藤黄酸白蛋白纳米粒的制备及稳定性研究

Studies on preparation and stability of human serum albumin nanoparticles containing gambogic acid

目的以人血清白蛋白为载体制备藤黄酸白蛋白纳米粒,对处方和工艺进行优化,并进行稳定性考察。方法采用新型白蛋白纳米制备技术(Nab^(TM))制备藤黄酸白蛋白纳米粒(GA-HSA NPs),用透射电镜观察纳米粒的形态,用Nicomp TM PSS 380进行粒度仪测定其粒度分布及电位,超速离心法测定其包封率、载药率及过膜效率,并考察其稀释稳定性及储存稳定性。结果 GA-HSA NPs电镜下呈球状粒子,粒径为(103.2±34.4)nm,zeta电位为-25.10 mV,GA-HSA NPs具有较高的包封率、载药率和过膜效率。GA-HSA NPs冻干粉针储存12个月期间无塌陷或皱缩,GA-HSA NPs混悬液在储存6周内粒径无显著性变化。结论难溶性抗癌药物藤黄酸可以采用NabTM制备成白蛋白纳米粒,其粒径小,稳定性高,有望成为藤黄酸的新型给药系统。

Objective To develop human serum albumin(HSA) nanoparticles(NPs) as polymeric vehicles for intravenous injection of gambogic acid(GA), to optimize the formulation thereof and evaluate its stability. Methods GA-HSA NPs were prepared by the nanoparticle albumin-bound technology(Nab^(TM)). The morphology of the NPs was observed by TEM. The distribution of particle size and zeta potential of the NPs were determined by Nicomp TM PSS 380. The encapsulation efficiency(EE), drug-loading capacity(GA-LC) and filtration efficiency of the NPs were examined by ultracentrifugation method. And the stability upon dilution and storage stability were also investigated. Results GA-HSA NPs showed spherical in shape with a particle size of(103.2 ± 34.4) nm and a zeta potential of-25.10 mV. And high entrapment efficiency was achieved. Freeze–dried GA-HSA NPs showed no collapse or shrinkage after 12 months, and GA-HSA NP suspension demonstrated significant changes within 6 weeks. Conclusions This formulation could significantly increase the concentration of GA in water. GA-HSA NPs prepared by this method exhibited a small particle size, high stability. Therefore, this delivery system is a promising polymeric carrier for the transport of GA.