Division of Pharmaceutical Biosciences, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.
Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.
Pharm Res. 2018 May 22;35(7):145. doi: 10.1007/s11095-018-2428-z.
Bioadhesion is an important property of biological membranes, that can be utilized in pharmaceutical and biomedical applications. In this study, we have fabricated mucoadhesive drug releasing films with bio-based, non-toxic and biodegradable polymers that do not require chemical modifications.
Nanofibrillar cellulose and anionic type nanofibrillar cellulose were used as film forming materials with known mucoadhesive components mucin, pectin and chitosan as functional bioadhesion enhancers. Different polymer combinations were investigated to study the adhesiveness, solid state characteristics, film morphology, swelling, mechanical properties, drug release with the model compound metronidazole and in vitro cytotoxicity using TR146 cells to model buccal epithelium.
SEM revealed lamellar structures within the films, which had a thickness ranging 40-240 μm depending on the film polymer composition. All bioadhesive components were non-toxic and showed high adhesiveness. Rapid drug release was observed, as 60-80% of the total amount of metronidazole was released in 30 min depending on the film formulation.
The liquid molding used was a straightforward and simple method to produce drug releasing highly mucoadhesive films, which could be utilized in treating local oral diseases, such as periodontitis. All materials used were natural biodegradable polymers from renewable sources, which are generally regarded as safe.
生物黏附性是生物膜的一个重要特性，可应用于药物和生物医学领域。本研究采用生物基、无毒、可生物降解的聚合物制备了具有黏膜黏附性的药物释放膜，无需进行化学修饰。
使用纳米原纤纤维素和阴离子型纳米原纤纤维素作为成膜材料，将具有已知黏膜黏附成分的黏蛋白、果胶和壳聚糖作为功能性生物黏附增强剂。研究了不同的聚合物组合，以研究黏附性、固体状态特性、膜形态、溶胀、机械性能、以甲硝唑为模型化合物的药物释放以及使用 TR146 细胞模拟颊上皮的体外细胞毒性。
SEM 显示薄膜内部具有层状结构，其厚度取决于薄膜聚合物组成，范围为 40-240 μm。所有生物黏附成分均无毒，具有高黏附性。观察到快速药物释放，取决于薄膜配方，甲硝唑的总量的 60-80%在 30 分钟内释放。
使用的液体成型是一种生产具有高度黏膜黏附性的药物释放膜的简单方法，可用于治疗局部口腔疾病，如牙周炎。所用的所有材料均为天然可生物降解的聚合物，来源于可再生资源，通常被认为是安全的。
