title: Enhancing the buccal mucosal uptake and retention of triamcinolone acetonide.
abstract: In this study, the buccal mucosal uptake and retention of triamcinolone acetonide (TAC) were assessed in the presence of the skin penetration enhancer, Azone (AZ). Porcine buccal mucosa was excised, mounted in modified Ussing chambers, and pretreated with ethanolic solutions of AZ. After 2 h, the rate of TAC disappearance from the donor chamber and TAC appearance in the receptor chamber was monitored, and the mucosal retention of TAC was determined at the completion of the experiment. The permeability and mucosal uptake of TAC was also determined using the TAC-containing proprietary product, Kenalog in Orabase (KO), in the presence and absence of AZ. Pretreatment of the buccal mucosa with AZ increased the TAC disappearance permeability coefficient from 4.78+/-0.31x10(-5) cm/s to 7.12+/-0.53x10(-5) cm/s. While the TAC appearance permeability coefficient was also enhanced 3.8-fold, a 4.4-fold increase in the tissue concentration of TAC was observed. Incorporation of AZ into KO did not result in an enhanced tissue concentration of TAC, however, when the tissue was pretreated with AZ, significantly higher amounts of TAC accumulated in the tissue. Pretreatment of the buccal mucosa with AZ results in increased tissue concentrations of TAC, which may be of clinical benefit in the treatment of oral mucosal inflammatory conditions.
authors.affiliation: Department of Pharmaceutics, Monash University, 381 Royal Parade, Parkville, Victoria, 3052, Australia.
authors.forename: Joseph A
authors.initials: JA
authors.lastname: Nicolazzo
authors.forename: Barry L
authors.initials: BL
authors.lastname: Reed
authors.forename: Barrie C
authors.initials: BC
authors.lastname: Finnin
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001381:Azepines / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D005079:Excipients / Q000494:pharmacology; D066298:In Vitro Techniques; D009061:Mouth Mucosa / Q000378:metabolism*; D010539:Permeability / Q000187:drug effects; D013552:Swine; D014222:Triamcinolone Acetonide / Q000008:administration & dosage* / Q000493:pharmacokinetics*
chemical_list: D000893:Anti-Inflammatory Agents; D001381:Azepines; D005079:Excipients; C035229:laurocapram; D014222:Triamcinolone Acetonide