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Bactericidal Dendritic Polycation Cloaked with Stealth Material via Lipase-Sensitive Intersegment Acquires Neutral Surface Charge without Losing Membrane-Disruptive Activity.
- Source :
-
ACS applied materials & interfaces [ACS Appl Mater Interfaces] 2015 Dec 23; Vol. 7 (50), pp. 27602-7. Date of Electronic Publication: 2015 Dec 08. - Publication Year :
- 2015
-
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.
- Subjects :
- Antimicrobial Cationic Peptides chemistry
Bacteria pathogenicity
Dendrimers chemistry
Drug Carriers chemistry
Drug Carriers pharmacology
Ethylene Glycols chemistry
Humans
Lipase antagonists & inhibitors
Lipase chemistry
Nanoparticles chemistry
Polyesters chemistry
Proteolysis drug effects
Antimicrobial Cationic Peptides pharmacology
Bacteria drug effects
Dendrimers pharmacology
Ethylene Glycols pharmacokinetics
Polyesters pharmacokinetics
Subjects
Details
- Language :
- English
- ISSN :
- 1944-8252
- Volume :
- 7
- Issue :
- 50
- Database :
- MEDLINE
- Journal :
- ACS applied materials & interfaces
- Publication Type :
- Report
- Accession number :
- 26632646
- Full Text :
- https://doi.org/10.1021/acsami.5b09581