Purpose: Furosemide (FURO) is a BCS class IV drug preferentially absorbed in the gastric environment. A previous study demonstrated that its intercalation into the lamellar inorganic matrix MgAl-HTlc, giving rise to MgAl-HTlc-FURO, improves its dissolution in acidic medium. As the gastric absorption of drugs can be hindered from the biological barriers mucus and gastric mucosa, the purpose of this work was to evaluate the effect of MgAl-HTlc on gastric pH, the possible modifications induced on mucus rheology and the influence on both artificial and biological membranes. Methods: First the effect of growing MgAl-HTlc concentrations on gastric pH has been evaluated. Drug flux across the mucus layer and drug permeability across an artificial and biological membrane (gastric mucosa) have been studied as well. Results: The results highlighted that drug flux across gastric mucus is improved in presence of MgAl-HTlc-FURO and that MgAl-HTlc is able to modify drug structure in a reversible manner. From permeability studies emerged that the use of a biological membrane is the most suitable for such studies and that MgAl-HTlc-FURO enhances FURO Papp. Conclusions: Data obtained suggest that MgAl-HTlc is a suitable material able to improve the biopharmaceutical properties of class IV BCS drugs.

Influence of the nanocomposite MgAl-hydrotalcite on gastric absorption of drugs: in vitro and ex vivo studies.

PERIOLI, Luana
;
PAGANO, CINZIA
2013

Abstract

Purpose: Furosemide (FURO) is a BCS class IV drug preferentially absorbed in the gastric environment. A previous study demonstrated that its intercalation into the lamellar inorganic matrix MgAl-HTlc, giving rise to MgAl-HTlc-FURO, improves its dissolution in acidic medium. As the gastric absorption of drugs can be hindered from the biological barriers mucus and gastric mucosa, the purpose of this work was to evaluate the effect of MgAl-HTlc on gastric pH, the possible modifications induced on mucus rheology and the influence on both artificial and biological membranes. Methods: First the effect of growing MgAl-HTlc concentrations on gastric pH has been evaluated. Drug flux across the mucus layer and drug permeability across an artificial and biological membrane (gastric mucosa) have been studied as well. Results: The results highlighted that drug flux across gastric mucus is improved in presence of MgAl-HTlc-FURO and that MgAl-HTlc is able to modify drug structure in a reversible manner. From permeability studies emerged that the use of a biological membrane is the most suitable for such studies and that MgAl-HTlc-FURO enhances FURO Papp. Conclusions: Data obtained suggest that MgAl-HTlc is a suitable material able to improve the biopharmaceutical properties of class IV BCS drugs.
2013
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11391/988981
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 23
  • ???jsp.display-item.citation.isi??? 20
social impact