Up-take and releasing kinetics of model fluoroquinolones loaded in carbomer hydrogels

ANA P, VILCHES; FABIANA L. ALOVERO Ó F. L. ALOVERO; ALVARO F, JIMENEZ KAIRUZ; MARIA E, OLIVERA; DANIEL ALBERTO, ALLEMANDI; RUBEN HILARIO, MANZO

ELSEVIER SCIENCE BV

Año: 2002 vol. 246 p. 17 - 17

ydrogels of carbomer (C) loaded with model slightly soluble fluoroquinolone antimicrobials (AMFQ), norfloxacin (I) and ciprofloxacin (II) were prepared to evaluate their physical and delivery properties. Thus, dispersions of 0.25% of C loaded with 0.2?0.5 mol equivalents of AMFQ and 0.2?0.5 mol equivalents of NaOH yielded pseudoplastic hydrogels with a high negative electrokinetic potential and good physical stability. Concentration of AMFQ in the hydrogels was, respectively, 7.2 and 34 times higher than I and II aqueous solubility, indicating a high increase in aqueous compatibility. Release of AMFQ in bicompartimetal Franz type cell occurred by zero order kinetics. Delivery rate constant (k0) was five to six times higher as water was replaced by NaCl solution as receptor medium. Release in agar dishes revealed that, even under high dilution, delivery remains modulated. Intestinal absorption flux coefficient in everted rat intestine were measured with reference solu