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引用本文:陆瑾,展冠军,郭立玮.PEG-PLA-α-细辛脑纳米粒的表征及其鼻纤毛毒性研究[J].中国现代应用药学,2019,36(18):2280-2284.
LU Jin,ZHAN Guanjun,GUO Liwei.Characterization of PEG-PLA-α-asarone nanoparticles and Its Nasal Cilia Toxicity[J].Chin J Mod Appl Pharm(中国现代应用药学),2019,36(18):2280-2284.
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PEG-PLA-α-细辛脑纳米粒的表征及其鼻纤毛毒性研究
陆瑾1,2, 展冠军2, 郭立玮3
1.南京市大厂医院, 南京 210048;2.东南大学附属中大医院, 南京 210009;3.南京中医药大学, 南京 210023
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。
关键词:  PEG-PLA-α-细辛脑纳米粒  鼻腔给药  表征  鼻纤毛毒性
DOI:10.13748/j.cnki.issn1007-7693.2019.18.009
分类号:R944.4
基金项目:
Characterization of PEG-PLA-α-asarone nanoparticles and Its Nasal Cilia Toxicity
LU Jin1,2, ZHAN Guanjun2, GUO Liwei3
1.Nanjing Dachang Hospital, Nanjing 210048, China;2.Zhongda Hospital, Southeast University, Nanjing 210009, China;3.Nanjing University of Chinese Medicine, Nanjing 210023, China
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.
Key words:  PEG-PLA-α-asarone nanoparticles  intranasal  characterization  nasal cilia toxicity
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