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

作者：Wang, Xiaoyun; Wu, Fengbo; Chen, Yuyu; Qin, Feifei; Bao, Jinku^*; Chen, Guo^*

来源：Journal of Microencapsulation, 2018, 35(1): 78-89.

DOI：10.1080/02652048.2018.1425751

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

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 200.0nm, a slower and sustained release. An antibacterial experiment showed that XW-12 NPs had a lower minimal inhibitory concentration value of 1g/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.

• 出版日期2018
• 单位四川大学