Formulation and in vivo evaluation of chlorhexidine buccal tablets prepared using drug-loaded chitosan microspheres.
This investigation deals with the development of buccal formulations (tablets) based on chitosan microspheres containing chlorhexidine diacetate. The microparticles were prepared by a spray-drying technique, their morphological characteristics were studied by scanning electron microscopy and the in vitro release behaviour was investigated in pH 7.0 USP buffer. Chlorhexidine in the chitosan microspheres dissolves more quickly in vitro than does chlorhexidine powder. The anti-microbial activity of the microparticles was investigated as minimum inhibitory concentration, minimum bacterial concentration and killing time. The loading of chlorhexidine into chitosan is able to maintain or improve the anti-microbial activity of the drug. The improvement is particularly high against Candida albicans. This is important for a formulation whose potential use is against buccal infections. Drug-empty microparticles have an anti-microbial activity due to the polymer itself. Buccal tablets were prepared by direct compression of the microparticles with mannitol alone or with sodium alginate. After their in vivo administration the determination of chlorhexidine in saliva showed the capacity of these formulations to give a prolonged release of the drug in the buccal cavity.
Giunchedi
Paolo
P
Dipartimento di Scienze del Farmaco, Università degli Studi di Sassari, Sassari, Italy. pgiunc@ssmain.uniss.it
Juliano
Claudia
C
Gavini
Elisabetta
E
Cossu
Massimo
M
Sorrenti
Milena
M
D000278:Administration, Buccal; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D001672:Biocompatible Materials / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D002686:Chitin / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics* / Q000648:ultrastructure; D048271:Chitosan; D002710:Chlorhexidine / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D008826:Microbial Sensitivity Tests / Q000379:methods / Q000706:statistics & numerical data; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D013607:Tablets
D000891:Anti-Infective Agents, Local; D001672:Biocompatible Materials; D013607:Tablets; D002686:Chitin; D048271:Chitosan; D002710:Chlorhexidine