Influence of the Nanocomposite MgAl-HTlc on Gastric Absorption of Drugs: In Vitro and Ex Vivo Studies
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.
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.
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.
Data obtained suggest that MgAl-HTlc is a suitable material able to improve the biopharmaceutical properties of class IV BCS drugs.
KEY WORDSgastric mucosa hydrotalcite mucus Papp viscoelasticity
ACKNOWLEDGMENTS AND DISCLOSURES
Authors are very grateful to Dr. Simonetta De Angelis and Dr. Elvio Capecci from ASL N. 1 (Città di Castello, Perugia, Italy), for providing pig samples. Special tanks are due to Mr. Marco Marani, from the Department of Chimica e Tecnologia del Farmaco, for his collaboration and technical assistance.
- 3.Lipinski C. Poor aqueous solubility—an industry wide problem in drug delivery. Am Pharm Rev. 2002;5:82–5.Google Scholar
- 5.Hauss D. Oral lipid based formulations: enhancing the bioavailability of poorly water-soluble drugs. 1st ed. New York: Informa Healthcare, Marcel Dekker; 2007.Google Scholar
- 33.Perioli L, Ambrogi V, Pagano C, Massetti E, Tiralti MC, Nocchetti M, et al. Nanostructured compounds to improve biopharmaceutical properties of drugs. 7th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology, Malta Valletta 8th–11th March 2010.Google Scholar
- 44.Schnaare RL, Block LH, Rohanin LC. Rheology. In: Troy DB, editor. Remington. The science and practice of pharmacy. 21st ed. Baltimore: Lippincott Williams & Wilkins; 2005. p. 350–1.Google Scholar