title: Development of imiquimod-loaded mucoadhesive films for oral dysplasia.
abstract: Oral squamous dysplasia, which can usually be readily visualized as leukoplakia during an oral examination and confirmed by histology, is often considered a premalignant condition. Current treatments, however, focus on the final stages of disease, and treatments such as surgery can lead to postoperative disabilities. Hence, this study was designed to develop a noninvasive, mucoadhesive drug delivery system loaded with an immune response modifier, imiquimod, as a treatment for precancerous dysplastic lesions. Blends of polyvinylpyrrolidone and carboxymethylcellulose were used to prepare mucoadhesive films that were backed with poly(ethylene-co-vinyl acetate). Because of the hydrophobic nature of imiquimod, four loading methods (sonication, linoleic acid, 2-hydroxypropyl-β-cyclodextrin, and acetate buffer) were compared. The formation of imiquimod-cyclodextrin complexes and their solubility was studied by differential scanning calorimetry and phase solubility studies. All films achieved sustained release of drug for 3 h except those prepared by linoleic acid. The high solubility of imiquimod in acetate buffer facilitated high loading capacity and greater release (68%) of drug than did the other formulations (approximately 40%). In summary, a noninvasive and local approach with the potential to treat precancerous lesions may be achieved by this described mucoadhesive drug delivery system.
authors.affiliation: Center for Biomedical Engineering, University of Kentucky, Lexington, Kentucky 40506, USA.
authors.forename: Sandeep K
authors.initials: SK
authors.lastname: Ramineni
authors.forename: Larry L
authors.initials: LL
authors.lastname: Cunningham
authors.forename: Thomas D
authors.initials: TD
authors.lastname: Dziubla
authors.forename: David A
authors.initials: DA
authors.lastname: Puleo
mesh_terms: D000269:Adhesives / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000378:metabolism; D000634:Aminoquinolines / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000378:metabolism; D000818:Animals; D002460:Cell Line; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods*; D000077271:Imiquimod; D007972:Leukoplakia, Oral / Q000188:drug therapy* / Q000378:metabolism; D051379:Mice
chemical_list: D000269:Adhesives; D000634:Aminoquinolines; D000077271:Imiquimod