果胶口腔黏附性的设计、修饰及体外评价
Design, modification and in vitro evaluation of pectin's bucco-adhesiveness.
作者信息
Laffleur Flavia, Zilio Martina, Menzel Claudia, Lupo Noemi, Schmutzler Matthias
机构信息
Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Austria.
Institute of Analytical Chemistry & Radiochemistry, Center for Chemistry & Biomedicine (CCB), University of Innsbruck, Austria.
出版信息
Ther Deliv. 2016 Jun;7(6):369-75. doi: 10.4155/tde-2016-0019. Epub 2016 Jun 2.
AIM
It was the aim of this study to synthesize pectin (PEC) with sulfhydryl groups and evaluate its suitability in buccal application.
MATERIALS & METHODS: Native PEC was chemically modified by covalent attachment of sulfhydryl-bearing cysteine (CYS). Stability assays in form of water uptake behavior and erosion study were performed. Additionally, mucoadhesive study on buccal mucosa was performed.
RESULTS
Pectin-cysteine (PECCYS) was successfully synthesized as proved by IR and Ellman's assay exhibiting 436.59 ± 127.87 µmol thiol groups per gram polymer. Stability assay showed that PECCYS revealed a 2.27-fold improved water uptake and mucoadhesiveness augmented 3.75-fold in comparison to unmodified PEC.
CONCLUSION
PECCYS might be a future suitable excipient for buccal adhesive application.
目的
本研究旨在合成带有巯基的果胶（PEC）并评估其在口腔给药中的适用性。
材料与方法
通过将含巯基的半胱氨酸（CYS）共价连接对天然PEC进行化学修饰。进行了以吸水行为形式的稳定性测定和侵蚀研究。此外，还对口腔黏膜进行了黏膜黏附性研究。
结果
红外光谱和埃尔曼测定法证明成功合成了果胶-半胱氨酸（PECCYS），每克聚合物显示出436.59±127.87微摩尔的巯基。稳定性测定表明，与未修饰的PEC相比，PECCYS的吸水量提高了2.27倍，黏膜黏附性增强了3.75倍。
结论
PECCYS可能是未来口腔黏附应用的合适辅料。
Zotero 插件