State Key Laboratory of Applied Organic Chemistry, Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province and Department of Chemistry, Lanzhou University, Lanzhou 730000, PR China.
J Biomater Sci Polym Ed. 2013;24(9):1127-39. doi: 10.1080/09205063.2012.743059. Epub 2012 Nov 20.
Cationic polymers have been widely used as drug delivery systems. Herein, an oxidized sodium alginate/chitosan (OSA/CS) core-shell microgel was prepared via water-in-oil emulsion method. Morphological properties of the resulting microgel were determined by transmission electron microscopy, hydrodynamic diameter of the microgel was characterized by dynamic light scattering. The objective of this work was to achieve the colon-specific delivery of an antiulcerative colitis drug using a fully nontoxic carrier. 5-aminosalicylic acid (5-ASA) was chosen as a model drug, which is rapidly absorbed before entering the colon, thus it is necessary to develop a colon-specific delivery system for it. The in vitro drug release profile was established in buffer solutions with 0.1 M HCl/NaCl (pH 1.2) and 0.1 M phosphate buffered saline (pH 7.4) at 37 °C. The results indicated that this OSA/CS core-shell microgel inhibited the release of 5-ASA in stomach to a certain extent and is degradable in physiological conditions. Due to the excellent biocompatible nature of CS and OSA, this core-shell microgel has good biocompatibility and may have potential applications in oral controlled drug delivery systems.
阳离子聚合物已被广泛用作药物传递系统。在此，通过水包油乳液法制备了氧化的海藻酸钠/壳聚糖（OSA/CS）核壳微凝胶。通过透射电子显微镜确定所得微凝胶的形态特性，通过动态光散射来表征微凝胶的水动力学直径。本工作的目的是使用完全无毒的载体实现溃疡性结肠炎药物的结肠特异性传递。选择 5-氨基水杨酸（5-ASA）作为模型药物，该药物在进入结肠之前被迅速吸收，因此需要为其开发结肠特异性传递系统。在 37°C下，在 0.1 M HCl/NaCl（pH 1.2）和 0.1 M 磷酸盐缓冲盐水（pH 7.4）的缓冲溶液中建立了体外药物释放曲线。结果表明，该 OSA/CS 核壳微凝胶在一定程度上抑制了 5-ASA 在胃中的释放，并且在生理条件下可降解。由于 CS 和 OSA 的优异的生物相容性，该核壳微凝胶具有良好的生物相容性，可能在口服控释药物传递系统中有潜在的应用。
