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目的:考察中药冰片-薄荷脑低共熔物对神经毒素纳米粒鼻腔给药吸收入脑的影响。方法:采用125I同位素标记法,以清醒自由活动大鼠为实验模型,运用脑微透析取样技术,测定脑内神经毒素浓度的变化,并应用药动学软件计算药动学参数。结果:添加冰片-薄荷脑低共熔物的神经毒素纳米粒脑药动学符合二室模型,tmax,Cmax,AUC,t1/2(β)分别为0.68 h、27.32μg.L-1,132.68μg.h.L-1,3.107 6 h,其入脑的速度与程度均优于单用薄荷脑或者冰片。结论:神经毒素纳米粒在冰片-薄荷脑低共熔物作用下,可显著增加其鼻腔吸收入脑的药量,且能较快达到峰浓度,消除缓慢。
OBJECTIVE: To investigate the effect of borneol-menthol eutectic absorbed into the brain by nasal administration of neurotoxin nanoparticles. Methods: 125I isotope labeling method was used to study the change of neurotoxin concentration in the brain of conscious and free-moving rats using brain microdialysis sampling. The pharmacokinetic parameters were calculated by pharmacokinetic software. Results: Neurotoxin NPs with addition of borneol-menthol eutectic were consistent with two-compartment model. The tmax, Cmax, AUC and t1 / 2 (β) were 0.68 h, 27.32 μg.L-1 and 132.68 μg, respectively. hL-1,3.107 6 h, its brain speed and degree are better than single menthol or borneol. CONCLUSION: Neurotoxin nanoparticles can significantly increase the amount of nasal absorption into the brain under the action of borneol-menthol eutectic, and can reach the peak concentration faster and eliminate slowly.