Rifampin and Cis-2-Decenoic Acid Co-entrapment in Solid Lipid Nanoparticles as an Efficient Nano-system with Potent Anti-biofilm Activities

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