title: Chitosan-based mucoadhesive films containing 5-aminolevulinic acid for buccal cancer's treatment.
abstract: Photodynamic therapy (PDT) is a relatively new method to treat various kinds of tumors, including those of the oral cavity. The topical 5-ALA-PDT treatment for tumors of the oral mucosa is preferred, since when administered systemically, there is a general photosensitization drawback in the patient. However, 5-ALA is a hydrophilic molecule and its penetration and retention is limited by topical route, including oral mucosa. We propose a topical delivery system of chitosan-based mucoadhesive film, aiming to promote greater retention of 5-ALA in tissue. The chitosan (CHT) films (4% w/w) were prepared using the solvent evaporation/casting technique. They were tested without 5-ALA resulting in permeability to water vapor (W.V.P=2.15-8.54 g mm/(h cm(2)Pa) swelling ∼300.0% (±10.5) at 4 h or 24 h and in vitro residence time >24 h for all tests. CHT films containing 10.0% (w/w) 5-ALA have resulted in average weight of 0.22 g and thickness of 0.608 mm as suitable characteristics for oral application. In the presence of CHT films both in vitro permeation and retention of 5-ALA (1.0% or 10.0%) were increased. However, 10.0% 5-ALA presented highest values of permeation and retention (∼4 and 17 times respectively, compared to propylene glycol vehicle). On the other hand, in vitro mucoadhesion of CHT films was decreased (18.2-fold and 3.1-fold) by 5-ALA addition (1.0% or 10.0% respectively). However, CHT film containing 10.0% of 5-ALA can be a potential delivery system for topical use in the treatment of tumors of the oral cavity using PDT because it favored the retention of 5-ALA in this tissue and has shown convenient mucoadhesion.
authors.affiliation: School of Pharmacy, Federal University of Rio de Janeiro, Av. Carlos Chagas Filho 373, 21.941.902 Rio de Janeiro, RJ, Brazil.
authors.forename: Irina dos Santos Miranda
authors.initials: Idos S
authors.lastname: Costa
authors.affiliation: School of Pharmacy, Federal University of Rio de Janeiro, Av. Carlos Chagas Filho 373, 21.941.902 Rio de Janeiro, RJ, Brazil.
authors.forename: Renata Pereira
authors.initials: RP
authors.lastname: Abranches
authors.affiliation: School of Pharmacy, University of Uberaba, Av. Nenê Sabino, 1801, Bairro Universitário, 38055-500 Uberaba, MG, Brazil.
authors.forename: Maria Teresa Junqueira
authors.initials: MT
authors.lastname: Garcia
authors.affiliation: School of Pharmacy, Federal University of Rio de Janeiro, Av. Carlos Chagas Filho 373, 21.941.902 Rio de Janeiro, RJ, Brazil. Electronic address: bernadete@pharma.ufrj.br.
authors.forename: Maria Bernadete Riemma
authors.initials: MB
authors.lastname: Pierre
mesh_terms: D000269:Adhesives / Q000737:chemistry*; D000622:Aminolevulinic Acid / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D048271:Chitosan / Q000737:chemistry*; D065546:Drug Liberation; D009061:Mouth Mucosa / Q000378:metabolism; D009062:Mouth Neoplasms / Q000188:drug therapy*; D010539:Permeability; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D012997:Solvents / Q000737:chemistry; D013552:Swine
chemical_list: D000269:Adhesives; D017319:Photosensitizing Agents; D012997:Solvents; D000622:Aminolevulinic Acid; D048271:Chitosan
keywords: 5-Aminolevulinic acid; Chitosan; Mucoadhesive film; Oral cancer; Photodynamic therapy