Key Laboratory of Synthetic and Biological Colloids, Ministry of Education, Wuxi 214122, Jiangsu Province, People's Republic of China; School of Food Science and Technology, Jiangnan University, Wuxi 214122, Jiangsu Province, People's Republic of China; Collaborative Innovation Center for Food Safety and Quality Control, Jiangnan University, Wuxi 214122, Jiangsu Province, People's Republic of China.
Institute of Agro-products Processing Science and Technology, Academy of Agricultural Science, Nanning 530007, Guangxi Province, People's Republic of China.
Carbohydr Polym. 2022 Sep 1;291:119571. doi: 10.1016/j.carbpol.2022.119571. Epub 2022 May 6.
A porous starch-based carrier coated with chitosan-phytic acid was designed for oral administration to improve drug delivery to the colon. Using hydrophobic paclitaxel as a model drug, improved drug loading (15.12% ± 0.31%) and entrapment efficiency (86.63 ± 1.30%) of porous starch were achieved by size/shape matching and adsorption force. Fluorescent paclitaxel particles inside starch were captured clearly. Furthermore, chitosan-phytic acid was added as a second protection since porous starch showed a dissolution rate of only 14.98-20.27% during the simulated digestion in stomach and small intestine, which was far lower than that of raw paclitaxel in porous starch (59.65 ± 2.57%). The release curve in the colon was also obtained and showed that 86.98 ± 2.90% of the drug was released. Finally, we verified the non-covalent interactions between starch and paclitaxel. This showed that the retention of paclitaxel into porous starch decreased once hydrogen bonding stopped. The hydrophobic CH-π effect provides a binding complementing contribution.
设计了一种多孔淀粉为载体，壳聚糖-植酸为涂层的口服给药载体，以改善药物向结肠的传递。以疏水性紫杉醇为模型药物，通过大小/形状匹配和吸附力，实现了多孔淀粉的载药量（15.12%±0.31%）和包封率（86.63%±1.30%）的提高。荧光紫杉醇颗粒在淀粉内清晰可见。此外，添加壳聚糖-植酸作为第二层保护，因为多孔淀粉在胃和小肠的模拟消化中仅显示 14.98-20.27%的溶解率，远低于多孔淀粉中原紫杉醇的溶解率（59.65%±2.57%）。还获得了在结肠中的释放曲线，显示 86.98%±2.90%的药物被释放。最后，我们验证了淀粉和紫杉醇之间的非共价相互作用。这表明一旦氢键停止，紫杉醇在多孔淀粉中的保留就会减少。疏水 CH-π 效应提供了一种互补的结合贡献。
