Barakat Heba S, Kassem Mervat A, El-Khordagui Labiba K, Khalafallah Nawal M
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, 1 Khartoum Square, Azarita, Alexandria, 21521, Egypt,
AAPS PharmSciTech. 2014 Oct;15(5):1263-74. doi: 10.1208/s12249-014-0141-8. Epub 2014 Jun 4.
A new vancomycin (VCM)-eluting mixed bilayer niosome formulation was evaluated for the control of staphylococcal colonization and biofilm formation on abiotic surfaces, a niosome application not explored to date. Cosurfactant niosomes were prepared using a Span 60/Tween 40/cholesterol blend (1: 1: 2). Tween 40, a polyethoxylated amphiphile, was included to enhance VCM entrapment and confer niosomal surface properties precluding bacterial adhesion. VCM-eluting niosomes showed good quality attributes including relatively high entrapment efficiency (∼50%), association of Tween 40 with vesicles in a constant proportion (∼87%), biphasic release profile suitable for inhibiting early bacterial colonization, and long-term stability at 4°C for a 12-month study period. Niosomes significantly enhanced VCM activity against planktonic bacteria of nine staphylococcal strains. Using microtiter plates as abiotic surface, VCM-eluting niosomes proved superior to VCM in inhibiting biofilm formation, eradicating surface-borne biofilms, inhibiting biofilm growth, and interfering with biofilm induction by VCM subminimal inhibitory concentrations. Data suggest dual functionality of cosurfactant VCM-eluting niosomes as passive colonization inhibiting barrier and active antimicrobial-controlled delivery system, two functions recognized in infection control of abiotic surfaces and medical devices.
一种新型的万古霉素(VCM)洗脱混合双层脂质体配方被用于评估其对非生物表面葡萄球菌定植和生物膜形成的控制效果,脂质体的这种应用在之前尚未被探索过。使用Span 60/吐温40/胆固醇混合物(1:1:2)制备了助表面活性剂脂质体。加入吐温40这种聚乙氧基化两亲物,以提高VCM的包封率,并赋予脂质体表面特性以防止细菌粘附。VCM洗脱脂质体表现出良好的质量属性,包括相对较高的包封效率(约50%)、吐温40与囊泡以恒定比例结合(约87%)、适合抑制早期细菌定植的双相释放曲线,以及在4°C下12个月研究期内的长期稳定性。脂质体显著增强了VCM对9种葡萄球菌菌株浮游菌的活性。使用微量滴定板作为非生物表面,VCM洗脱脂质体在抑制生物膜形成、根除表面生物膜、抑制生物膜生长以及干扰VCM亚最小抑菌浓度诱导生物膜方面被证明优于VCM。数据表明,助表面活性剂VCM洗脱脂质体具有双重功能,既是被动的定植抑制屏障,又是主动的抗菌控释系统,这两种功能在非生物表面和医疗器械的感染控制中都得到认可。