The Russell Berrie Nanotechnology Institute, Technion-Israel Institute of Technology, Haifa 32000, Israel.
Department of Chemical Engineering, Technion-Israel Institute of Technology, Haifa 32000, Israel.
Int J Pharm. 2016 Jun 15;506(1-2):25-34. doi: 10.1016/j.ijpharm.2016.04.019. Epub 2016 Apr 12.
Utilization of animal parts in ex-vivo mucoadhesion assays is a common approach that presents many difficulties due to animal rights issues and large variance between animals. This study examines the suitability of two PEGDA (poly(ethylene glycol) diacrylate) based hydrogels to serve as tissue mimetics for mucoadhesion evaluation. One hydrogel, termed PEGDA-QT, was composed of pentaerythritol tetrakis (3-mercaptopropionate) and PEG and contained free thiol groups mimicking those found in natural mucosa. The other hydrogel was formed by UV (ultraviolet) curing of PEGDA and mimicked the mechanical property of mucosa but not its chemical constitute. When ranking different first generation mucoadhesive polymers using a tensile assay, both hydrogels showed good agreement with the ranking achieved for porcine small intestine. However, only PEGDA-QT and porcine small intestine shared a similar displacement curve. The same ranking for PEGDA-QT and porcine small intestine was also observed when comparing a second-generation mucoadhesive polymer, thiolated alginate, to native alginate. Our findings suggest that PEGDA-QT could serve as a replacement for porcine small intestine in both mucoadhesion evaluations using a tensile machine and the flow-through method for first and second-generation mucoadhesive polymers.
在离体黏附测定中使用动物组织是一种常见的方法，但由于动物权利问题和动物之间的巨大差异，这种方法存在许多困难。本研究考察了两种基于聚乙二醇二丙烯酸酯（PEGDA）的水凝胶作为黏附评估的组织模拟物的适用性。一种水凝胶，称为 PEGDA-QT，由季戊四醇四（3-巯基丙酸酯）和 PEG 组成，含有模拟天然黏膜中存在的游离巯基的基团。另一种水凝胶是通过 PEGDA 的紫外（UV）固化形成的，模拟了黏膜的机械性能，但不模拟其化学组成。当使用拉伸测定对不同第一代黏附聚合物进行排序时，两种水凝胶与猪小肠的排序结果都非常吻合。然而，只有 PEGDA-QT 和猪小肠具有相似的位移曲线。当比较第二代黏附聚合物巯基化藻酸盐与天然藻酸盐时，PEGDA-QT 和猪小肠的排序也相同。我们的研究结果表明，PEGDA-QT 可以替代猪小肠，用于拉伸机和第二代黏附聚合物的流动法进行黏附评估。
