Innovative Engineering Research Center of Veterinary Pharmaceutics, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, China.
Innovative Engineering Research Center of Veterinary Pharmaceutics, College of Veterinary Medicine, Sichuan Agricultural University, Chengdu, 611130, China.
Colloids Surf B Biointerfaces. 2019 Oct 1;182:110323. doi: 10.1016/j.colsurfb.2019.06.053. Epub 2019 Jul 6.
Staphylococcus aureus (S. aureus) has the propensity to form biofilms, which eventually cause antibiotic resistance and treatment failure. Cefquinome sulfate (CS) is an animal-specific antibacterial agent for S. aureus infection. In this work, CS cationic proliposomes (CSCPs) were prepared by solid-dispersion method combined with effervescent hydration to eradicate bacterial biofilm and improve the antibacterial effect of the drug. CSCPs were readily dispersed in water, thereby forming CS cationic liposomes (CSCLs) as a white, uniform suspension. The CSCLs had an encapsulation efficiency (EE) of 63.21%, a drug loading of 4.04%, an average particle size of 201.5 nm, and a positive zeta-potential of 65.29 mV. In vitro release studies showed that CSCLs had good sustained-release behavior. The CS and CSCL minimal inhibitory concentration (MIC) of S. aureus type culture strain were 1 and 0.48 g/mL, respectively. The eradication effect of CS on bacterial biofilm (BBF) was relatively weak during culture in drug-containing medium for 8 h-24 h. However, the CSCL eradication effect on BBF increased gradually, and the clearance rate of CSCLs on BBF was about twice that of CS. The clearance rate reached 81.30% with 2.5 × MIC in 24 h. All these results indicated that CSCLs can significantly improve the eradication effect of cefquinome on biofilm to inhibit bacterial growth.
金黄色葡萄球菌（S. aureus）具有形成生物膜的倾向，这最终导致抗生素耐药性和治疗失败。硫酸头孢喹肟（CS）是一种专门用于治疗金黄色葡萄球菌感染的动物用抗菌剂。在这项工作中，采用固体分散法结合发酵水合作用制备 CS 阳离子前体脂质体（CSCPs）以根除细菌生物膜并提高药物的抗菌效果。CSCPs 容易分散在水中，从而形成 CS 阳离子脂质体（CSCLs）作为白色均匀的悬浮液。CSCLs 的包封效率（EE）为 63.21%，载药量为 4.04%，平均粒径为 201.5nm，zeta 电位为 65.29mV。体外释放研究表明 CSCLs 具有良好的缓释行为。CS 和 CSCLs 对金黄色葡萄球菌标准培养株的最小抑菌浓度（MIC）分别为 1 和 0.48g/mL。在含有药物的培养基中培养 8-24 小时时，CS 对细菌生物膜（BBF）的消除作用相对较弱。然而，CSCL 对 BBF 的消除作用逐渐增加，CSCL 对 BBF 的清除率约为 CS 的两倍。在 24 小时内用 2.5×MIC 时清除率达到 81.30%。所有这些结果表明，CSCLs 可以显著提高头孢喹肟对生物膜的消除作用，抑制细菌生长。
