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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 study its physico-chemical properties. Methods: QT-NLC was prepared by emulsification-ultrasonic dispersion method. The optimal prescription was screened by orthogonal test. The morphology of QT-NLC was observed by transmission electron microscopy. Zeta potential, particle size and distribution were measured by Zeta potential and particle size analyzer. Phase analysis was performed by differential scanning calorimetry (DSC). The entrapment efficiency was measured by centrifugal ultrafiltration. In vitro release behavior. Results: Most of the QT-NLC prepared under optimal conditions were spherical particles with an average particle size of (175 ± 25) nm, a uniform particle size distribution and a zeta potential of (-23 ± 0.3) mV. DSC results showed that the drug was dispersed in a non- The entrapment efficiency (95.43 ± 0.23)% and drug loading (2.38 ± 0.24)% in nanoparticles were 32.2% in vitro in 2 h, and the latter showed obvious sustained release characteristics. Conclusion: Emulsification - ultrasonic dispersion method is suitable for the preparation of QT-NLC. Nanoparticles are well dispersed in colloidal solution with good stability. The preparation process is safe, reliable and reproducible.