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

关键词:  PEG-PLA-α-细辛脑纳米粒  鼻腔给药  表征  鼻纤毛毒性

Key words:  PEG-PLA-α-asarone nanoparticles  intranasal  characterization  nasal cilia toxicity

摘要:

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。

Abstract:

OBJECTIVE To prepare α-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. METHODS α-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 that α-asarone was mainly in the form of molecular dispersion exist in PEG-PLA-α-asarone nanoparticles. In vitro release behavior of α-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.