Wong Tin W, Sumiran Nurjaya
Non-Destructive Biomedical and Pharmaceutical Research Centre, Universiti Teknologi MARA, Puncak Alam, Selangor, Malaysia; Particle Design Research Group, Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam, Selangor, Malaysia.
J Pharm Pharmacol. 2014 May;66(5):646-57. doi: 10.1111/jphp.12192. Epub 2013 Dec 11.
Examine the formation of pectin-insulin nanoparticles and their blood glucose lowering properties.
The calcium pectinate nanoparticles were prepared by ionotropic gelation method, with alginate, sodium chloride or Tween 80 as additive. Their in vitro physicochemical, drug release and in vivo blood glucose lowering characteristics were evaluated.
Spherical calcium pectinate-insulin nanoparticles were characterized by size, zeta potential, insulin content and insulin association efficiency of 348.4 ± 12.9 nm, -17.9 ± 0.8 mV, 8.4 ± 1.0% and 63.8 ± 7.4%, respectively. They released less than 25% insulin following 24 h in simulated intestinal medium and exhibited delayed blood glucose lowering effect in rats. Incorporation of solubilizer sodium chloride or Tween 80 into nanoparticles did not enhance blood glucose lowering capacity owing to sodium chloride reduced matrix insulin content and Tween 80 interacted with water and had its blood glucose dilution effect negated. Combination of nanoparticles with alginate gel to allow prolonged intestinal residence and more insulin release did not enhance their blood glucose lowering capacity because of calcium alginate-cross-linked gel formation that could retard insulin release and migration into systemic circulation.
Physicochemical responses of additives in vivo affected blood glucose regulation property of pectin-insulin nanoparticles.
研究果胶-胰岛素纳米粒的形成及其降血糖特性。
采用离子凝胶法制备果胶钙纳米粒，以海藻酸盐、氯化钠或吐温80作为添加剂。对其体外理化性质、药物释放及体内降血糖特性进行评价。
球形果胶钙-胰岛素纳米粒的粒径、ζ电位、胰岛素含量及胰岛素结合率分别为348.4 ± 12.9 nm、-17.9 ± 0.8 mV、8.4 ± 1.0%和63.8 ± 7.4%。在模拟肠液中24小时后，它们释放的胰岛素不到25%，并且在大鼠体内表现出延迟的降血糖作用。向纳米粒中加入增溶剂氯化钠或吐温80并未增强其降血糖能力，因为氯化钠降低了基质中的胰岛素含量，而吐温80与水相互作用，其血糖稀释作用被抵消。纳米粒与海藻酸盐凝胶结合以延长肠道滞留时间并增加胰岛素释放，但并未增强其降血糖能力，因为形成的海藻酸钙交联凝胶会阻碍胰岛素释放并迁移至体循环。
添加剂在体内的理化反应影响了果胶-胰岛素纳米粒的血糖调节特性。
