Abstract
Nanoparticles have become a focus of interest due to their ability as antibacterial agents. The aim of this study was to evaluate the anti-methicillin-resistant Staphylococcus aureus (MRSA) activity of cationic nanostructured lipid carriers (NLC) combined with oxacillin against ATCC 33591 and clinical isolate. The cationic resource on the NLC surface was soyaethyl morpholinium ethosulfate (SME). NLC loaded with oxacillin was produced to assess the antibacterial activity and the effectiveness of topical application for treating cutaneous infection. The hydrodynamic diameter and zeta potential of oxacillin-loaded NLC were 177 nm and 19 mV, respectively. When combined with NLC, oxacillin exhibited synergistic MRSA eradication. After NLC encapsulation, the minimum bactericidal concentration (MBC) of oxacillin decreased from 250 to 62.5 μg/ml. The combined NLC and oxacillin reduced the MRSA biofilm thickness from 31.2 to 13.0 μm, which was lower than the effect of NLC (18.2 μm) and antibiotic (25.2 μm) alone. The oxacillin-loaded NLC showed significant reduction in the burden of intracellular MRSA in differentiated THP-1 cells. This reduction was greater than that achieved with individual treatment. The mechanistic study demonstrated the ability of cationic NLC to disrupt the bacterial membrane, leading to protein leakage. The cell surface disintegration also increased oxacillin delivery into the cytoplasm, activating the bactericidal process. Topical NLC treatment of MRSA abscess in the skin decreased the bacterial load by log 4 and improved the skin’s architecture and barrier function. Our results demonstrated that a combination of nanocarriers and an antibiotic could synergistically inhibit MRSA growth.
Highlights
The growing amount of drug-resistant strains has become a serious health threat, especially the methicillin-resistant Staphylococcus aureus (MRSA) (Tong et al, 2015)
We proposed that oxacillin was entrapped in the inner core of nanostructured lipid carriers (NLC), whereas soyaethyl morpholinium ethosulfate (SME) was intercalated in the emulsifier layer
We achieved the synergism of anti-MRSA activity by combining NLC and antibiotic according to the minimum bactericidal concentration (MBC) profile of oxacillin
Summary
The growing amount of drug-resistant strains has become a serious health threat, especially the methicillin-resistant Staphylococcus aureus (MRSA) (Tong et al, 2015). Some MRSA strains are even resistant to second-line treatment such as vancomycin and doxycycline (Cihalova et al, 2015). The skin is the major organ infected by MRSA (Dréno et al, 2016). Topical application can be an efficient route to administer antibiotics for direct MRSA eradication. 6 antibacterial agents have been approved by the USFDA for MRSA management. Since none of these drugs is used for topical treatment (Rodvold and McConeghy, 2014), the development of new anti-MRSA agents for cutaneous use is urgently needed
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