冬凌草甲素聚乳酸纳米粒的制备和体外性质研究

 目的优化冬凌草甲素聚乳酸纳米粒的制备工艺,并对其理化性质和体外释药特性进行考察。方法以改良的自乳化溶剂扩散法制备冬凌草甲素聚乳酸纳米粒,采用均匀设计法优化处方工艺,对优化工艺所得产品通过透射电镜、激光粒度分布与Zeta电位分析仪、pH计、黏度计、差示扫描量热法和X-射线衍射法分析理化性质,并用超速离心法对其体外释药特性进行研究。结果分析结果证明,纳米粒确已形成,并测得所制备纳米粒的包封率为(91.88±1.83)%,载药量为(2.32±0.05)%,粒径为(125.3±11.2)nm,粒径跨距为(0.82±0.03),Zeta电位为(-15.88±0.41)mV,pH值为(5.57±0.04),黏度为(1.231±0.002)×10^-3 Ns.m^-2。体外释药符合Higuchi方程:Q=8.944t^1/2+11.246。结论实验建立的制备工艺可行,所得纳米粒的包封率高,理化性质稳定,体外释药具有缓释制剂特征。

Preparation and in Vitro Properties of Oridonin-Loaded Polylactic-acid Nanoparticles

OBJECTIVE To optimize the preparation method of the oridonin-loaded polylactic-acid nanoparticles,and investigate its properties and release behavior in vitro.METHODS The oridonin-loaded polylactic-acid nanoparticles were prepared by modified spontaneous emulsification solvent diffusion method.The uniformity design was used to optimize the preparation procedure.The transmission electron microscope,Zetasizer instrument,digital pH meter,rotational viscometer,differential scanning calorimetry and X-ray diffractometry were utilized to investigate the properties of the nanoparticles.The release behavior of the nanoparticles in vitro was studied using the ultracentrifugation technique.RESULTS The results showed that the nanoparticles were formed with the entrapment efficiency of(91.88±1.83)%,drug loading of(2.32±0.05)%,particle size of(125.3±11.2) nm,diameter span of(0.82±0.03),Zeta potential of(-15.88±0.41) mV,pH value of(5.57±0.04),viscosity of(1.231±0.002)×10^-3 Ns·m^-2,respectively.The in vitro release profile of the nanopartilces were expressed well by Higuchi equation:Q=8.944t^1/2+11.246.CONCLUSION The method is practicable with high entrapment efficiency and stable properties.The main release properties confirms to that of the sustained release preparations.