College of Chemical Engineering, Xinjiang Agricultural University, Urumchi 830052, Xinjiang, People's Republic of China.
College of Chemical Engineering, Xinjiang Agricultural University, Urumchi 830052, Xinjiang, People's Republic of China.
Int J Biol Macromol. 2019 Sep 15;137:512-520. doi: 10.1016/j.ijbiomac.2019.07.011. Epub 2019 Jul 2.
To overcome the instability of pectin-Ca gels based oral colon-specific drug delivery system (OCDDS) in the upper gastrointestinal tract, the chemical cross-linked pectin carriers were prepared by adding succinic anhydride and glutaric dialdehyde as the cross-linking reagents. The diclofenac sodium was employed as the water-soluble drug model to calculate the controlled release properties. The encapsulation efficiency and loading efficiency were measured and the sample PG1 shows the best efficiency of 78.81% and 7.78%, respectively. The simulative release rate was estimated and the cumulative release rate of sample PG reached to a maximum of 3.04, 3.66 and 79.43% in SGF, SSIF and SCF. The release data was employed to fit the First order, Higuchi, Bhaskar, and Ritger-peppas model and the goodness of the fit was calculated by the regression coefficient. The succinic anhydride and glutaric dialdehyde cross-linked pectin were characterized by FTIR to prove the cross-linking reaction. In addition, FE-SEM characterization of sample PG1 indicated the rally microsphere with smooth surface. The sample PG1 after the digestion was also characterized by the FE-SEM, and irregularly structure was obtained.
为了克服果胶-Ca 凝胶在上消化道中不稳定的问题,本研究采用琥珀酸酐和戊二醛作为交联试剂,制备了化学交联的果胶载体。以双氯芬酸钠为水溶性药物模型,计算了控制释放性能。测量了包封效率和载药效率,样品 PG1 表现出最好的效率,分别为 78.81%和 7.78%。估计了模拟释放率,样品 PG 在 SGF、SSIF 和 SCF 中的累积释放率分别达到 3.04%、3.66%和 79.43%。通过回归系数计算了拟合度,将释放数据拟合到一阶、Higuchi、Bhaskar 和 Ritger-peppas 模型中。采用傅里叶变换红外光谱(FTIR)对琥珀酸酐和戊二醛交联的果胶进行了表征,以证明交联反应的发生。此外,通过 FE-SEM 对样品 PG1 进行了表征,结果表明其为表面光滑的团聚微球。对经过消化的样品 PG1 也进行了 FE-SEM 表征,得到了不规则的结构。