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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-solid lipid nanoparticles and investigate their physico-chemical properties and in vitro release. Methods: Praziquantel - solid lipid nanoparticles were prepared by hot melt emulsification ultrasound with stearic acid as the lipid material and polyvinylpyrrolidone as the emulsifier. The morphology and uniformity of the nanoparticles were observed by scanning electron microscopy. The nanoparticle size Particle size, dispersion index, Zeta potential, encapsulation efficiency and drug loading, and in vitro release test. Results: The prepared solid lipid nanoparticles were spheroidal, the particle size distribution was more uniform and the surface was smooth. The average particle size, dispersion index, potential, entrapment efficiency and drug loading of the nanoparticles were (316.5 ± 22.8) nm, 0.23 ± 0.05, (-25.3 ± 0.7) mV, (92.64 ± 5.12)% and (18.45 ± 1.34 )%. The stability of the drug during formulation is good. In vitro release showed that praziquantel-stearic acid solid lipid nanoparticles have a certain degree of burst release and significant sustained release in physiological saline. Conclusion: The praziquantel-stearic acid solid lipid nanoparticles prepared in this study have good uniformity and high drug loading, and have good sustained-release properties.