Bactericidal Dendritic Polycation Cloaked with Stealth Material via Lipase-Sensitive Intersegment Acquires Neutral Surface Charge without Losing Membrane-Disruptive Activity

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• 作者：Lulu Xu ; Chen He ; Liwei Hui ; Yuntao Xie ; Jia-Min Li ; Wei-Dong He ; Lihua Yang
• 刊名：ACS Applied Materials & Interfaces
• 出版年：2015
• 出版时间：December 23, 2015
• 年：2015
• 卷：7
• 期：50
• 页码：27602-27607
• 全文大小：387K
• ISSN：1944-8252

文摘

Net cationicity of membrane-disruptive antimicrobials is necessary for their activity but may elicit immune attack when administered intravenously. By cloaking a dendritic polycation (G2) with poly(caprolactone-b-ethylene glycol) (PCL-b-PEG), we obtain a nanoparticle antimicrobial, G2-g-(PCL-b-PEG), which exhibits neutral surface charge but kills >99.9% of inoculated bacterial cells at ≤8 μg/mL. The observed activity may be attributed PCL’s responsive degradation by bacterial lipase and the consequent exposure of the membrane-disruptive, bactericidal G2 core. Moreover, G2-g-(PCL-b-PEG) exhibits good colloidal stability in the presence of serum and insignificant hemolytic toxicity even at ≥2048 μg/mL. suggesting good blood compatibility required for intravenous administration.