PEG-PLA-α-细辛脑纳米粒的表征及其鼻纤毛毒性研究

Characterization of PEG-PLA-α-asarone Nanoparticles and Its Nasal Cilia Toxicity

目的将α-细辛脑制备成聚乙二醇-聚乳酸-α-细辛脑纳米粒(PEG-PLA-α-细辛脑纳米粒),考察其表面性能及鼻腔给药后的鼻纤毛毒性。方法采用有机溶剂挥发法将α-细辛脑制备成PEG-PLA-α-细辛脑纳米粒。纳米粒度定位仪、透射电镜、差示扫描量热仪及X射线衍射法对PEG-PLA-α-细辛脑纳米粒进行表征;透析法研究PEG-PLA-α-细辛脑体外释放行为;大鼠模型考察PEG-PLA-α-细辛脑纳米粒鼻腔给药后的鼻纤毛毒性。结果PEG-PLA-α-细辛脑纳米粒平均粒径为172.3 nm,PDI指数0.256,载药量10.70%,包封率59.36%;α-细辛脑主要以分子分散的形式存在于PEG-PLA-α-细辛脑纳米粒中;PEG-PLA-α-细辛脑纳米粒中α-细辛脑的体外释放行为符合Ritger-peppas拟合方程;PEG-PLA-α-细辛脑纳米粒鼻腔给药后对鼻纤毛无明显的毒性。结论有机溶剂挥发法制备的PEG-PLA-α-细辛脑纳米粒可用于鼻腔给药。

OBJECTIVE To prepareα-asarone into polyethylene glycol-polylactic acid-α-asarone nanoparticles(PEG-PLA-α-asarone nanoparticles),and investigate the surface properties of PEG-PLA-α-asarone nanoparticles and the nasal cilia toxicity after nasal administration.METHODSα-Asarone was prepared into PEG-PLA-α-asarone nanoparticles by organic solvent evaporation method.PEG-PLA-α-asarone nanoparticles were characterized by nano-particle size locator,transmission electron microscope,differential scanning calorimeter and X-ray diffraction method.In vitro release behavior of PEG-PLA-α-asarone nanoparticles was studied by dialysis method.The rat model was used to investigate the nasal cilia toxicity of PEG-PLA-α-asarone nanoparticles after nasal administration.RESULTS The average particle size of PEG-PLA-α-asarone nanoparticles was 172.3 nm,the PDI index was 0.256,the drug loading was 10.70%,and the entrapment efficiency was 59.36%.The characterization results showed thatα-asarone was mainly in the form of molecular dispersion exist in PEG-PLA-α-asarone nanoparticles.In vitro release behavior ofα-asarone in PEG-PLA-α-asarone nanoparticles was in accordance with the Ritger-peppas fitting equation.The result of nasal cilia toxicity study showed that PEG-PLA-α-asarone nanoparticles had no apparent toxicity to nasal cilia after nasal administration.CONCLUSION PEG-PLA-α-asarone nanoparticles prepared by volatilization of organic solvents method can be used for nasal administration.