title: Mucoadhesive tablets for controlled release of acyclovir.
abstract: Mucoadhesive chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC) tablets for gastric drug delivery of acyclovir (ACV) have been developed in order to improve the ACV oral bioavailability. Swelling, bioadhesive and dissolution studies were carried out in two acidic media (pH 1.5 and 4) in order to determine the tablets behaviour in both fed and fasted states. All the designed tablets showed good mucoadhesive properties on gastric mucosa due to the presence of CS and/or HPMC. In vitro dissolution of ACV from tablets was influenced by the swelling behaviour of each polymer. All data release of the studied tablets fitted to Hopfenberg model, which describes drug release from tablets displaying heterogeneous erosion. HPMC and CS/HPMC tablets revealed a sustained release for 24 h, but a complete dissolution of the tablets was not produced at this time. On the contrary, tablets which contained only CS as polymer were able to release the total amount of ACV for 4 h, due to the CS imbibition and erosion processes in pH 1.5 medium. These results allowed us to conclude that CS is the excipient to be chosen to obtain gastroretentive formulations, due to its demonstrated gastric compatibility.
authors.affiliation: Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040-Madrid, Spain.
authors.forename: Roberto
authors.initials: R
authors.lastname: Ruiz-Caro
authors.forename: Manuel
authors.initials: M
authors.lastname: Gago-Guillan
authors.forename: Francisco Javier
authors.initials: FJ
authors.lastname: Otero-Espinar
authors.forename: María Dolores
authors.initials: MD
authors.lastname: Veiga
mesh_terms: D000212:Acyclovir / Q000008:administration & dosage*; D000284:Administration, Oral; D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage*; D048271:Chitosan / Q000737:chemistry* / Q000378:metabolism; D003692:Delayed-Action Preparations / Q000737:chemistry* / Q000378:metabolism; D005753:Gastric Mucosa / Q000378:metabolism*; D006801:Humans; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D013552:Swine; D013607:Tablets; D014014:Tissue Adhesives / Q000737:chemistry / Q000378:metabolism
chemical_list: D000998:Antiviral Agents; D003692:Delayed-Action Preparations; D013607:Tablets; D014014:Tissue Adhesives; D065347:Hypromellose Derivatives; D008747:Methylcellulose; D048271:Chitosan; D000212:Acyclovir