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聚电解质多层微胶囊对胃蛋白酶侵蚀的增强抗性及包封吲哚美辛的释放特性

Enhanced resistance of polyelectrolyte multilayer microcapsules to pepsin erosion and release properties of encapsulated indomethacin.

作者信息

Wang Chaoyang, Ye Shiqu, Dai Lin, Liu Xinxing, Tong Zhen

机构信息

Research Institute of Materials Science, South China University of Technology, Guangzhou 510640, China.

出版信息

Biomacromolecules. 2007 May;8(5):1739-44. doi: 10.1021/bm070110z. Epub 2007 Apr 26.

Abstract

Polyelectrolyte multilayer films were prepared through layer-by-layer (LbL) self-assembly using polysaccharide sodium alginate (ALG) and chitosan (CHI). After incubation in an enzyme pepsin solution, the multilayer film was partially destroyed as detected by the decrease in fluorescent intensity because of the enzymatic degradation of CHI. The enzymatic desorption was also observed from the microcapsule wall made of the ALG/CHI multilayer film directly deposited on indomethacin (IDM) microcrystals through LbL self-assembly. After pepsin erosion, the IDM release from the microcapsules monitored by UV absorbance was obviously accelerated because of desorption. To enhance the stability of the ALG/CHI multilayer film to the enzymatic erosion, some physical and chemical methods were established to increase film thickness or to cross-link the polysaccharides within the film. Increasing the layer number and raising the deposition temperature effectively slowed down the enzymatic desorption and release rate. Especially, increasing deposition temperature was more effective because of producing a more perfect structure in the ALG/CHI multilayer film. Cross-linking the neighboring layers of ALG and CHI with 1-ethyl-3-(3-dimethylamino-propyl)carbodiimide in the ALG/CHI multilayer film significantly reduced the enzymatic desorption and release rate. Therefore, increasing deposition temperature and cross-linking neighboring layers are effective methods to protect the multilayer film fabricated using LbL assembly from the enzymatic erosion and to prolong the release of the encapsulated drug.

摘要

通过层层(LbL)自组装,使用多糖海藻酸钠(ALG)和壳聚糖(CHI)制备了聚电解质多层膜。在酶促胃蛋白酶溶液中孵育后,由于CHI的酶促降解,荧光强度降低,检测到多层膜部分被破坏。还观察到通过LbL自组装直接沉积在吲哚美辛(IDM)微晶上的由ALG/CHI多层膜制成的微胶囊壁发生酶促解吸。胃蛋白酶侵蚀后,由于解吸作用,通过紫外吸光度监测的微胶囊中IDM的释放明显加速。为了提高ALG/CHI多层膜对酶促侵蚀的稳定性,建立了一些物理和化学方法来增加膜厚度或使膜内的多糖交联。增加层数和提高沉积温度有效地减缓了酶促解吸和释放速率。特别是,提高沉积温度更有效,因为在ALG/CHI多层膜中产生了更完美的结构。在ALG/CHI多层膜中用1-乙基-3-(3-二甲基氨基丙基)碳二亚胺交联ALG和CHI的相邻层显著降低了酶促解吸和释放速率。因此,提高沉积温度和交联相邻层是保护使用LbL组装制备的多层膜免受酶促侵蚀并延长包封药物释放的有效方法。

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