离子诱导结合化学交联法制备黄芩苷壳聚糖纳米粒

The Preparation of Baicalin-Chitosan-Nanoparticles by Ion-Induced Combining Chemical Crosslinking

采用离子诱导结合化学交联法,制备以黄芩苷为模型药物、壳聚糖为载体的黄芩苷壳聚糖纳米粒.通过单因素实验考察壳聚糖溶液pH、黄芩苷加入量、搅拌速度、壳聚糖与三聚磷酸钠质量比、牛血清白蛋白加入量和香草醛加入量对黄芩苷壳聚糖纳米粒包封率的影响,筛选出影响显著的因素.采用L16(45)正交实验设计法进一步优化黄芩苷壳聚糖纳米粒的工艺条件,并对该条件下制备的黄芩苷壳聚糖纳米粒进行表征.确定黄芩苷壳聚糖纳米粒的最佳工艺条件为:壳聚糖溶液pH为4,黄芩苷加入量10 mL,壳聚糖与三聚磷酸钠质量比5∶1,牛血清白蛋白加入量1 mg,香草醛加入量3 mg.该条件下,黄芩苷壳聚糖纳米粒包封率为(82.70±2.31)%,平均粒径为(287.7±3.1) nm,多分散系数为0.283±0.025,Zeta电位值为(+33.6±0.6) mV.在体外释放试验中,黄芩苷溶液在5 h时的药物累积释放量为95.40%,黄芩苷壳聚糖纳米粒在48 h时的药物累积释放量为82.72%.与黄芩苷溶液相比,黄芩苷壳聚糖纳米粒具有明显的缓释作用.

The preparation of baicalin-chitosan-nanoparticles was studied,and the nanoparticles were prepared by ion-induction chemical crosslinking with chitosan as carrier and baicalin as model drug.Based on results from single factor tests,orthogonal experimental design method was used to investigate the factors influence on envelopment rate of nanoparticles.In this experiment,the optimum conditions for the preparation of baicalin-chitosan-nanoparticles were:pH of chitosan solution 4,baicalin dosage 10 mL,the ratio of chitosan to Sodium tripolyphosphate 5∶1,Bovine albumin dosage 1 mg,and the amount of Vanillin 3 mg.The mean diameter was(287.7±3.1) nm,PDI was 0.283±0.025,and encapsulation rate(82.70±2.31)%.The method could be used to prepare baicalin-chitosan-nanoparticles. Comparing with the baicalin solution,Baicalin-chitosan-nanoparticles showed obvious sustained release effect in physiological saline.