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目的制备奥卡西平纳米脂质载体(oxcarbazepine nanostructured lipid carriers,OXC-NLC),并对其理化性质进行考察。方法采用乳化溶剂蒸发法制备OXC-NLC,正交试验筛选最优处方,使用扫描电镜、激光粒径测定仪、差示扫描量热仪等考察OXC-NLC的理化性质,通过溶出试验评价其体外释放效果。结果按优化条件制备的OXC-NLC为类球形粒子,平均粒径为(63.04±2.05)nm,粒度分布较均匀,Zeta电位为(-33.52±0.34)mV,DSC结果表明,药物以无定形状态分散于纳米粒中,包封率为(98.16±1.59)%,载药量为(4.27±0.70)%,体外8 h累积释放27.31%。结论采用乳化溶剂蒸发法制备的OXC-NLC粒径大小分布均匀,药物包封率高,具有明显的缓释效果。此制备工艺流程简单、可靠、重现性好。
OBJECTIVE To prepare oxcarbazepine nanostructured lipid carriers (OXC-NLC) and investigate its physico-chemical properties. Methods OXC-NLC was prepared by emulsion solvent evaporation method. The optimal prescription was screened by orthogonal test. The physicochemical properties of OXC-NLC were investigated by scanning electron microscopy, laser particle size analyzer and differential scanning calorimeter. Release effect. Results OXC-NLC prepared under optimal conditions was a spherical-like particle with an average particle size of (63.04 ± 2.05) nm with a uniform particle size distribution and a zeta potential of (-33.52 ± 0.34) mV. DSC results showed that the drug was in an amorphous state The encapsulation efficiency was (98.16 ± 1.59)% and the drug loading was (4.27 ± 0.70)%. The cumulative release in vitro was 27.31% in 8 h. Conclusion The particle size of OXC-NLC prepared by emulsification solvent evaporation is uniform and the drug encapsulation efficiency is high. It has obvious sustained release effect. The preparation process is simple, reliable and reproducible.