Léber Attila, Budai-Szűcs Mária, Urbán Edit, Vályi Péter, Gácsi Attila, Berkó Szilvia, Kovács Anita, Csányi Erzsébet
Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Szeged 6720, Hungary.
Institute of Clinical Microbiology, Faculty of Medicine, University of Szeged, Szeged 6720, Hungary.
Pharmaceutics. 2019 Mar 25;11(3):142. doi: 10.3390/pharmaceutics11030142.
Despite being a highly prevalent disease and a possible contributor to adult tooth loss, periodontitis possesses no well-established therapy. The aim of the recent study was the development and evaluation of a mucoadhesive monophase lipid formulation for the sustained local delivery of amoxicillin, metronidazole, and/or zinc hyaluronate or gluconate.
To investigate our formulations, differential scanning calorimetry, X-ray diffraction, swelling, erosion, mucoadhesivity, drug release, and antimicrobial measurements were performed.
Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) results show that the loaded drugs are in a suspended form, the softening of the formulations starts at body temperature, but a part remains solid, providing sustained release. Swelling of the lipid compositions is affected by the hydrophilic components, their concentration, and the strength of the coherent lipid structure, while their erosion is impacted by the emulsification of melted lipid components.
Results of drug release and antimicrobial effectiveness measurements show that a sustained release may be obtained. Amoxicillin had higher effectiveness against oral pathogens than metronidazole or zinc hyaluronate alone, but the combination of the two latter could provide similar effectiveness to amoxicillin. The applied mucoadhesive polymer may affect adhesivity, drug release through the swelling mechanism, and antimicrobial effect as well.
尽管牙周炎是一种高发性疾病且可能导致成人牙齿脱落，但目前尚无成熟的治疗方法。近期这项研究的目的是研发并评估一种用于持续局部递送阿莫西林、甲硝唑和/或透明质酸钠或葡萄糖酸锌的粘膜粘附单相脂质制剂。
为了研究我们的制剂，进行了差示扫描量热法、X射线衍射、溶胀、侵蚀、粘膜粘附性、药物释放及抗菌性能测定。
差示扫描量热法（DSC）和X射线衍射（XRD）结果表明，负载的药物呈悬浮形式，制剂在体温时开始软化，但仍有一部分保持固态，从而实现持续释放。脂质组合物的溶胀受亲水成分、其浓度以及连贯脂质结构强度的影响，而其侵蚀则受融化脂质成分乳化的影响。
药物释放和抗菌效果测定结果表明可以实现持续释放。阿莫西林对口腔病原体的有效性高于单独使用的甲硝唑或透明质酸钠，但后两者的组合可提供与阿莫西林相似的有效性。所应用的粘膜粘附聚合物可能会影响粘附性、通过溶胀机制的药物释放以及抗菌效果。
