Formulation design and in vitro characterization of clotrimazole dental implant for periodontal diseases

Abstract

Clotrimazole is an imidazole derivative novel broad spectrum antimicrobial agent extensively used topically for fungal
infection. The purpose of this study is to design and develop in situ implants containing clotrimazole that could be used in
the treatment of periodontal diseases by direct periodontal intrapocket administration. The dental film of clotrimazole was
prepared by solvent casting technique using hydroxyl propyl methyl cellulose, ethyl cellulose, hydroxyl propyl cellulose
and chitosan in different concentrations as biodegradable rate controlling polymers. The drug polymers interaction was
studied by Fourier Transform Infrared Spectroscopy (FTIR) and study suggesting no interaction between drug and
polymers. The implants were characterized for weight variation, thickness, surface pH, tensile strength, folding endurance,
moisture content, viscosity, drug content uniformity, in vitro drug release, mass balance, drug release kinetic, stability and
in vitro antibacterial activity studies. Mean weight data showed that the different films were uniform. Minimum thickness
was obtained with film containing chitosan. Almost all dental film formulations having satisfactory tensile strength. Good
physicochemical properties were shown by the films. In vitro drug release data indicate that the films showed an initial burst
release followed by sustained release of the drug(s). In vitro drug release rate for selected dental implant formulation (F6,
containing 4.5 % w/w of chitosan) was found to sustain clotrimazole over 10 h obeying zero order kinetic. The stability
study did not show any significant changes. The study suggesting the film containing chitosan is a potential drug delivery
device for the topical treatment of periodontal diseases.