Kefiran-alginate gel microspheres for oral delivery of ciprofloxacin

BLANDON LM; NOSEDA MD; ISLAN GA; THOMAZ-SOCCOL V; CASTRO GR; SOCCOL CR

COLLOIDS AND SURFACES B-BIOINTERFACES

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2016 p. 706 - 715

0927-7765

Ciprofloxacin is a broad-spectrum antibiotic associated with gastric and intestinalside effects after extended oral administration. Alginate is a biopolymer commonlyemployed in gel synthesis by ionotropic gelation, but unstable in the presence of biologicalmetal-chelating compounds and/or under dried conditions. Kefiran is a microbialbiopolymer able to form gels with the advantage of displaying antimicrobial activity. In thepresent study, kefiran-alginate gel microspheres were developed to encapsulateciprofloxacin for antimicrobial controlled release and enhanced bactericidal effect againstcommon pathogens. Scanning electron microscopy (SEM) analysis of the hybrid gelmicrospheres showed a spherical structure with a smoother surface compared to alginategel matrices. In vitro release of ciprofloxacin from kefiran-alginate microspheres was lessthan 3.0% and 5.0% at pH 1.2 (stomach), and 5.0% and 25.0% at pH 7.4 (intestine) in 3 and21 h, respectively. Infrared spectroscopy (FTIR) of ciprofloxacin-kefiran showed thedisplacement of typical bands of ciprofloxacin and kefiran, suggesting a cooperativeinteraction by hydrogen bridges between both molecules. Additionally, the thermal analysisof ciprofloxacin-kefiran showed a protective effect of the biopolymer against ciprofloxacindegradation at high temperatures. Finally, antimicrobial assays of E. coli, K. pneumoniae,P. aeruginosa, S. typhymurium, and S. aureus demonstrated the synergic effect betweenciprofloxacin and kefiran against the tested microorganisms.