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Preparation, in vitro characterization and preliminary in vivo evaluation of buccal polymeric films containing chlorhexidine

Juliano, Claudia Clelia Assunta and Cossu, Massimo and Pigozzi, Claudia and Rassu, Giovanna and Giunchedi, Paolo (2008) Preparation, in vitro characterization and preliminary in vivo evaluation of buccal polymeric films containing chlorhexidine. AAPS PharmSciTech, Vol. 9 (4), p. 1153-1158. ISSN 1530-9932. Article.

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DOI: 10.1208/s12249-008-9153-6


The aim of this work was to investigate the suitability of some polymeric films as buccal systems for the delivery of the antiseptic drug chlorhexidine diacetate, considered as a valid adjunct in the treatment of oral candidiasis. Six different film formulations, mono- or double-layered, containing 5 or 10 mg of chlorhexidine diacetate, respectively, and alginate and/or hydroxypropylmethylcellulose and/or chitosan as excipients, were prepared by a casting-solvent evaporation technique and characterized in terms of drug content, morphology (scanning electron microscopy), drug release behavior, and swelling properties. Moreover, the in vivo concentrations of chlorhexidine diacetate in saliva were evaluated after application of a selected formulation on the oral mucosa of healthy volunteers. The casting-solvent evaporation proved to be a suitable technique for preparing soft, flexible, and easily handy mono- or double-layered chlorhexidine-loaded films. Some prepared formulations showed favorable in vitro drug release rates and swelling properties. The behavior of a selected formulation, chosen on the basis of its in vitro release results, was preliminarily investigated in vivo after application in the oral cavity of healthy volunteers. The films were well tolerated and the salivary chlorhexidine concentrations were maintained above the minimum inhibitory concentration for Candida albicans for almost 3 h. These preliminary results indicate that polymeric films can represent a valid vehicle for buccal delivery of antifungal/antimicrobial drugs.

Item Type:Article
ID Code:1674
Uncontrolled Keywords:Buccal mucoadhesive, chitosan, chlorhexidine, polymeric films, sodium alginate
Subjects:Area 03 - Scienze chimiche > CHIM/09 Farmaceutico tecnologico applicativo
Divisions:001 Università di Sassari > 01 Dipartimenti > Scienze del farmaco
Publisher:Springer New York
Copyright Holders:© 2008 American Association of Pharmaceutical Scientists
Deposited On:18 Aug 2009 10:05

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