Micromatricial metronidazole benzoate film as a local mucoadhesive delivery system for treatment of periodontal diseases

Abstract

The main objective of this study was to develop a local, oral mucoadhesive metronidazole benzoate (MET) delivery system that can be applied and removed by the patient for the treatment of periodontal diseases. Mucoadhesive micromatricial chitosan/poly(ε-caprolactone) (CH/PCL) films and chitosan films were prepared. Thermal behavior, morphology, and particle size measurements were used to evaluate the prepared films. The effect of different molar masses of CH and different ratios of medium Mwt molar mass chitosan (MCH):PCL on water absorption, in vitro bioadhesion, mechanical properties, and in vitro drug release was examined. In vivo performance of the selected formulation was also evaluated. Differential scanning calorimetry examination revealed that MET existed mainly in amorphous form. Under microscopic examination, PCL microparticles were homogeneously dispersed in the films. The use of different molar masses of CH and different ratios of (MCH):PCL affected the size of the entrapped particles. Addition of PCL significantly decreased percentage water uptake and bioadhesion force compared with pure CH film. With regard to mechanical properties, the 2-layered film containing 1:0.625 MCH:PCL had the best tensile properties. At fixed CH:PCL ratio (1:1.25), the slowest drug release was obtained from films containing high molar mass CH. On the other hand, the 2-layered film that consisted of 1:0.625 MCH:PCL had the slowest MET release. In vivo evaluation of the selected film revealed that metronidazole concentration in saliva over 6 hours ranged from 5 to 15 μg/mL, which was within and higher than the reported range of minimum inhibitory concentration for metronidazole. A significant in vitro/in vivo correlation under the adopted experimental conditions was obtained.

Functionalised nanoscale coatings using layer-by-layer assembly for imparting antibacterial properties to polylactide-co-glycolide surfaces

“…Among antibiotics, MET is used in the oral cavity for treating infections by anaerobic bacteria associated with periodontal diseases due to its low minimum inhibitory concentration [5].…”

“…Among antibiotics, metronidazole (MET) is highly effective for the management of anaerobic infections, such as intraabdominal and gynecologic infections, septicemia, endocarditis, bone and joint infections, central nervous system infections, respiratory tract infections, skin and skin-structure infections. Moreover, MET is largely used for treating infections by anaerobic bacteria associated with periodontal diseases due to the low minimum inhibitory concentration it requires [5]. For treatment of mixed aerobic and anaerobic infections, metronidazole should be used in combination with other antibacterial agents that are appropriate for the treatment of the aerobic infection, because MET is ineffective against aerobic bacteria [6,7].…”

Advanced drug delivery approaches against periodontitis

“…A ratio of 1:0.625 for chitosan:PCL presented best tensile properties and slowest drug release. In vitro studies showed saliva concentrations of 5 to 15 mg/ml over 6 hours, which was within and above the MIC for metronidazole (El-Kamel et al, 2007). Recently Labib and coworkers developed films by solvent casting technique.…”

Newer Methods of Nanoparticle Synthesis: Nitroimidazole properties with Nanometal oxides in Polymer Cages as Drug-Biomarker Monitors

“…Different polymers such as polyethylene glycol [9,20], poly vinyl alcohol [4,24], polymethylmethacrylate [16],polysaccharides [6,11]. Other uses of nitroimidazole polymer complexes as delivery systems are reported in periodontal diseases [2,21], amebiasis [6,13,22], helicobector pylori [7], gentamycin [16], vaginitis [8], gastritis [10,12], sprays [19], liposomes [25].…”