In transbuccal absorption a major limitation could be the low permeability of the mucosa which implies low drug bioavailability. The ability of naltrexone hydrochloride(NLX)to penetrate a resembling histologically human buccal mucosa was assessed and the occurrence of any histomorphological changes observed. We used reconstituted human oral (RHO) non-keratinised epithelium as mucosal section and a Transwell diﬀusion cells system as bicompartmental model. Buccal permeation was expressed in terms of drug ﬂux (Js) and permeability coeﬃcients (Kp). Data were collected using both artiﬁcial and natural human saliva. The main ﬁnding was that RHO does not restrain NLX permeation. Drug transport across the epithelium was observed also in presence of various concentrations of penetration enhancers, without any signiﬁcant diﬀerences. On the contrary, the ﬂux throughout the mucosa was extensively aﬀected by iontophoresis. Histologically, no sign of ﬂogosis was observed in any specimen under experiment without iontophoresis, whereas cytoarchitectural changes, up to nuclear pycnosis or cellular swelling, were determined as a consequence of the application of electric ﬁelds.
|Numero di pagine||9|
|Rivista||European Journal of Pharmaceutics and Biopharmaceutics|
|Stato di pubblicazione||Published - 2007|
All Science Journal Classification (ASJC) codes
- Pharmaceutical Science