Release of naltrexone on buccal mucosa: Permeation studies, histological aspects and matrix system design

6533b86ffe1ef96bd12ce753

RESEARCH PRODUCT

Release of naltrexone on buccal mucosa: Permeation studies, histological aspects and matrix system design

Viviana De Caro Giuseppina Campisi Giulia Giandalia Maria Gabriella Siragusa Ada Maria Florena Claudio Tripodo Libero Italo Giannola

subject

Naltrexone Hydrochloride Time Factors Spectrophotometry Infrared Swine Chemistry Pharmaceutical Narcotic Antagonists Pharmaceutical Science Pharmacology Dosage form Drug Delivery Systems Formaldehyde Animals permeation studie NLX Iontophoresis Chemistry Narcotic antagonist Drug Administration Routes Mouth Mucosa Administration Buccal system design.General Medicine Buccal administration Iontophoresis Permeation matrix Kinetics buccal muco Drug delivery histological aspect naltrexone Tablets Biotechnology

description

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.

year	journal	country	edition	language
2007-09-01	European Journal of Pharmaceutics and Biopharmaceutics

https://doi.org/10.1016/j.ejpb.2007.02.020