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

• Published in: International journal of molecular sciences Vol. 16; no. 9; pp. 22425 - 22437
• Main Authors: Sarabia-Sainz, Andre-I, Sarabia-Sainz, Hector Manuel, Montfort, Gabriela Ramos-Clamont, Mata-Haro, Veronica, Guzman-Partida, Ana María, Guzman, Roberto, Garcia-Soto, Mariano, Vazquez-Moreno, Luz
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 16-09-2015; MDPI
• Subjects: Albumins - chemistry; Anti-Bacterial Agents - administration & dosage; Anti-Bacterial Agents - pharmacology; Antibiotics; Antigens, Bacterial - metabolism; Drug therapy; E coli; Escherichia coli - drug effects; Escherichia coli - metabolism; Escherichia coli Proteins - metabolism; Fimbriae Proteins - metabolism; gentamicin; Gentamicins - administration & dosage; Gentamicins - pharmacology; Lactose - chemistry; lactosylated microspheres; Microspheres; Plant Lectins - metabolism; Protein Binding; targeted active drug; gentamicin; targeted active drug; lactosylated microspheres
• ISSN: 1422-0067; 1661-6596; 1422-0067
• 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.