Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Austria; Massachusetts Institute of Technology, Koch Institute for Integrative Cancer Research at MIT, Langer Lab, 77 Massachussets Ave, Cambridge, MA, 02139, USA.
Int J Biol Macromol. 2017 Dec;105(Pt 1):1310-1314. doi: 10.1016/j.ijbiomac.2017.07.152. Epub 2017 Jul 27.
Skin delivery and transdermal delivery are key ambitions of the pharmaceutical and cosmetically researchers.
The study aimed to chemically modify well-known polymeric gelling agents in order to boost their topical suitability by fostering their dermal adhesiveness.
Conventional chitosan was modified via amide bound formation with sulfhydryl compound thioglycolic acid. Subsequently, preactivated chitosan conjugate was established by preactivation of chitosan-thioglycolic acid with mercaptonicotinamide being covalently attached via disulfide bond linkage. All conjugates were examined due to their dermal adhesiveness and controlled drug release properties.
Preactivated chitosan conjugates Exhibit 7.46-fold dermal adhesiveness on skin due to tensile adhesion strength. Furthermore a 1.9-fold controlled release of Rhodamine123 as model drug was determined in comparison to unmodified chitosan.
Taken together, preactivated chitosan gels show a promising platform for topical application.
皮肤给药和经皮给药是药物和化妆品研究人员的主要目标。
本研究旨在通过增强其皮肤黏附性来化学修饰众所周知的聚合物凝胶剂，以提高其局部适用性。
常规壳聚糖通过与巯基化合物巯基乙酸形成酰胺键进行修饰。随后，通过将壳聚糖-巯基乙酸与通过二硫键连接共价连接的烟酰胺巯基进行预激活，建立预激活壳聚糖缀合物。所有的缀合物都因其皮肤黏附性和控制药物释放性能而被检测。
由于拉伸粘附强度，预激活壳聚糖缀合物在皮肤上的皮肤粘附性提高了 7.46 倍。此外，与未修饰的壳聚糖相比，作为模型药物的罗丹明 123 的释放控制了 1.9 倍。
总之，预激活壳聚糖凝胶为局部应用提供了一个有前途的平台。
