College of Pharmaceutical Sciences, Zhejiang Chinese Medical University, Hangzhou, P.R China.
Drug Dev Ind Pharm. 2012 Jan;38(1):123-8. doi: 10.3109/03639045.2011.592533. Epub 2011 Jul 1.
Neurotoxin-II (NT-II), an analgesic peptide which was separated from the venom of Naja naja atra, is endowed an exceptional specificity of action that block transmission of the nerve impulse by binding to the acetylcholine receptor in the membrane. However, it has limited permeability across the blood-brain barrier (BBB) after intravenously (i.v.) injection.
In this study, we explored the potential application of nanoparticles overcoated with polysorbate 80 (P-80-NP) as drug carrier system for the nasal delivery of NT and the antinociceptive properties of NT-loaded P-80-NP (NT-P-NP) were also evaluated.
The brain delivery of NT-II could be enhanced with nanoparticles coated with polysorbate-80 through intranasally (i.n.) administration. Compared with NT-II solution, NT-P-NP exhibited sustained release in vitro and higher concentrations of NT-II in the brain. The antinociceptive animal testing also revealed that intranasal delivery of NT-loaded nanoparticle coated with polysorbate-80 were able to promote better biodistribution of the drug into the brain.
The nanoparticles overcoated with polysorbate-80 were capable of transporting the loaded drug across the BBB after intranasal administration.
神经毒素-II（NT-II）是从中华眼镜蛇毒液中分离出来的一种镇痛肽，具有独特的作用特异性，通过与膜上的乙酰胆碱受体结合来阻断神经冲动的传递。然而，它在静脉注射（i.v.）后穿过血脑屏障（BBB）的通透性有限。
在这项研究中，我们探索了用聚山梨酯 80（P-80）包被的纳米粒作为药物载体系统经鼻给药的可能性，并且评估了载 NT 的 P-80 纳米粒（NT-P-NP）的镇痛作用。
通过鼻内（i.n.）给予用聚山梨酯-80 包被的纳米粒，可增强 NT-II 的脑内传递。与 NT-II 溶液相比，NT-P-NP 在体外具有持续释放的特性，并且脑内的 NT-II 浓度更高。动物镇痛试验还表明，用聚山梨酯-80 包被的载 NT 纳米粒的鼻内给药能够促进药物更好地分布到大脑中。
用聚山梨酯-80 包被的纳米粒能够在鼻内给药后将负载药物转运穿过 BBB。
