Abstract
Purpose: Improving solubility and antibacterial efficiency of cephalothin by using silica-containing redox nanoparticle (siRNP) as a system to encapsulate and deliver this hydrophobic antibiotic.
 Methods: siRNP was synthesized by assembling amphiphilic block copolymers possessing a reactive oxygen species scavenging nitroxide radical and drug absorptive silica moieties in a hydrophobic side chain. Cephalothin, a hydrophobic antibiotic, was encapsulated into siRNP (cephalothin@siRNP) by mixing and dialysis methods. Antibacterial activity of cephalothin@siRNP against Staphylococcus aureus (S. aureus) và Escherichia coli (E. coli) was evaluated by the agar diffusion method.
 Results: The average size of siRNP and cephalothin@siRNP was 43.83 nm and 50.15 nm, respectively. After encapsulation in siRNP, the solubility of cephalothin was improved compared to cephalothin in an aqueous solution. The result showed that in vitro antibacterial activities of cephalothin and cephalothin@siRNP had no statistical difference after 24 h incubation on agar plates on both S. aureus and E. coli. However, after an extended incubation time, regrowth of E. coli colonies in the inhibitory zone was found in cephalothin treated plate. Interestingly, E. coli regrowth was significantly reduced in plates treated with cephalothin@siRNP.
 Conclusion: In this study, siRNP successfully encapsulated cephalothin and enhanced the solubility of this drug. The antibacterial activity of cephalothin is prolonged when encapsulated in siRNP, which suppressed the reccurrence of E. coli colonies. Cephalothin@siRNP has the potential to inhibit antibiotic resistance.
Highlights
Nowadays, indiscriminate use of antibiotics has increased the uncontrollable development of many multidrug resistance (MDR) bacteria, becoming one of the most dangerous threats to public health
The results showed that silica-containing redox nanoparticle (siRNP) had antioxidant activity and this activity was derived from the tempo radical attached in the core of nanoparticle
These results suggested that siRNP can be utilized as a drug nanocarrier and as an antioxidant agent, which may improve the therapeutic efficacy of the loaded antibiotics
Summary
Indiscriminate use of antibiotics has increased the uncontrollable development of many multidrug resistance (MDR) bacteria, becoming one of the most dangerous threats to public health. Many types of antibiotics have been developed, demand for antibacterial infection treatment are still an urgent need as the number of resistance of bacterial strains is increasing 2. Under microbial infection , inflammatory response and the use of antibiotics induce ROS overproduction. ROS overproduction might induce gene mutation, which activated the bacterial antibiotic resistance mechanism 4. Developing new efficacy antibacterial method to improve bioavailability is urgently necessary. We developed silica-contaning redox nanoparticle (siRNP) with ROS scavening from nitroxide radical and drug absorption silica moieties in the core of the nanoparticle 7. Silica moieties form cross-linking to stabilize the structure of the
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