三七皂苷长循环纳米粒制备及其体外溶出行为

Study on the preparation and dissolution of Panax notoginseng saponins long-circulating nanoparticles

目的:星点设计-效应面法优化复乳化法制备三七皂苷长循环纳米粒(PNS-LCN)并对其进行体外溶出行为研究。方法:以三七皂苷(PNS)浓度、油相中乳化剂浓度以及壳聚糖的浓度为考察因素,包封率、载药量、平均粒径及分散性为考察指标,根据星点设计原理进行实验安排,并用二项式拟合建立指标与因素之间的数学关系,经效应面法预测最佳工艺条件;采用动态透析法考察了PNS与PNS-LCN的体外溶出行为。结果:各指标的二项式拟合方程较好,以优化条件制备的样品包封率为(52.8±0.7)%、载药量为(13.1±0.6)%、平均粒径为(152.6±4.5)nm、分散性为(0.24±0.04);PNS-LCN中药物的释放显著慢于原料药磷酸盐缓冲溶液的释放。结论:星点设计-效应面法适用于PNS-LCN的工艺优化,所建立的数学模型预测性良好;PNS-LCN体外释药具有缓释效果。

OBJECTIVE To study the preparation of Panax notoginseng saponins long-circulating nanoparticles（PNS-LCN） by central composite design-response surface methods and its in vitro dissolution.METHODS The influencing factors included the concentration of PNS,the concentration of emulsifier in organic phase and the concentration of chitosan.The evaluation parameters included entrapment efficiency,drug loading,mean diameter and polydispersity index.Experiments were based on the theory of central composite design.The data were simulated using multi-linear equation and second-order polynomial equation.The possibly optimal formulation was predicted by response surface method;dynamic dialysis system was adopted to study the release dynamics of PNS-LCN and PNS in vitro.RESULTS The results showed that the latter was prior to the former.According to the optimal conditions,the entrapment efficiency,drug loading,the mean diameter and polydispersity index were（52.8±0.7）%,（13.1±0.6）%,（152.6±4.5）nm,（0.24±0.04）,respectively.PNS-LCN release of thedrug was significantly slower than the API release of phosphate buffer solution.CONCLUSION The central composite design and response surface method are useful for the optimization of preparing PNS nanoparticles.The estimation of the established model is good;PNS-LCN has a sustained-release effect in vitro.