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本研究的目的在于制备由Tat肽和麦胚凝集素修饰 (WGA) 修饰的脂质体递送系统,有效发挥抗菌效应.分别对其理化性质、耐甲氧西林金黄色葡萄球菌 (MRSA) 的最低抑菌浓度 (MIC)、杀菌动力学、细胞摄取、生物膜形成抑制以及体内抗菌效果进行评价.研究结果表明,由Tat和WGA双修饰的载克拉霉素脂质体具有最低的MIC值和杀菌曲线,流式细胞实验结果表明双修饰的脂质体可将更多的香豆素6导入细菌内部.此外,该脂质体还能有效抑制MRSA生物膜的形成.体内实验结果表明,经过双修饰脂质体给药,小鼠脓肿部位的MRSA菌落数显著低于其他组 (P＜0.01),即具有最强的体内抗菌效果.总之,由Tat和WGA修饰的脂质体递送系统希望称为有效的抗耐药菌感染的策略.“,”In this study, we developed a novel liposomal delivery system modified by Tat peptide and wheat germ agglutinin (WGA) with antimicrobial effect. Physicochemical parameters, in vitro antimicrobial, time-kill study, cellular uptake, biofilm formation inhibition and in vivo antibacterial efficacy against Methicillin-resistant Staphylococcus aureus (MRSA) were investigated. Minimum inhibitory concentrations (MICs) and colony-forming units (CFUs) in the time-kill study for Tat-WGA-modified liposomal clarithromycin (CLA-Tat WGALip) were lower than those of free and other modified liposomal CLA. Flow cytometry analysis disclosed that Tat WGALip delivered more coumarin 6 into bacteria. Furthermore, Tat-WGA-modified liposomal CLA efficiently inhibited the formation of MRSA biofiom. CFU of MRSA in the abscess of mice treated with CLA-Tat WGALip was significantly lower than that of any others (P＜0.01). Collectively, liposomal delivery system modified by Tat and WGA could be a promising anti-resistant infection strategy.