Drug release kinetics and biological properties of a novel local drug carrier system

Abstract

Background: The purpose of this in vitro study was to investigate drug release kinetics and
cytotoxicity of a novel drug delivery system for treatment of periodontitis.
Materials and Methods: This in vitro study addresses the fabrication of a polycaprolactone/
alginic acid‑based polymeric film loaded with metronidazole, as a basic drug in the treatment of
periodontal diseases. Films were prepared by solvent casting technique. Four formulations with
different percentages of drug by weight (3%, 5%, 9%, and 13%) were prepared. Drug release kinetics
were investigated using ultraviolet–visible spectroscopy during (one week). Data were analyzed
using repeated measures ANOVA. Cytotoxicity of drug‑loaded system extracts was evaluated by
3‑(4,5‑dimethylthiazol‑2‑yl)‑2,5‑diphenyltetrazolium bromide (MTT) assay using L929 cells after
24‑h incubation. The results were evaluated according to ISO standard 10993‑5 and assessed using
ANOVA and Tukey’s tests at a significance level of P < 0.05.
Results: All polymeric films showed a burst drug release followed by a gradual release. Drug
release data were fitted well with the first‑order kinetic model in all drug‑containing formulations
indicating that drug release is a fraction of remaining drug in the matrix. Drug release is mainly driven
by diffusion of medium into the composite matrix. 3%wt metronidazole‑containing formulation
exhibited the best MTT result.
Conclusion: The findings of this study supported the synthesis of drug‑loaded periodontal films
with 3% metronidazole due to better biological properties along with the ability of acceptable drug
release to eradicate anaerobic periodontal bacteria.
Key Words: Drug delivery system, metronidazole, periodontal diseases, pharmacokinetics,
toxicity