A new approach to improve gastric solubility and control intestinal release of drugs, based on the formation of new nanostructured compounds, is described. The nanostructured system is an inorganic-organic hybrid material constituted by an inorganic material, belonging to the hydrotalcite-like compound (HTlc), and by flurbiprofen (FLUR), a nonsteroidal antiinflammatory drug belonging to class II of BCS. HTlc is a inorganic solid able to lodge molecular anions into its interlayer region. It dissolves in acid conditions releasing the guests in the medium generating a supersaturation state. On the contrary, it is very stable in neutral or slightly alkaline conditions releasing the intercalated anions by ion exchange. This article describes: i) the nanocomposite (HTlc-FLUR) preparation and characterization; ii) the capability of HTlc to modify FLUR release, both in gastric and intestinal media; and iii) the ability of HTlc to modify FLUR gastric mucus permeation. A remarkable improvement of drug apparent solubility in gastric fluid, an enhancement of gastric mucus permeation and a drug controlled release in intestinal environment were observed
Effects of hydrotalcite-like nanostructured compounds on biopharmaceutical properties and release of BCS class II drugs: the case of flurbiprofen
PERIOLI, Luana;AMBROGI, Valeria;NOCCHETTI, Morena;ROSSI, Carlo
2011
Abstract
A new approach to improve gastric solubility and control intestinal release of drugs, based on the formation of new nanostructured compounds, is described. The nanostructured system is an inorganic-organic hybrid material constituted by an inorganic material, belonging to the hydrotalcite-like compound (HTlc), and by flurbiprofen (FLUR), a nonsteroidal antiinflammatory drug belonging to class II of BCS. HTlc is a inorganic solid able to lodge molecular anions into its interlayer region. It dissolves in acid conditions releasing the guests in the medium generating a supersaturation state. On the contrary, it is very stable in neutral or slightly alkaline conditions releasing the intercalated anions by ion exchange. This article describes: i) the nanocomposite (HTlc-FLUR) preparation and characterization; ii) the capability of HTlc to modify FLUR release, both in gastric and intestinal media; and iii) the ability of HTlc to modify FLUR gastric mucus permeation. A remarkable improvement of drug apparent solubility in gastric fluid, an enhancement of gastric mucus permeation and a drug controlled release in intestinal environment were observedI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.