Preparation and optimization of niosome encapsulated meropenem for significant antibacterial and anti-biofilm activity against methicillin-resistant Staphylococcus aureus isolates.

ABSTRACT

Background: One of the targeted drug delivery systems is the use of nanocarriers, and one of these drug delivery systems is niosome. Niosome have a nano-vesicular structure and are composed of non-ionic surfactants. Objective: In this study, various niosome-encapsulated meropenem formulations were prepared. Subsequently, their antibacterial and anti-biofilm activities were evaluated against methicillin-resistant Staphylococcus aureus (MRSA) strains. Methods: The physicochemical properties of niosomal formulations were characterized using a field scanning electron microscope, X-Ray diffraction, Zeta potential, and dynamic light scattering. Antibacterial and anti-biofilm activities were evaluated using broth microdilution and minimum biofilm inhibitory concentration, respectively. In addition, biofilm gene expression analysis was performed using quantitative Real-Time PCR. To evaluate biocompatibility, the cytotoxicity of niosome-encapsulated meropenem in a normal human diploid fibroblast (HDF) cell line was investigated using an MTT assay. Results: An F1 formulation of niosome-encapsulated meropenem with a size of 51.3 ± 5.84 nm and an encapsulation efficiency of 84.86 ± 3.14 % was achieved. The synthesized niosomes prevented biofilm capacity with a biofilm growth inhibition index of 69 % and significantly downregulated icaD, FnbA, Ebps, and Bap gene expression in MRSA strains (p < 0.05). In addition, the F1 formulation increased antibacterial activity by 4-6 times compared with free meropenem. Interestingly, the F1 formulation of niosome-encapsulated meropenem indicated cell viability >90 % at all tested concentrations against normal HDF cells. The results of the present study indicate that niosome-encapsulated meropenem increased antibacterial and anti-biofilm activities without profound cytotoxicity in normal human cells, which could prove useful as a good drug delivery system.