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.
Juliano
Claudia
C
Department of Drug Sciences, University of Sassari, 07100 Sassari, Italy.
Cossu
Massimo
M
Pigozzi
Paola
P
Rassu
Giovanna
G
Giunchedi
Paolo
P
D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D002610:Cheek; D002710:Chlorhexidine / Q000008:administration & dosage / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D006801:Humans; D066298:In Vitro Techniques; D011108:Polymers; D012016:Reference Values
D000890:Anti-Infective Agents; D011108:Polymers; D002710:Chlorhexidine