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采用乳化溶剂挥发法制备聚乳酸(PLA)-α-细辛脑纳米粒,并与静脉注射给药比较,研究PLA-α-细辛脑纳米粒鼻腔给药后药物的体内分布及脑组织的靶向性。结果显示:鼻腔给药和静脉注射后的脑靶向系数分别为1.65与1.16,PLA-α-细辛脑纳米粒鼻腔给药后的绝对生物利用度为74.2%,脑靶向效率为142.24%,鼻-脑传递百分比为29.83%。荧光标记法显示,PLA-α-细辛脑荧光纳米粒经鼻腔给药后,香豆素-6在脑组织中的荧光强度最大,达到脑靶向给药的目的;PLA-α-细辛脑荧光纳米粒静脉注射给药后,香豆素-6在肝组织中的荧光强度远高于鼻腔给药,表明PLA-α-细辛脑纳米粒经鼻腔给药可降低药物导致的肝毒性。此外,PLA-α-细辛脑荧光纳米粒经鼻腔给药后,香豆素-6在肺组织中的荧光强度较弱,解决了气流粉碎法制备的α-细辛脑干粉经鼻腔给药到达肺部量较多的缺点。体内研究表明:与静脉注射相比,PLA-α-细辛脑纳米粒鼻腔给药后的脑靶向性优于静脉注射。
The PLA-α-asarone nanoparticles were prepared by emulsion solvent evaporation method and compared with the intravenous injection, the drug distribution in vivo after PLA-α-asarone nanoparticles administration was studied, Targeted. The results showed that the brain targeting coefficients after intranasal administration and intravenous injection were 1.65 and 1.16 respectively. The absolute bioavailability of PLA-α-asarone nanoparticles after nasal administration was 74.2% and the brain targeting efficiency was 142.24% , Nasal-brain transmission percentage was 29.83%. Fluorescent labeling showed that the fluorescence intensity of coumarin-6 in brain tissue was maximal after PLA-α-asarone fluorescent nanoparticles were intranasally administered to achieve the purpose of brain-targeted drug delivery. PLA-α-Asarum The fluorescence intensity of coumarin-6 in hepatic tissue was much higher than that in the nasal cavity after intravenous injection of brain fluorescent nanoparticles, indicating that the intranasal administration of PLA-α-asarone could reduce drug-induced hepatotoxicity . In addition, the fluorescence intensity of coumarin-6 in lung tissue after intranasal administration of PLA-α-Asarone fluorescent nanoparticles was weaker, which solved the problem that the α-Asarone brain dry powder Drugs reach the lungs more disadvantages. In vivo studies have shown that, compared with intravenous injection, PLA-α-asarone nanoparticles after intranasal administration of brain targeting than intravenous injection.