葛根素聚合物胶束的制备及包封率的测定

Preparation and Determination of Entrapment Efficiency of Puerarin Polymeric Micelles

目的:制备葛根素聚合物胶束并建立其包封率测定方法。方法:采用薄膜分散法制备葛根素聚合物胶束;以离心-微孔滤膜法分离胶束和游离药物,采用高效液相色谱法测定聚合物胶束包封率,色谱柱为Diamonsil C_(18)(2),流动相为1%柠檬酸溶液-甲醇(65∶35),流速为1 ml/min,检测波长为250 nm,柱温为室温。结果:制备的聚合物胶束形态为规则的球形或类球形,平均粒径为54.12 nm,多分散系数为0.122,Zeta电位为-13.60 m V;葛根素检测质量浓度线性范围为2~10μg/ml(R^2=0.999 4),方法回收率平均值为99.2%(RSD=0.9%,n=3),游离药物回收率为95.3%(RSD=1.7%,n=3);葛根素胶束平均包封率为(35.5±2.12)%、载药量为(0.3±0.07)%(n=3)。结论:薄膜分散法适用于制备葛根素聚合物胶束;所建立的葛根素含量及其包封率测定方法操作简单、准确、可靠。

OBJECTIVE：To prepare Puerarin polymeric micelles and establish a method to determine its entrapment efficiency.METHODS：Puerarin polymeric micelles were prepared by film dispersion method. The polymeric micelles and free drug were separated by centrifugal-millipore filter filtration method. The entrapment efficiency of puerarin polymeric micelles was determined by HPLC. Diamonsil C_（18）（2）column was used with 1% citric acid solution-methanol（65 ∶ 35）at the flow rate of 1 ml/min. The detection wavelength was set at 250 nm,and column temperature was room temperature. RESULTS：The prepared polymeric micelles were spherical and spherical-like in shape with a mean particle size of 54.12 nm,polydispersity index of 0.122,Zeta potential of-13.60 m V;the linear range of puerarin was 2-10 μg/ml（R-2=0.999 4）with average recovery rate of 99.2%（RSD=0.9%,n=3）. The recovery rate of free drug was 95.3%（RSD=1.7%,n=3）. The mean entrapment efficiency and drug-loading amount of puerarin were（35.5±2.12）% and（0.3±0.07）%,respectively（n=3）. CONCLUSIONS：Film dispersion method is suitable for the preparation of Puerarin polymeric micelles. Established method is convenient,accurate and reliable for the content and entrapment efficiency determination of Puerarin polymeric micelles.