酶响应型捏合淀粉药物载体的制备和性能

Preparation and Characterization of Enzyme-Responsive Knead Starch-Based Drug Carriers

采用机械捏合的方法制备了不同抗消化性能的捏合淀粉基载体材料。利用扫描电子显微技术(SEM)、X射线衍射技术(XRD)和体外模拟人体消化试验(In-Vitro)对捏合淀粉的颗粒形貌、结晶结构和在人体上消化道中的消化性能进行了考察。发现随着抗消化性能的降低,淀粉颗粒的破损程度越大,淀粉结晶结构结晶形态由B型向V型转变,消化速度增大。同时以胰酶为模型药物,考察了捏合淀粉对药物的体外释放性能。结果显示,不同抗消化性能的捏合淀粉可望作为不同消化道靶向要求的药物载体材料。

Knead starch-based carriers with different digestion resistivity were obtained. The granule appearance, the crystal structure and the digestion rate in the upper gastrointestinal tract of kneaded starches were investigated by using the technique of scanning electron microscopy （SEM）, X- ray diffraction and In-Vitro enzymatic digestion test. The results indicate that the surface of the sample granule becomes rougher as the digestion resistance ability decreased, and that the crystal structure changes from B-type to V-type, and that the degradability of kneaded starch carrier materials is increased indicating the different enzyme-responsive of kneaded starch carriers. Furthermore, Starch-based matrix tablets for macromolecular drugs were designed using pancreatic enzyme as drug model. The pancreatic enzyme release in simulated gastric fluid and in simulated intestinal fluid from matrix tablets was investigated. It is found that the kneaded starches with different digestion resistivity can be used as drug carriers for different gastrointestinal tract target drug delivery.