title: Aloin delivery on buccal mucosa: ex vivo studies and design of a new locoregional dosing system.
abstract: BACKGROUND
  Chemoprevention of potential malignant disorders or cancerous lesions that affect oral mucosae requires extended duration of treatment. Locoregional delivery of natural products could represent a promising strategy for this purpose.
  
  
  OBJECTIVE
  To investigate the aptitude of aloin to permeate through, or accumulate in, the buccal mucosa and to develop a new prolonged oro-mucosal drug delivery system.
  
  
  METHODS
  Permeation/accumulation of aloin from Curacao Aloe (containing 50% barbaloin) was evaluated ex vivo, using porcine buccal mucosa as the most useful model to simulate human epithelium. Oro-mucosal matrix tablets were prepared by dispersing aloin (10% w/w) in Eudragit® RS 100 as, biocompatible, low permeable, pH-independent, and non-swelling polymer. The prepared tablets were evaluated for drug-polymer compatibility, weight variation, drug uniformity content, diameter, thickness, hardness, friability, swelling, mucoadhesive strength, and drug release.
  
  
  RESULTS
  Aloin has low tendency to cross buccal mucosa, permeation is marginal, and high drug amounts remain entrapped into the epithelium. Matrix tablets characteristics were in agreement with pharmacopoeial requirements. Drug release showed highly reproducible Higuchian profile. Delivery through matrix tablets promoted drug accumulation in the mucosal tissue.
  
  
  CONCLUSIONS
  Following application of matrix tablets on porcine buccal mucosa, the amount of discharged drug recovered in the tissue should be sufficient to produce the desired effects, providing therapeutic drug levels directly at the site of action. Aloin-loaded tablets are valid candidates for prevention/treatment of potentially malignant disorders and oral cancer and could potentially lead to clinically relevant drug delivery system as coadjuvant of conventional chemotherapy/radiation therapy.
authors.affiliation: a Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF) , Università degli Studi di Palermo , Palermo , Italy and.
authors.forename: Viviana
authors.initials: V
authors.lastname: De Caro
authors.forename: Anna Lisa
authors.initials: AL
authors.lastname: Scaturro
authors.forename: Giulia
authors.initials: G
authors.lastname: Di Prima
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Avellone
authors.forename: Flavia Maria
authors.initials: FM
authors.lastname: Sutera
authors.forename: Olga
authors.initials: O
authors.lastname: Di Fede
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Campisi
authors.forename: Libero Italo
authors.initials: LI
authors.lastname: Giannola
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000268:Adhesiveness; D000504:Aloe / Q000737:chemistry; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004642:Emodin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D009061:Mouth Mucosa / Q000378:metabolism*; D010539:Permeability; D011108:Polymers / Q000737:chemistry*; D015203:Reproducibility of Results; D013552:Swine; D013607:Tablets
chemical_list: D000180:Acrylic Resins; D011108:Polymers; D013607:Tablets; C050528:Eudragit RS; D004642:Emodin; C006457:alloin
keywords: Aloin matrix tablets; barbaloin; buccal mucosa; buccal tablets; locoregional drug delivery; oro-mucosal delivery