壳聚糖包裹的海藻酸钠-明胶-罗氏海盘车生物黏附微球的抗消化性溃疡作用

Effect of chitosan-coated alginate/gelatin gastric mucoadhesive Asterias rollestoni loaded microspheres on peptic ulcer

目的制备、表征壳聚糖包裹的海藻酸钠-明胶-罗氏海盘车生物黏附微球,评价其抗消化性溃疡的作用。方法采用油包水(water-in-oil,W/O)乳化技术制备微球,扫描电镜、激光散射粒度分析仪、组织存留量测定法、紫外-可见分光光度法分别表征微球表面形态、粒径和黏附百分率、微球的载药量和包封率、大鼠实验分析载药微球抗胃溃疡的作用。结果微球稳定性良好。呈类球形,表面褶皱,平均粒径为368.15μm,包封率为(98.55±0.09)%,生物黏附率为(90.42±0.15)%。大鼠实验表明,载药微球能降低溃疡指数,提高PGE2、NO、SOD的含量。结论壳聚糖包裹的载药生物黏附微球可能通过促进胃溃疡大鼠上皮细胞合成分泌、增强胃黏膜屏障作用和清除自由基等机制达到治疗胃溃疡的作用。

Objective To innovatively prepare chitosan-coated alginate/gelatin Asterias rollestoni loaded microspheres,evaluate their pharmaceutical characteristics and analyze their effect on peptic ulcer.Methods The bioadhesive microspheres were prepared using an emulsification technique.SEM,laser diffractometry,remaining quantity measurement and UV-VIS spectrophotometry were individually applied to analyze surface features,particle size,in situ bioadhesion percentage and drug loading of microspheres.Effect of microspheres on peptic ulcer was investigated by rat studies.Results Microspheres showed good stability,and almost spherical with shallow elevation on surfaces.The mean particle size of microspheres was 368.15μm,drug entrapment efficiency was（98.55±0.09）%,and in situ bioadhesion percentage was（90.42±0.15）%.Studies in rats indicated that the microspheres could decrease ulcer index and enhance PGE2、NO、SOD contention.Conclusion Effect mechanism of chitosan-coated alginate/gelatin gastric mucoadhesive Asterias rollestoni loaded microspheres on peptic ulcer might be promotion of synthesis and secretion of epithelial cell,enhancement of barrier function of gastric mucosa and free radical scavenging.