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用于口服胰岛素传递的 pH 敏感 N-琥珀酰壳聚糖接枝聚丙烯酰胺水凝胶。

pH sensitive N-succinyl chitosan grafted polyacrylamide hydrogel for oral insulin delivery.

机构信息

Department of Polymer Science and Technology, University of Calcutta, 92, A.P.C. Road, Kolkata 700009, India.

Department of Physiology, University of Calcutta, 92, A.P.C. Road, Kolkata 700009, India.

出版信息

Carbohydr Polym. 2014 Nov 4;112:627-37. doi: 10.1016/j.carbpol.2014.06.045. Epub 2014 Jun 28.

Abstract

pH sensitive PAA/S-chitosan hydrogel was prepared using ammonium persulfate (APS) as an initiator and methylenebisacrylamide (MBA) as a crosslinker for oral insulin delivery. The synthesized copolymer was characterized by Fourier transform infrared spectroscopy (FT-IR) and X-ray diffraction (XRD) study; morphology was observed under scanning electron microscope (SEM). The PAA/S-chitosan with ∼ 38% of insulin loading efficiency (LE) and ∼ 76% of insulin encapsulation efficiency (EE), showed excellent pH sensitivity, retaining ∼ 26% of encapsulated insulin in acidic stomach pH 1.2 and releasing of ∼ 98% of insulin in the intestine (pH 7.4), providing a prolonged attachment with the intestinal tissue. The oral administration of insulin loaded PAA/S-chitosan hydrogel was successful in lowering the blood glucose level of diabetic mice. The bioavailability of insulin was ∼ 4.43%. Furthermore, no lethality or toxicity was documented after its peroral administration. Thus, PAA/S-chitosan hydrogel could serve as a promising oral insulin carrier in future.

摘要

采用过硫酸铵 (APS) 作为引发剂,亚甲基双丙烯酰胺 (MBA) 作为交联剂,制备了对 pH 敏感的 PAA/S-壳聚糖水凝胶,用于口服胰岛素传递。合成的共聚物通过傅里叶变换红外光谱 (FT-IR) 和 X 射线衍射 (XRD) 研究进行了表征;通过扫描电子显微镜 (SEM) 观察了形态。PAA/S-壳聚糖的胰岛素负载效率 (LE) 约为 38%,胰岛素包封效率 (EE) 约为 76%,具有优异的 pH 敏感性,在酸性胃 pH 值 1.2 下保留约 26%的包封胰岛素,在肠道 (pH 值 7.4) 中释放约 98%的胰岛素,从而与肠道组织长时间附着。胰岛素负载的 PAA/S-壳聚糖水凝胶的口服给药成功降低了糖尿病小鼠的血糖水平。胰岛素的生物利用度约为 4.43%。此外,口服给药后没有记录到致死性或毒性。因此,PAA/S-壳聚糖水凝胶有望成为未来有前途的口服胰岛素载体。

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