超分子水凝胶作为胰岛素缓释体系的研究  

Supramolecular Hydrogels as Carriers for Sustained Insulin Release

作　　者：孙立泷[1,2] 许韵华[1] 朱雯[2] 彭勃[3] 陈永明[2,3] 白茹 

机构地区：[1]北京交通大学理学院化学系,北京100044 [2]中国科学院化学研究所,北京100190 [3]中山大学化学与化学工程学院,广州510275 [4]深圳君圣泰生物技术有限公司,深圳518057

出　　处：《高分子学报》2015年第6期673-678,共6页Acta Polymerica Sinica

基　　金：国家自然科学基金(基金号21090353;51203171)资助

摘　　要：利用α-环糊精(α-CD)与含有聚乙二醇(PEG)链段的聚合物Pluronic F127的超分子作用制备水凝胶.该物理交联水凝胶的交联点包括α-CD与PEG链包合物堆积形成的微晶区和聚合物疏水链段聚集区.优化水凝胶组分,得到具有较低固含量和较短凝胶化时间的体系用于胰岛素的负载和释放研究.通过X射线衍射(XRD),扫描显微镜(SEM)对水凝胶结构进行表征.通过紫外分光光度计监测胰岛素的释放过程,结果表明,水凝胶释药时间约为65 h,且释放曲线较为平缓.细胞毒性实验结果表明该水凝胶材料对细胞生长无明显抑制作用.小鼠体内释药实验结果表明该水凝胶载体对延长胰岛素的释药时间有一定效果,可作为多肽类药物的缓释体系.The supramolecular inclusion of α-cyclodextrin（ α-CD） and PEG contained block copolymer Pluronic F127 was used to build a supramolecular hydrogel system. The composition and gelation behavior of the system were evaluated. There were two kinds of crosslinks in the hydrogels. One was the microcrystalline structure of packed PEG / α-CD inclusion complexes,and the other was the aggregated hydrophobic blocks of Pluronic F127. An optimized gel system with low solid content（ 17. 7 wt%） and short gelation time（ 6 ~ 8min） was established for sustained release of insulin. The structure of α-CD and PEG inclusion was characterized by wide-angle X-ray diffraction（ XRD）. The scanning electron microscopy（ SEM） images of the freeze-dried powders of the gels showed a porous structure,because of the high water content of the hydrogels.In vitro insulin release was monitored by UV analysis,and the release was sustained in 65 h with a burst release of 30% in the first 5 h. In vitro cytotoxicity studies showed that the hydrogels（ without insulin） had no evident growth inhibition to BEL-7402 cells when the concentration was lower than 109 mg / L. Animal experiment showed that the hydrogel was positive to prolong the in vivo insulin release. These results suggested that the supramolecular hydrogels hold great potential as a sustained delivery system of hydrophilic drugs and proteins,such as insulin.

关 键 词：环糊精 嵌段聚合物 聚乙二醇 超分子水凝胶 胰岛素 

分 类 号：TQ427.26[化学工程] TQ460.1