生物黏附性三七总皂苷-白及多糖-海藻酸钠复合微球的制备及表征

Preparation and characterization of bioadhesive Bletilla striata polysaccharide and sodium alginate microspheres loaded with Panax notoginseng saponins

目的利用白及多糖(BSP)的生物黏附性,与海藻酸钠(SA)混合作为复合载体,以具有缓释特性的三七总皂苷(PNS)分散体作为包封药物,制备具有生物黏附性的PNS-BSP-SA复合微球。方法采用离子交联法制备微球,通过单因素试验和正交设计考察并优化处方工艺。通过扫描电镜(SEM)、粒径分布、差示扫描量热法(DSC)分析、溶胀性能测定、体外黏附性能评价、体外释放研究对微球进行表征。结果 PNS-BSP-SA复合微球圆整度较好,表面粗糙不平有褶皱,粒径分布较窄,PNS原料药以无定形状态均匀分散于微球中。最佳处方工艺制备的微球工艺稳定,重现性较好,与直接加入PNS原料药制备的微球相比,PNS分散体微球的载药量、包封率和得率均明显增加,分别为10.34%、51.25%、82.21%,而PNS原料药微球的载药量、包封率、得率分别为4.04%、12.16%、61.35%。BSP的加入增加了SA微球的溶胀性能,明显增加了其在大鼠胃部的滞留率。PNS-BSP-SA复合微球中人参皂苷Rg1的释放较PNS原料药缓慢。结论 BSP增加了微球的生物黏附性,将PNS制备为分散体,提高了微球的载药量、包封率和得率,并使微球具有一定的缓释性能。

Objective Because of the adhesion of Bletilla striata polysaccharide(BSP), it was mixed with sodium alginate(SA) as a composite carrier to prepare mucoadhesive PNS-BSP composite microspheres. Panax notoginseng saponins(PNS) dispersion with sustained release property was used as an encapsulating drug. Methods The composite microsphere was prepared by ion cross-linking method. The formulation process was investigated and optimized by single factor test and orthogonal design. The microspheres were evaluated by scanning electron microscope(SEM), particle size distribution, DSC, swelling properties, in vitro mucoadhesive properties, and in vitro release characteristics. Results PNS-BSP composite microspheres had good roundness, rough surface and wrinkles. The microspheres showed a narrow size distribution. PNS was uniformly dispersed in microspheres in an amorphous state. The microspheres prepared by the best prescription process were stable in process and reproducible. Compared with the microspheres prepared by directly adding PNS, the drug loading, encapsulation efficiency and yield of PNS dispersion microspheres were increased significantly, which were 10.34%, 51.25%, and 82.21%, respectively. The drug loading, encapsulation efficiency, and yield were 4.04%, 12.16%, and 61.35% of PNS microspheres. The addition of BSP increased the swelling properties of the SA microspheres, and significantly increased the retention rate in the stomach of rats. The release of ginsenoside Rg1 in PNS-BSP microspheres was released slower compared to PNS. Conclusion The bioadhesion of microspheres was increased by the addition of BSP. The drug loading, encapsulation efficiency, and yield of the microspheres were increased by the preparation of PNS as a dispersion, and the microspheres also had a certain sustained-release effect.