葛根素聚合物胶束的制备及包封率的测定
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篇名: 葛根素聚合物胶束的制备及包封率的测定
TITLE:
摘要: 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 C18(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 mV;葛根素检测质量浓度线性范围为2~10 μg/ml(R2=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。
ABSTRACT: 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 C18(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 mV; the linear range of puerarin was 2-10 μg/ml (R2=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.
期刊: 2016年第27卷第22期
作者: 马晓星,韩翠艳,刘畅,朱丹,隋小宇,袁橙,黄海涛
AUTHORS: MA Xiaoxing,HAN Cuiyan,LIU Chang,ZHU Dan,SUI Xiaoyu,YUAN Cheng,HUANG Haitao
关键字: 葛根素聚合物胶束;薄膜分散法;高效液相色谱法;离心-微孔滤膜法;包封率
KEYWORDS: Puerarin polymeric micelles; Film dispersion method; HPLC; Centrifugal-millipore filter filtration method; Entrapment efficiency
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