1. Mucoadhesive Tablets for Controlled Release of Acyclovir
- Author
-
Roberto Ruiz-Caro, María Dolores Veiga, Manuel Gago-Guillan, and Francisco J. Otero-Espinar
- Subjects
Swine ,Bioadhesive ,Acyclovir ,Administration, Oral ,Excipient ,Methylcellulose ,Antiviral Agents ,Chitosan ,chemistry.chemical_compound ,Hypromellose Derivatives ,Drug Discovery ,medicine ,Animals ,Humans ,Chromatography ,General Chemistry ,General Medicine ,Controlled release ,Bioavailability ,chemistry ,Gastric Mucosa ,Delayed-Action Preparations ,Drug delivery ,Tissue Adhesives ,Swelling ,medicine.symptom ,Tablets ,medicine.drug - 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.
- Published
- 2012
- Full Text
- View/download PDF