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目的:表征聚乳酸-α-细辛脑(PLA-α-细辛脑)纳米粒,评价其鼻腔给药后鼻黏膜毒性,为其通过鼻腔给药方式用于体内的研究提供基础。方法:采用有机溶剂挥发法将α-细辛脑制备成PLA-α-细辛脑纳米粒,通过粒径分布、载药量和包封率评价纳米粒的工艺条件;红外光谱,差示扫描量热分析,X射线衍射分析及体外溶出试验分析药物在纳米粒中的分布状态;鼻纤毛毒性及鼻黏膜病理切片研究PLA-α-细辛脑纳米粒混悬液鼻腔给药后的鼻黏膜毒性。结果:α-细辛脑纳米粒平均粒径265.4 nm,多分散系数(PDI)0.038,载药量12.40%,包封率55.86%,α-细辛脑以分子状态分散或非晶型状态存在于PLA载体中,体外释放包括速释和缓释,呈双相动态,PLA-α-细辛脑纳米粒混悬液鼻腔给药后对鼻黏膜组织无明显的毒性作用。结论:有机溶剂挥发法制备的PLA-α-细辛脑纳米粒表征与鼻黏膜毒性试验结果表明该制剂适合于鼻腔给药。
OBJECTIVE: To characterize polylactic acid-α-asarone (PLA-α-asaroneine) nanoparticles for evaluating nasal mucosal toxicity after nasal administration, and to provide a basis for its application in vivo by nasal administration. Methods: Alpha-asarone was prepared into PLA-α-Asarone nanoparticles by organic solvent evaporation method. The technological conditions of nanoparticles were evaluated by particle size distribution, drug loading and entrapment efficiency. Infrared spectra, differential scanning Calorimetry, X-ray diffraction analysis and in vitro dissolution test to analyze the drug distribution in the nanoparticles; nasal cilia toxicity and nasal mucosa pathological sections of nasal mucosa after nasal administration of PLA-α- asarone nanoparticles suspension toxicity. Results: The average particle size of α-asarone brain nanoparticles was 265.4 nm, the PDI was 0.038, the drug loading was 12.40% and the encapsulation efficiency was 55.86%. The α-asarone was dispersed in molecular state or amorphous state In PLA carrier, the release in vitro including immediate release and sustained release, showed biphasic dynamic, nasal administration of PLA-α-Asarone nanoparticle suspension had no obvious toxic effect on nasal mucosa. CONCLUSIONS: Characterization of PLA-α-asarone nanoparticles prepared by organic solvent evaporation and nasal mucosal toxicity test results show that the preparation is suitable for nasal administration.