Mahkam M
Chemistry Department, Azarbaijan University of Tarbiat Moallem, Tabriz, Iran.
Drug Deliv. 2007 Mar;14(3):147-53. doi: 10.1080/10717540601067745.
pH-sensitive hydrogels are suitable candidates for oral delivery of therapeutic peptides, proteins, and drugs, due to their ability to respond to environmental pH changes. New pH-sensitive glycopolymers have been developed by free-radical polymerization of methacrylic acid and 6-acryloyl-glucose-1, 2, 3, 4-tetraacetate, using 1, 6-hexandiol diacrylate and 1, 6-hexandiol propoxylate diacrylate as cross-linking agents. The hydrogels were characterized by differential scanning calorimetry and FTIR. Equilibrium swelling studies were carried out in enzyme-free simulated gastric and intestinal fluids (SGF and SIF, respectively). A model drug, olsalazine [3, 3'-azobis (6-hydroxy benzoic acid)] as an azo derivative of 5-aminosalicylic acid, was entrapped in these gels and the in vitro release profiles were established separately in both enzyme-free SGF and SIF. The drug-release profiles indicated that the amount of drug released depended on the degree of swelling. The hydrogels containing polar propoxylate groups were hydrolyzed rather easily.
pH敏感水凝胶因其能够响应环境pH变化,是口服递送治疗性肽、蛋白质和药物的合适候选材料。通过甲基丙烯酸和6-丙烯酰基葡萄糖-1,2,3,4-四乙酸酯的自由基聚合反应,使用1,6-己二醇二丙烯酸酯和1,6-己二醇丙氧基化二丙烯酸酯作为交联剂,开发了新型pH敏感糖聚合物。通过差示扫描量热法和傅里叶变换红外光谱对水凝胶进行了表征。在无酶模拟胃液和肠液(分别为SGF和SIF)中进行了平衡溶胀研究。将一种模型药物奥沙拉嗪[3,3'-偶氮双(6-羟基苯甲酸)]作为5-氨基水杨酸的偶氮衍生物包封在这些水凝胶中,并分别在无酶SGF和SIF中建立了体外释放曲线。药物释放曲线表明,药物释放量取决于溶胀程度。含有极性丙氧基化基团的水凝胶相当容易水解。