Wróblewska Magdalena, Szymańska Emilia, Szekalska Marta, Winnicka Katarzyna
Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Białystok, A. Mickiewicza 2C, 15-222 Białystok, Poland.
Polymers (Basel). 2020 Mar 19;12(3):680. doi: 10.3390/polym12030680.
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.
牙周疾病是最普遍的口腔疾病之一,它们被归类为由牙菌斑中细菌积聚引起的慢性感染,这种感染会导致牙周组织局部炎症。使用局部给药系统治疗牙周疾病受到了更多关注,因为活性物质直接靶向受影响区域,从而将其全身副作用降至最低。因此,本研究的目的是开发并表征不同类型的凝胶制剂——双凝胶、水凝胶和油凝胶——作为含有甲硝唑(MET)的局部给药系统,该系统可应用于口腔黏膜。研究了制剂类型对机械、流变学和黏膜粘附性能的影响。此外,还评估了甲硝唑的体外释放、其通过猪颊黏膜的离体渗透以及通过平板扩散法测定的抗菌活性。结果发现,所获得的凝胶制剂是非牛顿体系,表现出剪切变稀行为和触变性,具有良好的质地特性,如硬度、可压缩性和粘附性。此外,所设计的制剂具有有益的黏膜粘附性能。与市售甲硝唑软膏相比,含有微粉化MET的水凝胶和双凝胶制剂在药物释放和抗菌活性方面被认为是更好的制剂。使用猪颊黏膜进行的离体渗透研究表明,双凝胶制剂的特点是初始渗透率较高,能提供快速治疗效果,同时在黏膜组织中适度保留,以降低局部细胞毒性风险。