Laffleur Flavia, Michalek Martina, Suchaoin Wongsakorn, Ijaz Muhammad
Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.
Ther Deliv. 2016 Jul;7(7):423-9. doi: 10.4155/tde-2016-0021.
Introducing the concept of mucoadhesion in the 1980s, application of mucoadhesive polymers for buccal drug delivery has been the subject of pharmaceutical interest.
The purpose of this study was to modify well-known xanthan in order to remarkably boost its suitability for buccal adhesiveness.
Xanthan (X) was chemically modified by covalent binding of L-cysteine (SH) exhibiting sulfhydryl groups on the polymeric backbone via amide bond formation. Cytotoxicity, stability properties and mucoadhesiveness, respectively, of sulfhydryl-modified xanthan (H-SH) was investigated compared with unmodified xanthan (X).
According to cell viability studies X-SH was safe to use. X-SH revealed 1.61-fold higher stability in comparison to unmodified xanthan. Thereafter, mucoadhesion of X-SH augmented 8.35-fold in case of rotating cylinder assay. Tensile study showed 2.65-fold higher total work of adhesion when comparing X-SH with X.
In completion, novel sulfhydryl-modified xanthan proved itself being a useful and promising excipient for buccal-adhesive delivery systems.
自20世纪80年代引入粘膜粘附概念以来，粘膜粘附聚合物在口腔给药中的应用一直是药学领域关注的课题。
本研究旨在对著名的黄原胶进行改性，以显著提高其口腔粘附适用性。
通过酰胺键形成，将具有巯基的L-半胱氨酸（SH）共价结合到聚合物主链上，对黄原胶（X）进行化学改性。将巯基改性黄原胶（H-SH）与未改性黄原胶（X）分别进行细胞毒性、稳定性和粘膜粘附性研究。
根据细胞活力研究，X-SH使用安全。与未改性黄原胶相比，X-SH的稳定性提高了1.61倍。此后，在旋转圆筒试验中，X-SH的粘膜粘附性提高了8.35倍。拉伸研究表明，与X相比，X-SH的总粘附功高2.65倍。
总之，新型巯基改性黄原胶被证明是一种用于口腔粘附给药系统的有用且有前景的辅料。
