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目的制备聚山梨酯80包裹的神经毒素-Ⅰ(NT-Ⅰ)聚氰基丙烯酸正丁酯(PBCA)纳米粒(T-80-NT-Ⅰ-PBCA-NP),并考察其脑内药动学特征。方法以PBCA为纳米材料,采用乳化聚合法制备T-80-NT-Ⅰ-PBCA-NP,以大鼠为实验对象,经鼻腔给药后,运用脑微透析取样技术,以未包裹的NT-ⅠPBCA纳米粒(NT-Ⅰ-PBCANP)为对照组,研究神经毒素-Ⅰ在脑内中脑导水管周围灰质(PAG)的动力学过程。结果大鼠鼻腔给药后,聚山梨酯-80包裹与未包裹的NT-ⅠPBCA纳米粒药物浓度-时间曲线符合开放性二室模型,其主要药动学参数t_(max)分别为(71.018±7.641)、(55.830±6.072) min;C_(max)分别为(117.189±10.036)、(52.277±6.217) ng/mL;AUC_(0→∞)分别为(22 836.633±51.052)、(12 786.934±30.723) ng·min·mL~(-1)。结论T-80-NT-Ⅰ-PBCA-NP鼻腔给药后延长NT-Ⅰ达峰时间,且显著提高NT-Ⅰ的脑内浓度。
Objective To prepare polysorbate 80 (NT-Ⅰ) polybutylcyanoacrylate nanoparticles (T-80-NT-Ⅰ-PBCA-NP) Learn characteristics. Methods T-80-NT-Ⅰ-PBCA-NP was prepared by emulsion polymerization using PBCA as the nanomaterial. The rats were used as experimental materials. After intranasal administration, the brain microdialysis sampling technique was used. ⅠPBCA nanoparticles (NT-Ⅰ-PBCANP) as a control group, to study the neurotoxin-Ⅰ in the brain midbrain periaqueductal gray (PAG) kinetics. Results After intranasal administration, the drug concentration-time curves of polysorbate-80 coated and uncoated NT-Ⅰ PBCA nanoparticles conformed to the open two-compartment model. The main pharmacokinetic parameters t max were (71.018 ± 7.641) and (55.830 ± 6.072) min, respectively; C max were (117.189 ± 10.036) and (52.277 ± 6.217) ng / mL, respectively; AUC 0 to ∞ were 22 836.633 ± 51.052 and 12 786.934 ± 30.723) ng · min · mL -1. Conclusions The nasal administration of T-80-NT-Ⅰ-PBCA-NP prolongs the peak time of NT-Ⅰ and significantly increases the intracerebral concentration of NT-Ⅰ.