Design and evaluation of chitosan/ethylcellulose mucoadhesive bilayered devices for buccal drug delivery.

This paper describes the preparation of new buccal bilayered devices comprising a drug-containing mucoadhesive layer and a drug-free backing layer, by two different methods. Bilaminated films were produced by a casting/solvent evaporation technique and bilayered tablets were obtained by direct compression. The mucoadhesive layer was composed of a mixture of drug and chitosan, with or without an anionic crosslinking polymer (polycarbophil, sodium alginate, gellan gum), and the backing layer was made of ethylcellulose. The double-layered structure design was expected to provide drug delivery in a unidirectional fashion to the mucosa and avoid loss of drug due to wash-out with saliva. Using nifedipine and propranolol hydrochloride as slightly and highly water-soluble model drugs, respectively, it was demonstrated that these new devices show promising potential for use in controlled delivery of drugs to the oral cavity. The uncrosslinked chitosan-containing devices absorbed a large quantity of water, gelled and then eroded, allowing drug release. The bilaminated films showed a sustained drug release in a phosphate buffer (pH 6.4). Furthermore, tablets that displayed controlled swelling and drug release and adequate adhesivity were produced by in situ crosslinking the chitosan with polycarbophil.