Schröder U, Sabel B A
Institute of Medical Psychology, Medical Faculty, Otto-v.-Guericke University, Magdeburg, Germany.
Brain Res. 1996 Feb 26;710(1-2):121-4. doi: 10.1016/0006-8993(95)01375-x.
The Leu-enkephalin dalargin does not normally penetrate the blood brain barrier when given intravenously. Drug targeting to the brain was investigated by using poly(butylcyanoacrylate) nanoparticles which were coated with polysorbate 80. When injected intravenously in mice, dalargin-loaded nanoparticles coated with the polysorbate 80 induced an analgesic effect at doses of 5.0 mg/kg and 7.5 mg/kg dalargin as shown by hindlimb licking on the hot plate. Neither the intravenous injection of dalargin alone at various doses nor the mixture of dalargin-loaded nanoparticles without the polysorbate 80 were able to induce an analgesic activity. This confirms previous observations that nanoparticles provide a convenient method to deliver drugs across the blood-brain barrier.
亮氨酸脑啡肽达来argin通常静脉给药时不能穿透血脑屏障。通过使用涂有聚山梨酯80的聚（氰基丙烯酸丁酯）纳米颗粒来研究药物向脑的靶向作用。当以5.0毫克/千克和7.5毫克/千克的达来argin剂量静脉注射到小鼠体内时，涂有聚山梨酯80的载有达来argin的纳米颗粒在热板上通过后肢舔舐表现出镇痛作用。单独静脉注射各种剂量的达来argin或不含聚山梨酯80的载有达来argin的纳米颗粒混合物均不能诱导镇痛活性。这证实了先前的观察结果，即纳米颗粒提供了一种方便的方法来使药物穿过血脑屏障。
