Influence of the nanocomposite MgAl-HTlc on gastric absorption of drugs: in vitro and ex vivo studies.
OBJECTIVE
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
Firstly the effect of growing MgAl-HTlc concentrations on gastric pH was evaluated. Both drug flux across the mucus layer and 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 mucus 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.
Dipartimento di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia, Via del Liceo 1, Perugia 06123, Italy. luanaper@unipg.it
Luana
L
Perioli
Pamela
P
Mutascio
Cinzia
C
Pagano
D000535:Aluminum / Q000737:chemistry*; D000818:Animals; D004232:Diuretics / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D005665:Furosemide / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D005753:Gastric Mucosa / Q000378:metabolism*; D006878:Hydroxides / Q000737:chemistry*; D008274:Magnesium / Q000737:chemistry*; D008567:Membranes, Artificial; D053761:Nanocomposites / Q000737:chemistry*; D012212:Rheology; D012995:Solubility; D013552:Swine
D004232:Diuretics; D006878:Hydroxides; D008567:Membranes, Artificial; D005665:Furosemide; D000535:Aluminum; D008274:Magnesium