Influence of particle size on transport of methotrexate across blood brain barrier by polysorbate 80-coated polybutylcyanoacrylate nanoparticles
Influence of particle size on transport of methotrexate across blood brain barrier by polysorbate 80-coated polybutylcyanoacrylate nanoparticles
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DOI：
10.1016/j.ijpharm.2005.11.040
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发表时间：
2006-03-09
影响因子：
5.8
通讯作者：
Jiang, XG
中科院分区：
文献类型：
--
作者：
Gao, KP;Jiang, XG
本实验研究了不同大小的甲氨蝶呤聚氰基丙烯酸丁酯纳米粒的血脑屏障转运。采用乳液聚合法制备载药纳米粒。用聚山梨酯80包被后，分别静脉注射大小为70、170、220、345 nm的纳米颗粒。给大鼠注射3.2 mg/kg。未包被的纳米粒和甲氨蝶呤溶液也被静脉注射。注射剂量与对照组相同。分别于注射后0.5h、1 h、1.5 h、2 h、3 h、4 h采集脑脊液和脑组织进行检测。用高效液相色谱法测定所有生物样品中的药物浓度。研究发现，与未包被的纳米粒和单纯的溶液相比，包被聚山梨酸酯80的纳米粒可以显著提高脑组织和脑脊液中的药物浓度。70纳米纳米颗粒可以将更多的药物输送到脑内，而其他三种尺寸的纳米颗粒之间没有明显的差异。综上所述，聚山梨酸酯80包覆的聚氰基丙烯酸丁酯纳米粒可用于克服血脑屏障，尤其是直径小于100 nm的血脑屏障。(C)2005 Elsevier B.V.保留所有权利。
Transports of methotrexate-loaded polybutylcyanoacrylate nanoparticles with different sizes across blood brain barrier were investigated in this experiment. The drug-loaded nanoparticles were prepared by emulsion polymerization method. After coating with polysorbate 80, nanoparticles with the size 70, 170, 220, 345 nm were, respectively, i.v. injected into rats at the dose of 3.2 mg/kg. Uncoated nanoparticles and methotrexate solution were also i.v. injected at the same dosage as controls. 0.5, 1, 1.5, 2, 3, 4 h after injection, cerebrospinal fluids and brain tissues were collected for tests. Drug level in all biological samples was determined by HPLC. It was found out that nanoparticles overcoated by polysorbate 80 could significantly improve the drug level in both brain tissues and cerebrospinal fluids compared with uncoated ones and simple solution. Seventy-nanometer nanoparticles could deliver more drugs into brain while no significant difference was observed among the other three size ranges. In conclusion, polysorbate 80-coated polybutylcyanoacrylate nanoparticles could be used to overcome blood brain barrier especially those whose diameter was below 100 nm. (C) 2005 Elsevier B.V. All rights reserved.