Aliautdin R N, Petrov V E, Ivanov A A, Kreuter J, Kharkevich D A
Eksp Klin Farmakol. 1996 May-Jun;59(3):57-60.
The drug targeting to the brain by polysorbate 80-coated nanoparticles was studied. The leu-enkephalin analog dalargin was used as a model drug for investigating the drug penetration through the blood-brain barrier. The nociceptive threshold was measured by the tail flick test. The intravenous injection of dalargin bound by sorption to poly(butylcyanoacrylate) nanoparticles subsequently coated with polysorbate 80 induced the analgesic effect in 5.0 and 7.5 mg/kg doses. The pretreatment with naloxone prevented this effect No other controls exhibited the analgesic activity, including the dalargin solution (10 mg/kg, i.v.), dalargin bound to nanoparticles not coated with polysorbate 80; and a simple mixture of dalargin, nanoparticles, and polysorbate 80 mixed directly before the intravenous injection. The luminescent and electron microscopy demonstrated the presence of separate nanoparticles in the capillary endothelium and cerebral neurons, as well as luminescent-labeled polymer in Purkinje's cells of the cerebellum.
研究了聚山梨酯80包被的纳米颗粒对脑的药物靶向作用。亮脑啡肽类似物达乐argin被用作模型药物，以研究药物透过血脑屏障的情况。通过甩尾试验测量痛觉阈值。静脉注射吸附结合于随后用聚山梨酯80包被的聚（氰基丙烯酸丁酯）纳米颗粒上的达乐argin，在5.0和7.5mg/kg剂量下可诱导镇痛作用。用纳洛酮预处理可防止这种作用。没有其他对照显示出镇痛活性，包括达乐argin溶液（10mg/kg，静脉注射）、结合于未用聚山梨酯80包被的纳米颗粒上的达乐argin，以及在静脉注射前直接混合的达乐argin、纳米颗粒和聚山梨酯80的简单混合物。发光和电子显微镜检查表明，在毛细血管内皮细胞和脑神经元中存在单独的纳米颗粒，以及在小脑浦肯野细胞中存在发光标记的聚合物。
