Schroeder U, Sommerfeld P, Ulrich S, Sabel B A
Institute of Medical Psychology, and Institute of Clinical Pharmacology, Medical Faculty, Otto-v.-Guericke University, Leipziger Str. 44, 39120 Magdeburg, Germany.
J Pharm Sci. 1998 Nov;87(11):1305-7. doi: 10.1021/js980084y.
The Leu-enkephalin dalargin and the Met-enkephalin kyotorphin normally do not cross the blood-brain barrier (BBB) when given systemically. To transport these neuropeptides across the BBB they were adsorbed onto the surface of poly(butylcyanoacrylate) nanoparticles (NPs) and the NPs were coated with polysorbate 80. Central analgesia was measured by the hot plate test in mice. The antidepressant amitriptyline, which normally penetrates the BBB, was used to examine the versatility of the NP method. The concentration of amitriptyline in serum and brain of mice was determined by a gas chromatographic method. Furthermore, NPs were fabricated with different stabilizers. After the adsorption of the peptides on polysorbate 85-stabilized NPs, analgesia was noted after intravenous application when NPs were not coated. The amitriptyline level was significantly enhanced in brain when the substance was adsorbed onto the NP and coated or when the particles were stabilized with polysorbate 85.
亮氨酸脑啡肽达来argin和甲硫氨酸脑啡肽京都啡肽经全身给药时通常不能穿过血脑屏障（BBB）。为了使这些神经肽穿过血脑屏障，将它们吸附到聚（氰基丙烯酸丁酯）纳米颗粒（NPs）表面，并用聚山梨酯80包被NPs。通过小鼠热板试验测定中枢镇痛作用。通常能穿透血脑屏障的抗抑郁药阿米替林用于检验NP方法的通用性。采用气相色谱法测定小鼠血清和脑中阿米替林的浓度。此外，用不同的稳定剂制备了NPs。在聚山梨酯85稳定的NPs上吸附肽后，静脉给药未包被NPs时可观察到镇痛作用。当物质吸附到NP上并包被或颗粒用聚山梨酯85稳定时，脑中阿米替林水平显著提高。
