title: Release of naltrexone on buccal mucosa: permeation studies, histological aspects and matrix system design.
abstract: Transbuccal drug delivery has got several well-known advantages especially with respect to peroral way. Since a major limitation in buccal drug delivery could be the low permeability of the epithelium, the aptitude of NLX to penetrate the mucosal barrier was assessed. Ex vivo permeation across porcine buccal mucosa 800 microm thick was investigated using Franz type diffusion cells and compared with in vitro data previously obtained by reconstituted human oral epithelium 100 microm thick. Both fluxes (Js) and permeability coefficients (K(p)) are in accordance, using either buffer solution simulating saliva or natural human saliva. Permeation was evaluated also in presence of chemical enhancers or iontophoresis. No significant differences in penetration rate were observed using chemical enhancers; in contrast, Js and K(p) were extensively affected by application of electric fields. Tablets, designed for Naltrexone hydrochloride (NLX) administration on buccal mucosa, were developed and prepared by direct compression of drug loaded (56%) poly-octylcyanocrylate (poly-OCA) matrices. NLX is slowly discharged from buccal tablets following Higuchian kinetic. Histologically, no signs of flogosis ascribable to NLX and/or poly-OCA were observed, while cytoarchitectural changes due to iontophoresis were detected. Buccal tablets containing NLX may represent a potential alternative dosage form in addiction management.
authors: Dipartimento di Chimica e Tecnologie Farmaceutiche, Università di Palermo, Palermo, Italy. litagian@unipa.it
authors: Libero Italo
authors: LI
authors: Giannola
authors: Viviana
authors: V
authors: De Caro
authors: Giulia
authors: G
authors: Giandalia
authors: Maria Gabriella
authors: MG
authors: Siragusa
authors: Claudio
authors: C
authors: Tripodo
authors: Ada Maria
authors: AM
authors: Florena
authors: Giuseppina
authors: G
authors: Campisi
mesh_terms: D000278:Administration, Buccal; D000818:Animals; D002626:Chemistry, Pharmaceutical; D004333:Drug Administration Routes; D016503:Drug Delivery Systems / Q000379:methods; D005557:Formaldehyde / Q000737:chemistry; D007478:Iontophoresis; D007700:Kinetics; D009061:Mouth Mucosa / Q000187:drug effects*; D009271:Naltrexone / Q000008:administration & dosage* / Q000493:pharmacokinetics; D009292:Narcotic Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D013055:Spectrophotometry, Infrared; D013552:Swine; D013607:Tablets; D013997:Time Factors
chemical_list: D009292:Narcotic Antagonists; D013607:Tablets; D005557:Formaldehyde; D009271:Naltrexone