title: Acitretin and treatment of the oral leucoplakias. A model to have an active molecules release.
abstract: OBJECTIVE
  The aim of this study was to investigate the effectiveness of acitretin in a new topical formulation (mucoadhesive two-layer tablets) for the treatment of oral leucoplakias.
  
  
  METHODS
  Twenty-one volunteers, 16 men, five women, with oral leucoplakia (histologically diagnosed), were included in this double-blind placebo-controlled study. Patients were randomized in three groups (A, B, C) of seven patients each. Groups A and B received tablets with different in vitro release profiles, and group C subjects (controls) received tablets without acitretin. The acitretin dose was 20 mg/day (two 10 mg tablets daily). Serum aspartate aminotransferase, alanine aminotransferase, cholesterol and triglycerides were evaluated before and after treatment. At the end of therapy the concentrations of acitretin in plasma, saliva and tissue were measured by high-performance liquid chromatography.
  
  
  RESULTS
  At the end of the study 71% (groups A and B) of patients showed clinical remission or marked improvement. No improvement was noted in the control subjects (group C). These results were further confirmed by histological findings. There were no significant changes in laboratory values in the three groups. The acitretin concentration in plasma and tissue ranged from 0 to 50 mg with no difference between groups A and B, and it was very high in saliva (ranging from 4.9 to 43 mg) with higher concentrations in group A than in group B (due to a longer adhesion time in group A). Patients' compliance was excellent. The results show that mucoadhesive tablets of topical acitretin are efficacious in the treatment of oral leucoplakia without systemic side-effects.
authors.affiliation: Department of Oral Pathology-School of Dentistry II University of Naples, Italy. jodga@tin.it
authors.forename: G M
authors.initials: GM
authors.lastname: Gaeta
authors.forename: F
authors.initials: F
authors.lastname: Gombos
authors.forename: F
authors.initials: F
authors.lastname: Femiano
authors.forename: C
authors.initials: C
authors.lastname: Battista
authors.forename: P
authors.initials: P
authors.lastname: Minghetti
authors.forename: L
authors.initials: L
authors.lastname: Montanari
authors.forename: R A
authors.initials: RA
authors.lastname: Satriano
authors.forename: G
authors.initials: G
authors.lastname: Argenziano
mesh_terms: D017255:Acitretin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000278:Administration, Buccal; D000287:Administration, Topical; D000328:Adult; D000368:Aged; D001707:Biopsy, Needle; D003692:Delayed-Action Preparations; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004334:Drug Administration Schedule; D005260:Female; D006801:Humans; D007641:Keratolytic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D007971:Leukoplakia / Q000188:drug therapy* / Q000473:pathology; D008297:Male; D008875:Middle Aged; D009061:Mouth Mucosa / Q000187:drug effects / Q000473:pathology*; D009062:Mouth Neoplasms / Q000188:drug therapy* / Q000473:pathology; D012016:Reference Values; D012463:Saliva / Q000737:chemistry; D013607:Tablets; D016896:Treatment Outcome
chemical_list: D003692:Delayed-Action Preparations; D007641:Keratolytic Agents; D013607:Tablets; D017255:Acitretin