灯盏花素羧甲基壳聚糖鼻黏膜微球的研制

Preparation of Carboxymethyl Chitosan Microspheres Loaded with Breviscapine for Nasal Mucous

目的:对灯盏花素(BRE)鼻黏膜微球的制备工艺进行优化,并对其体外质量进行考察,为进一步体内实验奠定基础。方法:以羧甲基壳聚糖(CMCS)为载体,采用喷雾干燥法制备BRE微球。以包封率及载药量的综合评分为评价指标,采用正交试验优化其处方及制备工艺,并对其形态、粒径及体外释药特性进行考察。结果:优选出的BRE微球最佳制备条件为:CMCS浓度为0.8 g·ml^-1,BRE∶CMCS为1∶5(g∶g),CMCS∶三聚磷酸钠(TPP)为15∶1(g∶g),蠕动泵速度为20 ml·min^-1。BRE微球外形圆整光滑,粒径均匀,体外释药呈明显缓释性,包封率和载药量分别为(68.33±0.35)%和(16.26±0.42)%。结论:BRE-CMCS微球制备简单,体外质量理想,值得进一步研究。

Objective:To optimize the preparation of breviscapine(BRE)microspheres for nasal mucosa,and study the quality in vitro,so as to lay foundation for in vivo studies.Methods:Carboxymethyl chitosan(CMCS)was used as the matrix,and spray-drying technology was applied to prepare BRE microspheres.The formula and preparation parameters were optimized by orthogonal design using the comprehensive score of encapsulation efficiency and loading rate as the evaluation index,and the morphology,size and drug release in vitro were investigated.Results:The optimal preparation conditions were as follows:the concentration of CMCS was 0.8 g·ml^-1,BRE∶CMCS was 1∶5(g∶g),CMCS∶TPP was 15∶1(g∶g),and the speed of pump was 20 ml·min^-1.The morphology of BRE microspheres was spherical with smooth surface,the size was uniform,and the drug release in vitro was sustained.The encapsulation efficiency and the loading rate of BRE microspheres was(68.33±0.35)%and(16.26±0.42)%,respectively.Conclusion:The preparation of BRE microspheres is simple,and the in vitro quality is promising,which are valuable to be studied further.