槲皮素/壳聚糖纳米粒的制备、表征及其体外抗氧化活性研究  

Preparation,characterization and antioxidation activity in vitro of quercetin loaded chitosan nanoparticles

作　　者：刘康[1] 秦梦[1] 杨婷婷[1] 石玮玮[1] 唐铭泽 唐金宝[1] 张维芬[1] 

机构地区：[1]潍坊医学院药学院,山东潍坊261053 [2]山东省寿光市第一中学,山东寿光262700

出　　处：《中国生化药物杂志》2016年第11期17-21,共5页Chinese Journal of Biochemical Pharmaceutics

基　　金：国家自然科学基金(81573717);国家科技部科技计划项目(2013GA740103);山东省自然科学基金(ZR2012CM025);山东省医药卫生科技发展计划项目(2015WS0057);山东省潍坊市科技计划项目(2014WS045)

摘　　要：目的制备载槲皮素(quercetin,QUE)的壳聚糖纳米粒(chitosan nanoparticles,CS-NPs)并考察其理化特性及体外抗氧化活性。方法采用离子交联法和自组装法制备了QUE-CS-NPs,并且以载药量,包封率为指标优化纳米粒的制备工艺,在此基础上以粒径和包封率为指标采用正交实验设计优化筛选纳米粒的处方。透射电镜表征QUE-CS-NPs的形态,动态光散射粒度仪测定QUE-CS-NPs粒径,多分散系数和电位大小。用0.5%的SDS溶液为释放介质,研究其体外释药行为,并且通过QUE-CS-NPs对HO·和O_2^-·的清除作用考察其体外抗氧化活性。结果制备的QUE-CS-NPs为圆形且分布均匀,平均粒径为(282.9±20)nm,多分散系数为0.185,Zeta电位为(30.5±2)m V,平均包封率为(80.02±1.04)%,载药量为(8.81±0.65)%。QUE-CS-NPs在72h内药物累积释放率66.2%具有明显的缓释效果。QUE-CS-NPs对HO·和O_2^-·具有较强的清除作用显示出了浓度依赖性,且清除作用高于QUE。结论 QUE-CS-NPs具有合适的粒径,明显的缓释效果和较强的体外抗氧化作用。Objective To prepare quercetin（ QUE） loaded chitosan nanoparticles（ CS-NPs）,evaluate its physicochemical properties and antioxidation activity in vitro. Methods Quercetin chitosan nanoparticles were prepared by ionic crosslinking method and self-assembly method. The preparation method was optimized using entrapment efficiency（ EE）,drug loading（ DL） and size as indexes. The best formulation and preparation conditions were optimized by orthogonal test based on single-factor test,evaluation indicator as particle size and EE. The physicochemical properties of the obtained QUE-CS-NPs were characterized by the following methods： the transmission electron microscope（ TEM）,dynamic light scattering（ DLS）analysis for morphology,size distribution and Zeta potential. In vitro release behavior in 0. 5% SDS solution was evaluated by dialysis tube method. In vitro antioxidant activity assays were performed by evaluating the abilities of the microspheres for hydroxide radicals and superoxide anions. Results TEM results revealed QUE-CS-NPs with round and uniform. Particle-size analysis showed that the diameters and Zeta potential of the QUE-CS-NPs were（ 282. 9 ± 20） nm and（ 30. 5 ± 2） m V,with uniform distribution（ polydispersity below 0. 185）. DL and EE of QUE-CS-NPs were（ 8. 81 ± 0. 65） %and（ 80. 02 ± 1. 04） %,respectively. QUE-CS-NPs showed extended administration times with 66. 2% cumulative release within 72 h. QUE-CS-NPs showed pronounced antioxidant activity and a concentration dependent,even more substantial than that of pure QUE. Conclusion QUE-CS-NPs show a good size,sustain release effect and pronounce antioxidant activity.

关 键 词：槲皮素 壳聚糖 纳米粒 体外释放 体外抗氧化活性 

分 类 号：Q946.833[生物学—植物学]