,采用微量稀释法评估负载β-lap的脂质体对MRSA和新型隐球菌的体外抗菌活性。脂质体的平均粒径为88.7±1.5nm至112.4±1.9nm,多分散指数为0.255至0.340,ζ电位为-0.26±0.01mV至+0.25±0.05mV,药物包封率为97.4±0.3%至98.9±0.4%。β-Lap和β-lap:HPβ-CD的最低抑菌浓度(MIC)为2mg/L至4mg/L,而对于所测试的MRSA菌株,β-lap-lipo或β-lap:HPβ-CD-lipo的MIC为4mg/L至16mg/L。β-Lap和β-lap:HPβ-CD能够抑制真菌生长[MIC=2-8mg/L,最低杀菌浓度(MFC)=4-8mg/L]。然而,β-lap-lipo和β-lap:HPβ-CD-lipo的效果更佳,MIC和MFC均<4mg/L。这些研究结果表明,所测试的脂质体制剂不会显著干扰β-lap对MRSA的抗菌活性,且能提高其对新型隐球菌的抗真菌特性。