Department of Pharmaceutics Utrecht Institute for Pharmaceutical Sciences, Utrecht University, PO Box 80082, 3508 TB Utrecht, The Netherlands.
Pharm Res. 2011 Mar;28(3):456-71. doi: 10.1007/s11095-010-0291-7. Epub 2010 Oct 7.
Several in vivo techniques have been developed to study and measure the uptake of CNS compounds into the brain. With these techniques, various parameters can be determined after drug administration, including the blood-to-brain influx constant (K(in)), the permeability-surface area (PS) product, and the brain uptake index (BUI). These techniques have been mostly used for drugs that are expected to enter the brain via transmembrane diffusion or by carrier-mediated transcytosis. Drugs that have limitations in entering the brain via such pathways have been encapsulated in nanoparticles (based on lipids or synthetic polymers) to enhance brain uptake. Nanoparticles are different from CNS compounds in size, composition and uptake mechanisms. This has led to different methods and approaches to study brain uptake in vivo. Here we discuss the techniques generally used to measure nanoparticle uptake in addition to the techniques used for CNS compounds. Techniques include visualization methods, behavioral tests, and quantitative methods.
已经开发出几种体内技术来研究和测量 CNS 化合物进入大脑的情况。使用这些技术，在给药后可以确定各种参数，包括血脑内流常数 (K(in))、渗透性表面积 (PS) 产物和脑摄取指数 (BUI)。这些技术主要用于预期通过跨膜扩散或载体介导的胞吞作用进入大脑的药物。那些通过这些途径进入大脑有限制的药物被包裹在纳米颗粒（基于脂质或合成聚合物）中以增强脑摄取。纳米颗粒在大小、组成和摄取机制方面与 CNS 化合物不同。这导致了研究体内脑摄取的不同方法和途径。除了 CNS 化合物使用的技术外，本文还讨论了一般用于测量纳米颗粒摄取的技术。这些技术包括可视化方法、行为测试和定量方法。
