Department of Pharmacy .
Pharm Dev Technol. 2014 Mar;19(2):173-80. doi: 10.3109/10837450.2013.763262. Epub 2013 Jan 28.
Ethylcellulose microparticles containing metronidazole and propolis extractive solution were prepared and evaluated in vitro against periodontal pathogens. Scanning electron microscopy, particle size analysis, drug entrapment efficiency and drug release of microparticles were determined. The antimicrobial activity of microparticles was evaluated against microorganisms of periodontal importance (Enterococcus faecalis, Streptococcus pyogenes, Streptococcus mutans, Staphylococcus aureus, Klebsiella pneumoniae and Escherichia coli). It was obtained particles with regular morphology, mean diameter of 1.23 µm, and entrapment efficiency for propolis and metronidazole were 91.41% and 22.23%, respectively. In vitro release studies of propolis and metronidazole from microparticles showed prolonged drug release and controlled by Fickian diffusion. Both propolis and metronidazole displayed activity against the tested strains. Moreover, the results showed that the strains of E. faecalis, S. pyogenes and S. mutans were more susceptible to the propolis and E. faecalis to the metronidazole. It was also observed that the amount of metronidazole to inhibit the microorganism strains in the physical mixture with propolis was smaller than in the metronidazole alone, suggesting potentiation effect between propolis and metronidazole. These microparticles would be useful for developing intermediary or eventual dosage form to be administered into the periodontal pocket more easily and safely.
载有甲硝唑和蜂胶提取物溶液的乙基纤维素微球被制备并在体外对牙周病病原体进行评估。扫描电子显微镜、粒径分析、药物包封效率和微球的药物释放进行了测定。微球的抗菌活性针对牙周病重要的微生物(粪肠球菌、酿脓链球菌、变形链球菌、金黄色葡萄球菌、肺炎克雷伯菌和大肠杆菌)进行了评估。获得了具有规则形态、平均直径为 1.23μm 的颗粒,蜂胶和甲硝唑的包封效率分别为 91.41%和 22.23%。蜂胶和甲硝唑从微球中的体外释放研究表明药物释放延长且受菲克扩散控制。蜂胶和甲硝唑均对测试菌株表现出活性。此外,结果表明,粪肠球菌、酿脓链球菌和变形链球菌的菌株对蜂胶更敏感,而粪肠球菌对甲硝唑更敏感。还观察到甲硝唑与蜂胶物理混合物中抑制微生物菌株的量比单独使用甲硝唑时小,表明蜂胶和甲硝唑之间存在增效作用。这些微球将有助于开发中间或最终剂型,以便更轻松、更安全地施用于牙周袋。