Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Pharmaceutical Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Int J Pharm. 2019 Sep 10;568:118527. doi: 10.1016/j.ijpharm.2019.118527. Epub 2019 Jul 15.
This study aims at identifying the more suitable polysaccharide in a composite film based on Eudragit RS for 5-ASA delivery to the colon. Different polysaccharides (pectin, chitosan, guar, inulin, and dextran) were examined. The mechanical properties, swelling index, loss of film mass and permeability of films to 5-ASA were recorded at simulating gastric (SGF), intestinal (SIF) and colonic fluids (SCF). Films containing inulin or dextran were more flexible and showed better mechanical properties. Films containing chitosan, pectin or guar exhibited extensive swelling in SGF and SIF. Loss of film mass and drug permeation was more pronounced in SCF than SIF for all samples indicating their sensitivity to colonic bacteria. However, films containing inulin or dextran showed minimum swelling index in SGF and SIF and the highest ratio of permeability in SCF to SIF. Accordingly, inulin and dextran are suggested as appropriate polysaccharides in a film based on Eudragit RS for colon delivery of 5-ASA.
本研究旨在确定基于 Eudragit RS 的 5-ASA 结肠递药复合膜中更适宜的多糖。考察了不同多糖(果胶、壳聚糖、瓜尔胶、菊粉和葡聚糖)。在模拟胃液(SGF)、肠液(SIF)和结肠液(SCF)中记录了薄膜的机械性能、溶胀指数、薄膜质量损失和对 5-ASA 的渗透性。含有菊粉或葡聚糖的薄膜更具柔韧性,力学性能更好。壳聚糖、果胶或瓜尔胶的薄膜在 SGF 和 SIF 中表现出广泛的溶胀。所有样品在 SCF 中的薄膜质量损失和药物渗透都比 SIF 更为显著,表明它们对结肠细菌敏感。然而,含有菊粉或葡聚糖的薄膜在 SGF 和 SIF 中的溶胀指数最小,在 SCF 中对 SIF 的渗透性最高。因此,菊粉和葡聚糖被建议作为基于 Eudragit RS 的用于 5-ASA 结肠递药薄膜的合适多糖。