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Formulation of pH-responsive carboxymethyl chitosan and alginate beads for the oral delivery of insulin

机译:pH响应的羧甲基壳聚糖和藻酸盐微珠的配方,用于口服胰岛素

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摘要

pH-sensitive beads were prepared from the interpenetrating polymer networks (IPNs) of carboxymethyl chitosan (CMCTS) and alginate to study their application in oral insulin administration. CMCTS was synthesized from chitosan and was characterized by Fourier transform infrared spectroscopy and wide-angle X-ray diffraction. Calcium chloride, a relatively less toxic material, was used to crosslink both the alginate and CMCTS to prepare the IPN beads. The IPN beads were used to encapsulate insulin at different weight ratios. The swelling behavior and insulin release profile in response to simulated gastric and intestinal media of the beads were investigated. The beads observed under scanning electron microscopy were almost spherical, with an average diameter of 780 μm. The bead with about a 54% insulin loading efficiency was observed to contain about 98% encapsulated insulin. The maxima of about 20% insulin retention at acidic pH (1.2) and about 94% insulin release at intestinal pH (7.4) justified the good pH-responsive nature of these IPN beads. Moreover, the insulin released from the IPN beads was stable and biologically active.
机译:从羧甲基壳聚糖(CMCTS)和藻酸盐的互穿聚合物网络(IPN)制备pH敏感珠,以研究其在口服胰岛素给药中的应用。 CMCTS由壳聚糖合成,并通过傅里叶变换红外光谱和广角X射线衍射进行表征。氯化钙是一种毒性较小的物质,用于交联藻酸盐和CMCTS以制备IPN珠。 IPN珠用于封装不同重量比的胰岛素。研究了模拟珠粒的胃和肠介质的溶胀行为和胰岛素释放曲线。在扫描电子显微镜下观察到的珠几乎是球形的,平均直径为780μm。观察到具有约54%的胰岛素负载效率的珠子包含约98%的胶囊化胰岛素。在酸性pH(1.2)时约有20%的胰岛素保留,在肠道pH(7.4)时有约94%的胰岛素释放,这证明了这些IPN珠具有良好的pH响应特性。而且,从IPN磁珠释放的胰岛素是稳定的并且具有生物活性。

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