K88 Fimbrial Adhesin Targeting of Microspheres Containing Gentamicin Made with Albumin Glycated with Lactose

Int J Mol Sci. 2015 Sep 16;16(9):22425-37. doi: 10.3390/ijms160922425.


The formulation and characterization of gentamicin-loaded microspheres as a delivery system targeting enterotoxigenic Escherichia coli K88 (E. coli K88) was investigated. Glycated albumin with lactose (BSA-glucose-β (4-1) galactose) was used as the microsphere matrix (MS-Lac) and gentamicin included as the transported antibiotic. The proposed target strategy was that exposed galactoses of MS-Lac could be specifically recognized by E. coli K88 adhesins, and the delivery of gentamicin would inhibit bacterial growth. Lactosylated microspheres (MS-Lac1, MS-Lac2 and MS-Lac3) were obtained using a water-in-oil emulsion, containing gentamicin, followed by crosslinking with different concentrations of glutaraldehyde. Electron microscopy displayed spherical particles with a mean size of 10-17 µm. In vitro release of gentamicin from MS-Lac was best fitted to a first order model, and the antibacterial activity of encapsulated and free gentamicin was comparable. MS-Lac treatments were recognized by plant galactose-specific lectins from Ricinus communis and Sophora japonica and by E. coli K88 adhesins. Results indicate MS-Lac1, produced with 4.2 mg/mL of crosslinker, as the best treatment and that lactosylated microsphere are promising platforms to obtain an active, targeted system against E. coli K88 infections.

Keywords: gentamicin; lactosylated microspheres; targeted active drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Albumins / chemistry
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / pharmacology
  • Antigens, Bacterial / metabolism*
  • Escherichia coli / drug effects
  • Escherichia coli / metabolism
  • Escherichia coli Proteins / metabolism*
  • Fimbriae Proteins / metabolism*
  • Gentamicins / administration & dosage*
  • Gentamicins / pharmacology
  • Lactose / chemistry
  • Microspheres*
  • Plant Lectins / metabolism
  • Protein Binding


  • Albumins
  • Anti-Bacterial Agents
  • Antigens, Bacterial
  • Escherichia coli Proteins
  • Gentamicins
  • K88 antigen, E coli
  • Plant Lectins
  • Fimbriae Proteins
  • Lactose