Novel pogostone analogous XW-12-loading nanoparticles display enhanced systematic activity against methicillin-resistant Staphylococcus aureus

Abstract

Pogostone analogous XW-12 displays an inhibitory effect on Staphylococcus aureus. However, the insolubility of the compound has restricted its further applications. This work aims to improve the water-solubility of XW-12, we used previously synthesised pogostone derivatives XW-12, forming nanoparticles with PLGA-PEG by a single-emulsion solvent-evaporation technique. Characterisations of XW-12 nanoparticles were performed. The in vitro and in vivo experiments confirmed its antimicrobial efficacy and toxicity. The results revealed that the XW-12 NPs had a particle size of approximately 200.0 nm, a slower and sustained release. An antibacterial experiment showed that XW-12 NPs had a lower minimal inhibitory concentration value of 1 μg/mL. In the mouse systemic infection model of MRSA, XW-12 NPs indicated high antibacterial activity. In addition, in vivo, toxicity studies declared that XW-12 NPs had a low cytotoxicity. Therefore, this study suggested that XW-12 NPs may be a great potential antibacterial agent in the treatment of clinical MRSA infection.

Keywords:

• Pogostone analogous
• XW-12 nanoparticles
• MRSA
• antibacterial activity
• pharmacological and toxicity in vivo

Acknowledgements

We wish to acknowledge the College of Life Sciences, Sichuan University and State Key Laboratory of Biotherapy/Collaborative Innovation Center for Biotherapy, West China Hospital, Sichuan University. Xingjun Cheng and Mao Lian (State Key Laboratory of Biotherapy/Collaborative Innovation Center for Biotherapy, West China Hospital, Sichuan University) are acknowledged for their help with the experiments.

Disclosure statement

The authors report no conflict of interest in this work.

Additional information

Funding

We are grateful for financial support from the National High Technology Research and Development Program of China (863 Program, 2015AA020905).