Department of Biomedical Sciences, University of Modena and Reggio Emilia, Modena, Italy.
Nanomedicine. 2009 Dec;5(4):369-77. doi: 10.1016/j.nano.2009.02.005. Epub 2009 Mar 31.
The pharmacological treatment of neurological disorders is often complicated by the inability of drugs to pass the blood-brain barrier. Recently we discovered that polymeric nanoparticles (NPs) made of poly(D,L-lactide-co-glycolide), surface-decorated with the peptide Gly-L-Phe-D-Thr-Gly-L-Phe-L-Leu-L-Ser(O-beta-D-glucose)-CONH2 are able to deliver, after intravenous administration, the model drug loperamide into the central nervous system (CNS). This new drug delivery agent is able to ensure a strong and long-lasting pharmacological effect, far greater than that previously observed with other nanoparticulate carriers. Here we confirmed the effectiveness of this carrier for brain targeting, comparing the effect obtained by the administration of loperamide-loaded NPs with the effect of an intracerebroventricular administration of the drug; moreover, the biodistribution of these NPs showed a localization into the CNS in a quantity about two orders of magnitude greater than that found with the other known NP drug carriers. Thus, a new kind of NPs that target the CNS with very high specificity was discovered.
This paper discusses a nanoparticle-based technique of targeted drug delivery through the blood-brain barrier. The biodistribution of these novel nanoparticles showed two orders of magnitude greater efficiency compared to other known NP drug carriers.
神经障碍的药物治疗常常由于药物无法穿透血脑屏障而变得复杂。最近我们发现，由聚（D，L-丙交酯-co-乙交酯）制成的聚合物纳米颗粒（NPs），表面用肽 Gly-L-Phe-D-Thr-Gly-L-Phe-L-Leu-L-Ser（O-β-D-葡萄糖）-CONH2 修饰，经静脉给药后，可将模型药物洛哌丁胺递送至中枢神经系统（CNS）。这种新的药物递送剂能够确保强大而持久的药理作用，远远超过以前使用其他纳米载体观察到的作用。在这里，我们通过比较洛哌丁胺负载 NPs 给药和脑室内给药获得的效果，证实了这种载体对大脑靶向的有效性；此外，这些 NPs 的生物分布显示出 CNS 定位，其数量比其他已知的 NP 药物载体高两个数量级。因此，发现了一种针对中枢神经系统具有非常高特异性的新型 NPs。
本文讨论了一种基于纳米颗粒的靶向药物递送技术，通过血脑屏障。与其他已知的 NP 药物载体相比，这些新型纳米粒子的生物分布效率提高了两个数量级。
