Purpose

This study was performed to explore the physicochemical and anti-biofilm properties of rifampin (Rif) and cis-2-decenoic acid (C2DA) co-entrapped in solid lipid nanoparticles, Rif-C2DA-SLN, against staphylococcal biofilm.

Methods

The formulation was prepared by high-shear homogenization and ultrasound methods and characterized for size, zeta potentials, encapsulation efficacy, drug lipid interaction studies (DSC), shape morphology (TEM), stability studies, and in vitro anti-biofilm activity against Staphylococcus aureus and S. epidermidis biofilm.

Results

The zeta potentials, particle sizes, and encapsulation efficacy of final formulations were 19.0 ± 7.64 mV, 127.2 ± 2.8 nm, and approximately 69% (Rif) and 46% (C2DA), respectively. SLN formulations were stable for 12 months. DSC studies showed no chemical interaction between drugs and lipids. SLN formulations showed better in vitro anti-biofilm activity than free forms especially in the stage of biofilm formation. Nanoparticles were not able to remove the formed biofilm.

Conclusions

Simultaneous entrapment of Rif and C2DA by SLN is reported for the first time, and Rif-C2DA-SLN can be applied as an efficient nanoparticulate system with potential anti-biofilm activities. These data suggest that the combined strategies for delivery of both C2DA and Rif by nanoparticulate systems would pave the way toward developing the strategies to combat biofilms.

The SLN formulations of antibacterial agents have better anti-biofilm activities with respect to the free form of them against bacterial biofilm.

中文翻译：

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利福平和顺式-2-癸酸在固体脂质纳米颗粒中的共包埋作为高效的具有强抗生物膜活性的纳米系统

目的

进行这项研究是为了探讨利福平（Rif）和顺式-2-癸烯酸（C2DA）共同包裹在固体脂质纳米颗粒Rif-C2DA-SLN中对葡萄球菌生物膜的理化和抗生物膜特性。

方法

通过高剪切均质化和超声方法制备该制剂，并针对大小，ζ电位，包封功效，药物脂质相互作用研究（DSC），形状形态（TEM），稳定性研究以及针对金黄色葡萄球菌的体外抗生物膜活性进行了表征。和表皮葡萄球菌生物膜。

结果

最终制剂的ζ电势，粒度和包封功效分别为19.0±7.64 mV，127.2±2.8 nm和大约69％（Rif）和46％（C2DA）。SLN配方稳定12个月。DSC研究表明，药物与脂质之间没有化学相互作用。SLN制剂显示出比游离形式更好的体外抗生物膜活性，尤其是在生物膜形成阶段。纳米颗粒不能去除形成的生物膜。

结论

首次报道了SLN同时捕获Rif和C2DA，并且Rif-C2DA-SLN可以用作具有潜在抗生物膜活性的高效纳米颗粒系统。这些数据表明，通过纳米颗粒系统同时递送C2DA和Rif的联合策略将为开发对抗生物膜的策略铺平道路。

抗菌剂的SLN制剂相对于它们对细菌生物膜的游离形式具有更好的抗生物膜活性。