Abstract

Periodontal diseases are some of the most widespread oral afflictions, and they are labeled as chronic infections caused by the accumulation of bacteria in dental plaque that produces localized inflammation of the periodontium. The use of local drug delivery systems to treat periodontal diseases has received greater attention, because the active substance is targeted directly to the affected area, which minimizes its systemic side effects. Therefore, the purpose of the investigation was to develop and characterize different types of gel formulations—bigel, hydrogel and oleogel—as local delivery systems containing metronidazole (MET), which can be applied to the oral mucosa. The influence of the formulation type on the mechanical, rheological and mucoadhesive properties were examined. Moreover, in vitro release of metronidazole, its ex vivo permeation through buccal porcine mucosa and antimicrobial activity measured by the plate diffusion method were estimated. It was found that the gel formulations obtained were non-Newtonian systems, showing a shear-thinning behavior and thixotropic properties with good textural features such as firmness, compressibility and adhesiveness. Moreover, the preparations designed possessed beneficial mucoadhesive properties. The formulated hydrogels and bigels containing micronized MET were considered as better formulations in terms of drug release and antimicrobial activity compared to commercially available metronidazole ointment. An ex vivo permeation study with the use of porcine buccal mucosa demonstrated that the bigel formulation was characterized by higher initial permeability rate providing a fast therapeutic effect with simultaneous moderate retention in mucosal tissue to decrease the risk of local cytotoxicity.

Highlights

  • Periodontal diseases are very common oral afflictions that may affect as much as 90% of the worldwide population [1]

  • The formulated hydrogels and bigels containing micronized MET were considered as better formulations in terms of drug release and antimicrobial activity compared to commercially available metronidazole ointment

  • Mucoadhesive conventional preparations used treatment. They characterized by better efficacy conventional preparations used in in thisthis treatment

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Summary

Introduction

Periodontal diseases are very common oral afflictions that may affect as much as 90% of the worldwide population [1]. They are defined as a chronic inflammation of gum and tissues that surround and support the teeth and are classified into two major stages according to the severity of the disease, namely gingivitis and periodontitis. Gingivitis, the mildest form and an early stage of periodontal disease, is a nondestructive periodontal infection caused by the bacterial biofilm that accumulates on teeth adjacent to the gingival. Periodontitis, an advanced stage characterized by progression of gingivitis, may even lead to loss of teeth and erosion of supporting tissues. Different strategies are commonly used to treat periodontitis such as enhancement of Polymers 2020, 12, 680; doi:10.3390/polym12030680 www.mdpi.com/journal/polymers

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