盐酸米诺环素羧甲基壳聚糖微球的制备研究

Study on preparation of minocycline hydrochloride-loaded carboxymethyl chitosan microspheres

目的研究制备盐酸米诺环素羧甲基壳聚糖微球的方法。方法采用乳化-交联固化法制备盐酸米诺环素羧甲基壳聚糖微球,首先通过Plackett-Burman实验设计筛选出影响微球制剂性质的关键变量,然后采用Box-Behnken实验设计进行进一步优化。使用扫描电镜观察制备的微球的微观结构,粒度分析仪测定微球粒径分布。结果制备盐酸米诺环素羧甲基壳聚糖微球的优化配方为:羧甲基壳聚糖用量为3.0%,交联剂用量为1.4%,表面活性剂用量为0.6%。制备的微球呈规则球形,无粘连,收率为(61.7±0.6)%,粒径为(14.2±0.7)μm,包封率(7.5±0.3)%。结论根据本研究优化配方制备的盐酸米诺环素羧甲基壳聚糖微球的收率较高,粒径较为均匀,药物包封率较大,制备工艺简易,重现性良好。

Objective To study the preparation method of minocycline hydrochloride-loaded carboxymethyl chitosan(Min-loaded CMC)microspheres.Methods The Min-loaded CMC microspheres were prepared by emulsification and cross-linking method.Firstly,Plackett-Burman experimental design was used to screen the critical variables affecting the properties of microsphere preparation.Then,further optimization was conducted by Box-Behnken experimental design.The microstructure of prepared microspheres was observed with a scanning electron microscopy(SEM).The particle size distribution was determined with a granulometer.Results The optimized formulation of preparing Min-loaded CMC microspheres was composed of 3.0%carboxymethyl chitosan,1.4%cross-linker,and 0.6%surfactant.The prepared microspheres were regular in shape and free of adhesion,with the yield of(61.7±0.6)%,the particle size of(14.2±0.7)μm,and the encapsulation efficiency of(7.5±0.3)%.Conclusion The Min-loaded CMC microspheres prepared according to the optimized formula of this study have higher yield,relatively uniform particle size,higher drug encapsulation efficiency,as well as simple preparation process and good reproducibility.