壳聚糖-猪牙皂皂苷纳米微球的制备及其工艺优化

Preparation of Chitosan-Fructus Gleditsiae Saponin Nanospheres and Optimization of Its Process

目的以壳聚糖(CS)为载体制备壳聚糖-猪牙皂皂苷纳米微球(CS-SFGS-NPs),并考察其理化性质和体外释药性能。方法提取猪牙皂皂苷,利用紫外分光光度法测定皂苷含量。采用离子交联法制备壳聚糖-猪牙皂皂苷纳米微球,并以壳聚糖质量浓度、三聚磷酸钠(TPP)质量浓度、投料质量比为考察对象,以平均粒径、包封率为评价指标优化壳聚糖-猪牙皂皂苷纳米微球处方;采用Malvern粒度仪测定壳聚糖-猪牙皂皂苷纳米微球的粒径分布和Zeta电位,透射电子显微镜考察其形态;以透析法考察壳聚糖-猪牙皂皂苷纳米微球的体外释药行为。结果壳聚糖-猪牙皂皂苷纳米微球的最优处方:壳聚糖质量浓度为2.0 mg/m L、三聚磷酸钠质量浓度为1.5 mg/m L、壳聚糖-猪牙皂皂苷投料比为4∶1;制备的壳聚糖-猪牙皂皂苷纳米微球的包封率为84.7%±3.6%、粒径为(182.6±35.4)nm、Zeta电位为(+23.1±4.6)mV;透射电镜结果显示所制备的壳聚糖-猪牙皂皂苷纳米微球为类球形颗粒,大小分布较为均匀;壳聚糖-猪牙皂皂苷纳米微球在0.5h内的释放量低于40%。结论通过对处方的优化,制备得到的壳聚糖-猪牙皂皂苷纳米微球具有合适的粒径和包封率,并能达到缓释效果。

Objective To prepare chitosan-Fructus Gleditsiae saponin nanospheres(CS-SFGS-NPs)with chitosan(CS)as carrier,and to investigate its physicochemical properties and in vitro release properties.Methods Fructus Gleditsiae saponin was extracted and the content of saponin was determined by uv spectrophotometry.The CS-SFGS-NPs were prepared by ion cross-linking method,and the CS mass concentration,sodium tripolyphosphate(TPP)mass concentration and feed mass ratio were investigated.The average particle size and encapsulation efficiency were determined.The CS-SFGS-NPs were optimized for evaluation.The particle size distribution and zeta potential of CS-SFGS-NPs were determined by Malvern particle size analyzer.The morphology was investigated by transmission electron microscopy.In vitro release behavior of CS-SFGS-NPs was detected.Results The optimal formulation of CS-SFGS-NPs:CS mass concentration 2.0 mg/mL,sodium tripolyphosphate concentration was 1.5 mg/mL,the feed ratio of porphyry saponin was 4∶1;the encapsulation efficiency of CS-SFGS-NPs was84.7%±3.6%,the particle size was(182.6±35.4)nm,and the zeta potential was(+23.1±4.6)mV;transmission electron microscopyresults showed that the prepared CS-SFGS-NPs are spherical particles with uniform size distribution;the release of CS-SFGSNPs was less than 40%in 0.5 h.Conclusion The CS-SFGS-NPs prepared by the optimization of the prescription has suitable particle size and encapsulation efficiency,and can achieve sustained release effect.