Hekmatara Telli, Gelperina Svetlana, Vogel Vitali, Yang Shang-Ray, Kreuter Jörg
Institute of Pharmaceutical Technology, J.-W Goethe-University, Max-von-Laue Str 9, D-60438 Frankfurt, Germany.
J Nanosci Nanotechnol. 2009 Aug;9(8):5091-8. doi: 10.1166/jnn.2009.gr05.
Hydrophobic drugs, loperamide and paclitaxel, were loaded in poly(butyl cyanoacrylate) nanoparticles by polymerization of n-butyl-2-cyanoacrylate in aqueous-organic media in the presence of a drug. The particles were stabilized by dextran 70,000 and poloxamer 188 or by 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-5000] sodium salt. It was shown that in the presence of dichloromethane, methanol or ethanol the encapsulation efficiency of loperamide in the nanoparticles reached 80%. Loading of paclitaxel was efficient only in the presence of the lipid. The organic solvents did not significantly influence the nanoparticle morphology or their physicochemical parameters. Thus produced poly(butyl cyanoacrylate) nanoparticles enabled delivery of loperamide across the blood-brain barrier, which was evidenced by the drug analgesic effect evaluated by the tail-flick test.
疏水性药物洛哌丁胺和紫杉醇通过在药物存在下于水-有机介质中使氰基丙烯酸正丁酯聚合，被载入聚氰基丙烯酸丁酯纳米颗粒中。这些颗粒用70000葡聚糖和泊洛沙姆188或用1,2-二油酰基-sn-甘油-3-磷酸乙醇胺-N-[甲氧基(聚乙二醇)-5000]钠盐进行稳定化处理。结果表明，在二氯甲烷、甲醇或乙醇存在的情况下，洛哌丁胺在纳米颗粒中的包封率达到80%。紫杉醇仅在脂质存在时才能有效载入。有机溶剂对纳米颗粒的形态或其物理化学参数没有显著影响。如此制备的聚氰基丙烯酸丁酯纳米颗粒能够使洛哌丁胺透过血脑屏障，甩尾试验评估的药物镇痛作用证明了这一点。
