吡喹酮-硬脂酸固体脂质纳米粒的制备及性能评价

Preparation and performance evaluation of praziquantel-octadecanoic acid solid lipid nanoparticles

目的:制备吡喹酮-固体脂质纳米粒,考察其理化性质和体外释放度。方法:以硬脂酸为脂质材料,聚乙烯吡咯烷酮为乳化剂,利用热熔乳化超声法制备吡喹酮-固体脂质纳米粒,扫描电镜观察纳米粒形态和均匀度,纳米粒度仪测定其粒径、分散指数、Zeta电位、包封率和载药量,并进行体外释放试验。结果:制备的固体脂质纳米粒为类圆球状,粒径分布较均匀、表面光滑。纳米的平均粒径、分散指数、电位、包封率和载药量分别为(316.5±22.8)nm、0.23±0.05、(-25.3±0.7)mV,(92.64±5.12)%和(18.45±1.34)%。药物在制剂的过程中稳定性良好。体外释放表明吡喹酮-硬脂酸固体脂质纳米粒在生理盐水中具有一定程度的突释和显著的缓释效果。结论:本试验制备的吡喹酮-硬脂酸固体脂质纳米粒具有较好的均匀度和高载药量,并具有良好的缓释性能。

OBJECTIVE To prepare praziquantel-loaded octadecanoic acid-solid lipid nanoparticles（PZQ-SLN）.METHODS PZQ-SLN was prepared by a hot homogenization and ultrasonication method using octadecanoic acid,polyvinyl pyrrolidoneas matrix and surfactant.Selection of lipid and emulsifier,and optimization of preparation parameter were studied.Morphology was examined by transmission electron microscope.Particle size,entrapment efficiency and zeta potential were determined,and drug release profiles of PZQ SLN were investigated.Stability of PZQ during preparation was also studied.RESULTS Morphological investigation showed that nanoparticles had round and uniform shapes.Encapsulation efficiency,loading capacity,diameter,polydispersity index and zeta potential of praziquantel-SLN were（92.64±5.12）%,（18.45±1.34）%,（316.5±22.8）nm,0.23±0.05 and（-25.3±0.7）mV,respectively.In vitro release studies demonstrated that SLN exhibited an initial burst release followed by a sustained release.The drug was stable during preparation.CONCLUSION Lipophilic praziquantel-loaded SLN is successfully developed and the results indicate that SLN may be a promising delivery system to enhance therapeutic effects and prolong systemic circulation of praziquantel.