槲皮素纳米结构脂质载体的制备及理化性质研究

Study on preparation of quercetin nanostructured lipid carriers and their physicochemical properties

目的:制备槲皮素纳米结构脂质载体(quercetin nanostuctured lipid carriers,QT-NLC),并对其理化性质进行考察。方法:采用乳化-超声分散法制备QT-NLC,正交试验筛选最优处方。透射电镜观察QT-NLC形态,Zeta电位及粒度分析仪测定Zeta电位、粒径及分布,差示扫描量热法(DSC)进行物相分析,离心超滤法测定包封率,透析法测制剂体外释放行为。结果:按优化条件制备的QT-NLC多为类球形粒子,平均粒径(175±25)nm,粒度分布较均匀,Zeta电位(-23±0.3)mV,DSC结果表明药物以非结晶状分散于纳米粒中,包封率(95.43±0.23)%,载药量(2.38±0.24)%,体外2 h累积释放32.2%,后期具有明显的缓释特征。结论:乳化-超声分散法适用于QT-NLC的制备,纳米粒子在胶体溶液中分散均匀,稳定性良好。此制备工艺安全、可靠、重现性好。

Objective： To prepare quercetin nanostuctured lipid carriers （QT-NLC）, and detect their physicochemical proper- ties. Method： QT-NLC was prepared by emulsification ultrasonic dispersion method, and the optimum prescription was screened out by orthogonal design. Transmission electron microscope was used to observe QT-NLC morphology. Granulometer was applied to deter- mine zeta potential, particle size and distribution. DSC was adopted for phase analysis. Centrifugal ultra-filtration method was used to determine entrapment efficiency. Dialysis method was adopted to detect drug release in vitro of preparations. Result： QT-NLC prepared under optimum conditions was mostly spherical grains, with the average particle size of （ 175± 25） nm, which were distributed evenly, and zeta potential was（ -23 ± 0. 3 ） mV. DSC results indicated that the drug was dispersed in nano-particles in a non-crystalline state, with an entrapment efficiency of （95.43±0. 23） % and a drag-loading capacity of （2. 38±0. 24） %. The in vitro drug release was 32. 2% in 2 hours, which was followed by a sustained release. Conclusion： Emulsification ultrasonic dispersion method is applicable for preparing QT-NLC, as nano-particles are distributed evenly, with good reliability. This processing technology is safe, reliable and highly reproducible.