扎那米韦固体脂质纳米粒的制备及其包封率测定

Preparation of zanamivir-loaded solid lipid nanoparticles and determination of encapsulation efficiency

目的建立扎那米韦反相高效液相色谱(RP-HPLC)分析方法,测定其固体脂质纳米粒的包封率。方法色谱柱为Inertsil ODS-3 C18柱(250 mm×4.6 mm,5μm),流动相为乙腈–水(10∶90),流速0.6 ml/min,检测波长235 nm,进样量20μl。采用复乳化溶剂挥发法制备扎那米韦固体脂质纳米粒,扫描透射电镜观察纳米粒形态,激光粒度分析仪考察纳米粒的粒径分布和表面电位,并测定其包封率及载药量。结果在该色谱条件下扎那米韦与辅料及溶剂峰分离良好,扎那米韦在0.5～100.0μg/ml浓度线性范围内与峰面积呈良好的线性关系(r=0.999 9,n=8),日内精密度试验的相对标准偏差(RSD)为0.59%～2.03%(n=3),日间精密度试验的RSD为1.06%～1.88%(n=3),平均回收率为100.11%(n=3)。所制得固体脂质纳米粒形态比较圆整,粒径为(183.9±5.7)nm,Zeta电位为(-53.0±1.6)mV,包封率和载药量分别为(36.1±2.8)%和(0.32±0.03)%。结论该RP-HPLC分析方法简便、易行,可用于扎那米韦固体脂质纳米粒的包封率测定。

Objective To establish a reverse HPLC） method and to determine the encapsulation phase high performance liquid chromatography （RP- efficiency of zanamivir-loaded solid lipid nanoparticles （SLNs）. Methods RP-HPLC analysis was performed on an Inertsil ODS-3 C ls （250×4.6mm,5 μm） column with mobile phase of acetonitrile-water（ 10： 90）. The flow rate was 0.6 ml/min. The wavelength of UV detector was set at 235 nm and the injection volume was 20 p,1. Zanamivir-loaded SLNs was pre- pared by a double emulsion solvent evaporation method. Transmission electron microscropy （TEM） was conducted to investigate the morphology of SLNs. The mean diameter and zeta potential of SLNs were measured by photon correlation spectroscopy. The entrapment efficiency and drug loading amount of SLNs were detected by RP-HPLC. Results It had a good linear relation in the range of 0.5×100.0μ/ml （ r = 0.999 9 ）. The intra-day precision （RSD） was 0.59% - 2.03% （ n = 3 ）. The inter-day precision （RSD） was 1.06% -1.88% （n =3）. The average recovery rate was 100.11% （n =3）. The SLNs were sphere like with the average size of （ 183.9±5.7 ） nm and zeta potential of （ - 53.0±1.6 ） mV. The encapsulation efficiency and drug loading amount of SLNs were （36.1±2.8 ） % and （0.32±0.03 ） %, respectively. Conclusion The developed RP-HPLC method is simple, accurate and reliable for de- termination of entrapment efficiency of zanamivir-loaded SLNs.