Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Białystok, Mickiewicza 2C, Białystok 15-222, Poland.
Department of Institute of Applied Radiation Chemistry, Faculty of Chemistry, Łódź University of Technology, Wróblewskiego 15, Łódź 93-590, Poland.
Eur J Pharm Sci. 2024 Jan 1;192:106657. doi: 10.1016/j.ejps.2023.106657. Epub 2023 Nov 30.
Periodontitis consists a group of dental disorders that affect about 70 % of the world population. The therapy mainly relies on mechanical removing bacterial biofilm, nevertheless, local or systemic antibacterial agents play a key role in treating the acute conditions. Secnidazole is a newer derivative of commonly used metronidazole with high safety profile and broad spectrum of antimicrobial activity. The aim of the study was to evaluate the applicability of polyelectrolyte complex-based hydrogels composed of anionic tragacanth with addition of xanthan gum and cationic chitosan as carriers for buccal/intra pocket delivery of secnidazole. Prepared hydrogels with 5 % and 10 % (w/w) drug content were evaluated pharmaceutically towards inter alia physicomechanical, rheological and thermal properties, drug release kinetics, swelling behavior or antimicrobial activity. Cytotoxicity against human primary umbilical vein endothelial cells was also assessed with two independent method. Stable compositions with secnidazole were obtained, however, various miscibility of the drug with the polymers was noted. By adding chitosan, antibacterial activity and swelling performance of the gels were improved, nevertheless, drop of the mucoadhesiveness was also recorded. Hydrogels with 5 % secnidazole were selected as effective antimicrobial compositions with the highest cytocompatibility. They might be considered as promising for oromucosal application with special attention given to SEC as an alternative locally administered antimicrobial agent.
牙周炎是一组影响全球约 70%人口的口腔疾病。牙周炎的治疗主要依赖于机械去除细菌生物膜,但局部或全身抗菌药物在治疗急性病症中起着关键作用。塞克硝唑是一种新型的常用甲硝唑衍生物,具有高安全性和广谱抗菌活性。本研究的目的是评估基于聚电解质复合物的水凝胶作为塞克硝唑颊囊/牙周袋局部递药载体的适用性,该水凝胶由阴离子黄蓍胶与阴离子黄原胶和阳离子壳聚糖组成。评估了载药 5%和 10%(w/w)的水凝胶的药学性质,包括物理机械性能、流变学性能、热性能、药物释放动力学、溶胀行为和抗菌活性。还采用两种独立的方法评估了水凝胶对人脐静脉内皮细胞的细胞毒性。尽管药物与聚合物的各种混合性得到了稳定的塞克硝唑组合物,但仍存在着不稳定的问题。加入壳聚糖可以提高凝胶的抗菌活性和溶胀性能,但也会降低其粘膜粘附性。载有 5%塞克硝唑的水凝胶被选为具有最高细胞相容性的有效抗菌组合物。它们可能被认为是口腔黏膜应用的有前途的候选药物,特别关注 SEC 作为局部施用的替代抗菌药物。