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 compr...

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Bibliographic Details
Published in:Journal of controlled release 1998-11, Vol.55 (2), p.143-152
Main Authors: Remuñán-López, Carmen, Portero, Ana, Vila-Jato, José Luis, Alonso, Marı́a José
Format: Article
Language:English
Subjects:
Adhesives
Animals
Bilayered device
Biological and medical sciences
Buccal drug delivery
Cattle
Cellulose - analogs & derivatives
Cheek
Chitin - analogs & derivatives
Chitosan
Crosslinking
Drug Delivery Systems
Evaluation Studies as Topic
General pharmacology
Medical sciences
Microscopy, Electron
Mucoadhesion
Nifedipine
Nifedipine - administration & dosage
Nifedipine - pharmacokinetics
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Propranolol - administration & dosage
Propranolol - pharmacokinetics
Propranolol hydrochloride
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Summary: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.
ISSN:0168-3659
1873-4995
DOI:10.1016/S0168-3659(98)00044-3