Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Innrain 80/82, 6020, Innsbruck, Austria.
Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Innrain 80/82, 6020, Innsbruck, Austria.
Int J Biol Macromol. 2017 Sep;102:1250-1256. doi: 10.1016/j.ijbiomac.2017.04.123. Epub 2017 May 6.
The aim of this study was to modify xanthan, a well-known gelling agent, in order to treat sialorrhea, which increases salivary flow due to an excessive stimulus of the salivary reflex.
Chemical modification occurs by covalent attachment of l-cysteine (SH) to the polymeric backbone of xanthan (X) via amide bond formation. Safety considerations, water uptake capacity, and erosion were evaluated. Furthermore, mucoadhesiveness on buccal mucosa and vapor uptake studies were performed. In vitro/in vivo correlation of reduce of salivary flow was conducted and drug release of embedded tannin was determined.
Safety investigations ensured modified X-SH being safe to use. X-SH exposed 1.5-x higher water uptake capacity in comparison to unmodified xanthan. Then, stability of X-SH augmented 5.5-fold in the case of matrix erosion studies. Reduction of salivary flow could be obtained 1.6-fold improved in case of X-SH compared to X. Furthermore, tannin was 1.8-fold controlled released in comparison to unmodified xanthan.
Taking these findings into consideration, chemical modified xanthan emerged with its distinctive properties as a promising approach in treating sialorrhea.
本研究旨在修饰黄原胶，一种众所周知的胶凝剂，以治疗因唾液反射过度刺激而导致唾液流量增加的流涎症。
通过酰胺键形成，将 l-半胱氨酸 (SH) 共价连接到黄原胶 (X) 的聚合物主链上，从而发生化学修饰。评估了安全性考虑、吸水率和侵蚀。此外，还进行了颊黏膜的粘膜粘附性和蒸汽吸收研究。进行了体外/体内唾液流量减少相关性研究，并测定了嵌入单宁酸的药物释放。
安全性研究确保修饰后的 X-SH 安全使用。与未修饰的黄原胶相比，X-SH 暴露的吸水率高 1.5 倍。然后，在基质侵蚀研究中，X-SH 的稳定性增加了 5.5 倍。与 X 相比，X-SH 可使唾液流量减少 1.6 倍。此外，与未修饰的黄原胶相比，单宁酸的释放得到了 1.8 倍的控制。
考虑到这些发现，化学修饰的黄原胶因其独特的性质而成为治疗流涎症的一种有前途的方法。
