Departamento de Bioquímica y Biología Molecular A, Facultad de Biología, Universidad de Murcia, 30100 Espinardo, Murcia, Spain.
Durmishidze Institute of Biochemistry and Biotechnology of Agrarian University of Georgia, 0131 Tbilisi, Georgia.
Int J Pharm. 2015 Feb 1;479(1):96-102. doi: 10.1016/j.ijpharm.2014.12.064. Epub 2014 Dec 27.
Colon diseases are difficult to treat because oral administrated drugs are absorbed at the stomach and intestine levels and they do not reach colon; in addition, intravenous administrated drugs are eliminated from the body before reaching colon. Inulin is a naturally occurring polysaccharide found in many plants. It consists of β 2-1 linked D-fructose molecules having a glucosyl unit at the reducing end. Various inulin and dextran hydrogels have been developed that serve as potential carrier for introduction of drugs into the colon. Because inulin is not absorbed in the stomach or in the small intestine, and inulin is degraded by colonic bacteria, drugs encapsulated in inulin-coated vesicles could be specifically liberated in the colon. Therefore, the use of inulin-coated vesicles could represent an advance for the treatment of colon diseases. Here, we study the use of a cinnamoylated derivative of chicory inulin as a vehicle for the controlled delivery of colonic drugs. The encapsulation of methotrexate in inulin vesicles and its release and activity was studied in colon cancer cells in cultures.
结肠疾病难以治疗，因为口服药物在胃和肠道水平被吸收，而不能到达结肠；此外，静脉内给予的药物在到达结肠之前从体内排出。菊粉是一种天然存在的多糖，存在于许多植物中。它由β2-1 连接的 D-果糖分子组成，在还原端具有葡萄糖基单元。已经开发出各种菊粉和葡聚糖水凝胶，它们可用作将药物引入结肠的潜在载体。由于菊粉在胃或小肠中不被吸收，并且菊粉被结肠细菌降解，因此包封在菊粉包被囊泡中的药物可以在结肠中特异性释放。因此，使用菊粉包被囊泡可能代表治疗结肠疾病的一种进步。在这里，我们研究了菊苣菊粉的肉桂酰化衍生物作为结肠药物控释载体的用途。在培养的结肠癌细胞中研究了甲氨蝶呤在菊粉囊泡中的包封及其释放和活性。
