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 Massachusetts Ave, Cambridge, MA 02139, USA.
Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Austria.
Eur J Pharm Biopharm. 2018 Mar;124:89-94. doi: 10.1016/j.ejpb.2017.12.010. Epub 2017 Dec 21.
Topical delivery is one of the main challenges in the pharmaceutical technology. This study aimed to synthesize a potential adhesive polymeric excipient stable enough for pronounced skin adhesiveness to pave the skin delivery pathway. Polyacrylic acid an anionic well established polymer in the pharmaceutical field was chemically modified with sulfhydryl moieties and in a second step, this sulfhydryl bearing polymer was prone to a preactivation process. During this process, mercaptonicotinic acid was covalently bound to the sulfhydryl groups of polyacrylic acid. The obtained polymeric conjugates were characterized with respect to viscosity measurements, and evaluated in terms of skin adhesive properties with the help of tensile strength assay as well as bond strength assay. Findings exhibited promising potential of newly synthesized preactivated polyacrylic acid in terms of adhesive properties. Preactivated polyacrylic acid revealed a 15.39-fold improved adhesion compared to unmodified polymeric excipient. Therefore, the herein designed preactivated polyacrylic acid shows interesting features for skin application such as scar and wound management.
局部递药是制药技术中的主要挑战之一。本研究旨在合成一种潜在的粘合性高分子赋形剂，该赋形剂具有足够的稳定性，可显著增加皮肤粘性，为经皮递药开辟途径。聚丙烯酸是药物制剂领域中一种公认的阴离子聚合物，通过巯基部分进行化学修饰，然后在第二步中，使带有巯基的聚合物进行预激活过程。在此过程中，硫代烟酰胺酸与聚丙烯酸的巯基共价结合。通过粘度测量对获得的聚合物缀合物进行了表征，并借助拉伸强度测定法和结合强度测定法评估了其皮肤粘合性能。研究结果表明，新合成的预激活聚丙烯酸在粘合性能方面具有有前景的潜力。与未改性的高分子赋形剂相比，预激活聚丙烯酸的粘附性提高了 15.39 倍。因此，本文设计的预激活聚丙烯酸为疤痕和伤口管理等皮肤应用提供了有趣的特性。
