Virus-inspired surface-nanoengineered antimicrobial liposome:A potential system to simultaneously achieve high activity and selectivity  

作　　者：Yin Shi Xiaoqian Feng Liming Lin Jing Wang Jiaying Chi Biyuan Wu Guilin Zhou Feiyuan Yu Qian Xu Daojun Liu Guilan Quan Chao Lu Xin Pan Jianfeng Cai Chuanbin Wu 

机构地区：[1]College of Pharmacy,Jinan University,Guangzhou,Guangdong,511443,China [2]Department of Pharmaceutics,School of Pharmaceutical Sciences,Sun Yat-Sen University,Guangzhou,Guangdong,510006,China [3]Medical College,Shantou University,Shantou,Guangdong,15041,China [4]Department of Chemistry,University of South Florida,Tampa,FL,33620,United States

出　　处：《Bioactive Materials》2021年第10期3207-3217,共11页生物活性材料（英文）

基　　金：This work was financially supported by the National Natural Science Foundation of China(No.81803467,81773660);the Research and Development Plan for Key Areas in Guangdong Province(No.2019B020204002).

摘　　要：Enveloped viruses such as SARS-CoV-2 frequently have a highly infectious nature and are considered effective natural delivery systems exhibiting high efficiency and specificity.Since simultaneously enhancing the activity and selectivity of lipopeptides is a seemingly unsolvable problem for conventional chemistry and pharmaceutical approaches,we present a biomimetic strategy to construct lipopeptide-based mimics of viral architectures and infections to enhance their antimicrobial efficacy while avoiding side effects.Herein,a surface-nanoengineered antimicrobial liposome(SNAL)is developed with the morphological features of enveloped viruses,including a moderate size range,lipid-based membrane structure,and highly lipopeptide-enriched bilayer surface.The SNAL possesses virus-like infection to bacterial cells,which can mediate high-efficiency and high-selectivity bacteria binding,rapidly attack and invade bacteria via plasma membrane fusion pathway,and induce a local“burst”release of lipopeptide to produce irreversible damage of cell membrane.Remarkably,viral mimics are effective against multiple pathogens with low minimum inhibitory concentrations(1.6-6.3μg mL1),high bactericidal efficiency of>99%within 2 h,>10-fold enhanced selectivity over free lipopeptide,99.8%reduction in skin MRSA load after a single treatment,and negligible toxicity.This bioinspired design has significant potential to enhance the therapeutic efficacy of lipopeptides and may create new opportunities for designing next-generation antimicrobials.

关 键 词：Virus-inspired mimics Antimicrobial lipopeptides Liposomes Virus-like infections Activity and selectivity 

分 类 号：R318[医药卫生—生物医学工程]