title: Sugar-Grafted Cyclodextrin Nanocarrier as a "Trojan Horse" for Potentiating Antibiotic Activity.
abstract: OBJECTIVE
  The use of "Trojan Horse" nanocarriers for antibiotics to enhance the activity of antibiotics against susceptible and resistant bacteria is investigated.
  
  
  METHODS
  Antibiotic carriers (CD-MAN and CD-GLU) are prepared from β-cyclodextrin grafted with sugar molecules (D-mannose and D-glucose, respectively) via azide-alkyne click reaction. The sugar molecules serve as a chemoattractant enticing the bacteria to take in higher amounts of the antibiotic, resulting in rapid killing of the bacteria.
  
  
  RESULTS
  Three types of hydrophobic antibiotics, erythromycin, rifampicin and ciprofloxacin, are used as model drugs and loaded into the carriers. The minimum inhibitory concentration of the antibiotics in the CD-MAN-antibiotic and CD-GLU-antibiotic complexes for Gram-negative Escherichia coli, Pseudomonas aeruginosa and Acinetobacter baumannii strains, and a number of Gram-positive Staphylococcus aureus strains, including the methicillin-resistant strains (MRSA), are reduced by a factor ranging from 3 to >100. The CD-MAN-antibiotic complex is also able to prolong the stability of the loaded antibiotic and inhibit development of intrinsic antibiotic resistance in the bacteria.
  
  
  CONCLUSIONS
  These non-cytotoxic sugar-modfied nanocarriers can potentiate the activity of existing antibiotics, especially against multidrug-resistant bacteria, which is highly advantageous in view of the paucity of new antibiotics in the pipeline.
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore, Kent Ridge,, Singapore, 117585, Singapore.
authors.forename: Min
authors.initials: M
authors.lastname: Li
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore, Kent Ridge,, Singapore, 117585, Singapore. chenkg@nus.edu.sg.
authors.forename: Koon Gee
authors.initials: KG
authors.lastname: Neoh
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore, Kent Ridge,, Singapore, 117585, Singapore.
authors.forename: Liqun
authors.initials: L
authors.lastname: Xu
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore, Kent Ridge,, Singapore, 117585, Singapore.
authors.forename: Liang
authors.initials: L
authors.lastname: Yuan
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore, Kent Ridge,, Singapore, 117585, Singapore.
authors.forename: David Tai
authors.initials: DT
authors.lastname: Leong
authors.affiliation: Department of Chemical and Biomolecular Engineering, National University of Singapore, Kent Ridge,, Singapore, 117585, Singapore.
authors.forename: En-Tang
authors.initials: ET
authors.lastname: Kang
authors.affiliation: Department of Biochemistry, National University of Singapore, Kent Ridge,, Singapore, 117543, Singapore.
authors.forename: Kim Lee
authors.initials: KL
authors.lastname: Chua
authors.affiliation: Department of Medicine, National University of Singapore, Kent Ridge, Singapore, 119228, Singapore.
authors.forename: Li Yang
authors.initials: LY
authors.lastname: Hsu
mesh_terms: D040981:Acinetobacter baumannii / Q000187:drug effects; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy*; D002939:Ciprofloxacin / Q000008:administration & dosage / Q000494:pharmacology; D057930:Click Chemistry; D004337:Drug Carriers / Q000737:chemistry* / Q000378:metabolism; D024881:Drug Resistance, Bacterial; D004917:Erythromycin / Q000008:administration & dosage / Q000494:pharmacology; D005947:Glucose / Q000031:analogs & derivatives* / Q000378:metabolism; D006801:Humans; D008358:Mannose / Q000031:analogs & derivatives* / Q000378:metabolism; D008826:Microbial Sensitivity Tests; D012293:Rifampin / Q000008:administration & dosage / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D047392:beta-Cyclodextrins / Q000737:chemistry* / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D047392:beta-Cyclodextrins; D002939:Ciprofloxacin; D004917:Erythromycin; D005947:Glucose; C031215:betadex; D008358:Mannose; D012293:Rifampin
keywords: antibacterial; antibiotic nanocarrier; glucose; mannose; β-cyclodextrin