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目的考察3种吸收促进剂对于多肽类大分子物质神经毒素(NT-Ⅰ)鼻腔给药后脑内递药的作用。方法运用125I-NT-Ⅰ同位素标记法,以清醒大鼠为实验模型,采用同步多处脑微透析技术,连续测定单用NT-Ⅰ(105μg·kg-1)以及NT-Ⅰ合用冰片、薄荷和冰片/薄荷低共熔物大鼠鼻腔给药后分别在嗅球和小脑组织间液中NT-Ⅰ的浓度。结果单用NT-Ⅰ鼻腔给药进入脑内非常有限。冰片/薄荷低共熔物组小脑和嗅球中AUC分别是(2283.51±34.54)和(1358.58±32.56)ng.min.mL-1,均低于单用冰片或薄荷组中在同一脑区的AUC。而两个脑区中低共熔组的达峰时间均较单独使用冰片和薄荷脑组的达峰时间短(P<0.05)。结论冰片、薄荷和冰片/薄荷低共熔物均有促进NT-Ⅰ通过鼻黏膜吸收入脑的作用。冰片/薄荷脑低共熔物吸收促进作用较单独冰片和薄荷脑弱。但是,冰片/薄荷脑低共熔物可促进NT-Ⅰ鼻腔给药后快速入脑。
Objective To investigate the effects of three kinds of absorption enhancers on intracerebral delivery of polypeptide-like macromolecule neurotoxin (NT-Ⅰ) after intranasal administration. Methods 125I-NT-Ⅰ isotope labeling method and conscious rat model were used to detect NT-Ⅰ (NT-Ⅰ, NT-Ⅰ) and borneol NT-I in the fluid between the olfactory bulb and cerebellar tissue after intranasal administration of borneol / menthol eutectic rats. Results Nasal administration of NT-I alone was very limited. The AUC in the cerebellum and olfactory bulb of the borneol / menthol eutectic group were (2283.51 ± 34.54) and (1358.58 ± 32.56) ng.min.mL-1, respectively, which were lower than those in the same brain region . The peak elution time of eutectic group in both brain regions was shorter than that of borneol and menthol alone (P <0.05). Conclusion Both borneol, mint and borneol / mint eutectic can promote NT-Ⅰ absorption into the brain through nasal mucosa. Borneol / menthol eutectic absorption promoting role than the individual borneol and menthol weaker. However, borneol / menthol eutectic can promote NT-快 nasal delivery to the brain quickly.