Aliautdin R N, Petrov V E, Langer K, Berthold A, Kreuter J, Kharkevich D A
Department of Pharmacology, Sechenov Medical Academy, Moscow, Russia.
Eksp Klin Farmakol. 1998 Jan-Feb;61(1):17-20.
The possibility of using polysorbate 80-coated nanoparticles for the delivery of the water insoluble opioid (lyonist loperamide across the blood-brain barrier was investigated. The analgesic effect after i.v. injection of the preparations was used as the indication of drug transport through this barrier. Intravenous injection of the particulate formulation resulted in a long and significant analgesic effect. A polysorbate 80 loperamide solution induced a much less pronounced and very short analgesia. Uncoated nanoparticles loaded with loperamide were unable to produce analgesia. Polysorbate 80-coated PBCA nanoparticles loaded with loperamide led to the transport of loperamide to the brain.
研究了使用聚山梨醇酯80包被的纳米颗粒递送水不溶性阿片类药物（洛哌丁胺）穿过血脑屏障的可能性。静脉注射制剂后的镇痛效果被用作药物通过该屏障转运的指标。静脉注射颗粒制剂产生了长期且显著的镇痛效果。聚山梨醇酯80洛哌丁胺溶液引起的镇痛作用则不那么明显且非常短暂。载有洛哌丁胺的未包被纳米颗粒无法产生镇痛作用。载有洛哌丁胺的聚山梨醇酯80包被的聚氰基丙烯酸正丁酯纳米颗粒导致洛哌丁胺向脑内转运。
