Modelling drug release from a layered double hydroxide-ibuprofen complex

RICARDO ROJAS; M. CELESTE PALENA; ALVARO JIMÉNEZ-KAIRUZ; RUBEN H. MANZO; CARLA E. GIACOMELLI

APPLIED CLAY SCIENCE

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2012 vol. 62-6 p. 15 - 20

0169-1317

Drug delivery by layered double hydroxides (LDHs) is extensively studied due to the capacity of these solids to preserve the active agent and to modify its release rate and bioavailability. In this work, an ibuprofen-LDH complex was synthesized with high drug content (54 % w/w), incorporated both in the interlayer and on the surface. The mechanisms involved in the ibuprofen release process were studied as a function of the anion type (chloride, acetate, and phosphate) and concentration, and the pH of the release media. The experimental conditions selected were based on the composition of pharmaceutically relevant fluids such as gastric, intestinal and lysosomal simulated media. Three release mechanisms accounted for the rate and extent of the drug release: ion exchange (highly dependent on the anions), desorption and weathering (dependent on the pH). These mechanisms,together with the different solubility of the anionic and non-ionic ibuprofen species, also explained the release behavior for particulate solid and hydrogel formulations. Anion exchange determined ibuprofen release in intestinal medium (phosphate anions pH 6.8) whereas surface reactions mediated by solid weathering or drug solubility ruled the release in acid media (gastric fluid and lysosomal medium).