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

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.