Yao Yashu, Xia Mengxin, Wang Huizhen, Li Guowen, Shen Hongyi, Ji Guang, Meng Qianchao, Xie Yan
Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Research Center for Health and Nutrition, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Eur J Pharm Sci. 2016 Aug 25;91:144-53. doi: 10.1016/j.ejps.2016.06.014. Epub 2016 Jun 18.
A novel nanogel/gel based on chitosan (CS) for the oral delivery of myricetin (Myr) was developed and evaluated comprehensively. The particle size of the obtained Myr-loaded CS/β-glycerol phosphate (β-GP) nanogels was in the range of 100-300nm. The rheological tests showed that the sol-gel transition happened when the nanogels were exposed to physiological temperatures, and 3D network structures of the gelatinized nanogels (gels) were confirmed by Scanning Electron Microscopy. Myr was released from CS/β-GP nanogel/gel in acidic buffers via a Fickian mechanism, and this release was simultaneously accompanied by swelling and erosion. Moreover, the nanogel/gel exhibited no cytotoxicity by MTT assay, and the oral bioavailability of Myr in rats was improved with an accelerated absorption rate after Myr was loaded into CS/β-GP nanogel/gel. In summary, all of the above showed that CS/β-GP nanogel/gel was an excellent system for orally delivering Myr.
开发并全面评估了一种基于壳聚糖（CS）的新型纳米凝胶/凝胶，用于杨梅素（Myr）的口服给药。所制备的负载Myr的CS/β-甘油磷酸酯（β-GP）纳米凝胶的粒径在100-300nm范围内。流变学测试表明，当纳米凝胶暴露于生理温度时会发生溶胶-凝胶转变，并且通过扫描电子显微镜确认了凝胶化纳米凝胶（凝胶）的三维网络结构。Myr通过菲克扩散机制在酸性缓冲液中从CS/β-GP纳米凝胶/凝胶中释放出来，并且这种释放同时伴随着溶胀和侵蚀。此外，通过MTT法测定，纳米凝胶/凝胶没有细胞毒性，并且在将Myr负载到CS/β-GP纳米凝胶/凝胶中后，大鼠体内Myr的口服生物利用度提高，吸收速率加快。总之，上述所有结果表明CS/β-GP纳米凝胶/凝胶是口服递送Myr的优良体系。
