title: Bactericidal Dendritic Polycation Cloaked with Stealth Material via Lipase-Sensitive Intersegment Acquires Neutral Surface Charge without Losing Membrane-Disruptive Activity.
abstract: 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.
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, §School of Chemistry and Materials Science, and ⊥CAS Key Laboratory of Materials for Energy Conversion, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Lulu
authors.initials: L
authors.lastname: Xu
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, §School of Chemistry and Materials Science, and ⊥CAS Key Laboratory of Materials for Energy Conversion, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Chen
authors.initials: C
authors.lastname: He
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, §School of Chemistry and Materials Science, and ⊥CAS Key Laboratory of Materials for Energy Conversion, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Liwei
authors.initials: L
authors.lastname: Hui
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, §School of Chemistry and Materials Science, and ⊥CAS Key Laboratory of Materials for Energy Conversion, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Yuntao
authors.initials: Y
authors.lastname: Xie
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, §School of Chemistry and Materials Science, and ⊥CAS Key Laboratory of Materials for Energy Conversion, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Jia-Min
authors.initials: JM
authors.lastname: Li
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, §School of Chemistry and Materials Science, and ⊥CAS Key Laboratory of Materials for Energy Conversion, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Wei-Dong
authors.initials: WD
authors.lastname: He
authors.affiliation: CAS Key Laboratory of Soft Matter Chemistry, §School of Chemistry and Materials Science, and ⊥CAS Key Laboratory of Materials for Energy Conversion, University of Science and Technology of China , Hefei, Anhui 230026, China.
authors.forename: Lihua
authors.initials: L
authors.lastname: Yang
mesh_terms: D023181:Antimicrobial Cationic Peptides / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects* / Q000472:pathogenicity; D050091:Dendrimers / Q000737:chemistry / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry / Q000494:pharmacology; D005026:Ethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D008049:Lipase / Q000037:antagonists & inhibitors / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry; D011091:Polyesters / Q000737:chemistry / Q000493:pharmacokinetics*; D059748:Proteolysis / Q000187:drug effects
chemical_list: D023181:Antimicrobial Cationic Peptides; D050091:Dendrimers; D004337:Drug Carriers; D005026:Ethylene Glycols; D011091:Polyesters; C476300:poly(epsilon-caprolactone)-b-poly(ethylene glycol); D008049:Lipase
keywords: antimicrobial; drug resistance; nanoparticle; stealth coating; stimulus responsive