In Vitro Degradation and Drug-Release Properties of Water-Soluble Chitosan Cross-Linked Oxidized Sodium Alginate Core-Shell Microgels
In Vitro Degradation and Drug-Release Properties of Water-Soluble Chitosan Cross-Linked Oxidized Sodium Alginate Core-Shell Microgels
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DOI：
10.1163/092050611x601720
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发表时间：
2012-01-01
影响因子：
3.6
通讯作者：
Chen, Jiucun
中科院分区：
文献类型：
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作者：
Chen, Chen;Liu, Mingzhu;Chen, Jiucun
基于海藻酸钠（SA）的水凝胶已经广泛用于使用Ca 2+作为交联剂的生物医学应用中;然而，这些水凝胶倾向于在电解质溶液中崩解。为了解决这一问题，我们以水溶性壳聚糖（WSC）为交联剂制备了氧化海藻酸钠（OSA）微凝胶。该微凝胶是在室温下通过乳液交联技术成功制备的。该微凝胶通过形成席夫碱键和席夫碱间络合物进行交联，有效地消除了微凝胶在电解质溶液中的崩解。用透射电子显微镜（TEM）表征了微凝胶的形貌，用动态光散射（DLS）表征了微凝胶的流体力学直径。这项工作的目的是实现结肠特异性递送抗溃疡性结肠炎药物。5-选择氨基水杨酸（5-阿萨）作为模型药物，并在37 ℃下在含有0.1 M HCl/NaCl（pH 1.2）和0.1 M磷酸盐缓冲盐水（PBS，pH 7.4）的缓冲溶液中建立体外药物释放曲线。将微凝胶在0.1M PBS（pH 7.4）中在37 ℃下孵育以确定其降解行为。MTT法检测细胞毒性结果表明，该微凝胶无明显的细胞毒性。这些结果表明，通过将WSC引入OSA制备的微凝胶可能在口服控释系统中具有潜在的应用。因此，OSA/WSC微凝胶可能是一种有用的载体，用于结肠特异性递送抗炎药物，包括5-阿萨和增强溃疡性结肠炎的治疗效果。(C)Koninklijke Brill NV，莱顿，2011年
Hydrogels based on sodium alginate (SA) have already been widely used in biomedical applications using Ca2+ as a cross-linker; however, these hydrogels tend to disintegrate in electrolyte solutions. To solve this problem, we present a kind of oxidized sodium alginate (OSA) microgel using water-soluble chitosan (WSC) as a cross-linker. This microgel was successfully prepared via an emulsion cross-linking technique at room temperature. The microgel was cross-linked by the formation of both Schiff base bonds and inter-polyelectrolyte complexes, which can efficiently eliminate the disintegration of the microgel in electrolyte solutions. Morphological properties of the resulting microgels were determined by transmission electron microscopy (TEM), hydrodynamic diameters of the microgels were characterized by dynamic light scattering (DLS). The objective of this work was to achieve the colon-specific delivery of an anti-ulcerative colitis drug. 5-Aminosalicylic acid (5-ASA) was chosen as a model drug and 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 (PBS, pH 7.4) at 37 degrees C. The microgel was incubated in 0.1 M PBS (pH 7.4) at 37 degrees C to determine its degradation behavior. Cell cytotoxicity (tested by MTT assay) showed that this microgel had no significant cytotoxicity. These results indicated that this microgel prepared by introducing WSC into OSA may have potential applications in oral controlled drug-delivery systems. Therefore, the OSA/WSC microgel may be a useful carrier for the colon-specific delivery of anti-inflammatory drugs including 5-ASA and the enhanced therapeutic effect of ulcerative colitis. (C) Koninklijke Brill NV, Leiden, 2011