In Vivo Methods to Estimate Drug Transport to the Brain Across the Blood-Brain Barrier

Abstract

In this paper, we review the in vivo methods to estimate drug transport to the brain. These vary from invasive ones like the brain uptake index (BUI), multiple pass techniques, brain efflux index (BEI), in situ brain perfusion, CSF (cerebrospinal fluid) sampling (unit impulse response), quantitative autoradiography (QAR), and intracerebral microdialysis to non invasive ones like positron emission tomography (PET), and magnetic resonance techniques (imaging (MRI), spectroscopy (MRS)). The latter two methods can be applied in human also. In addition, in this review an overview is given for which purposes these methods can be applied.

An improved method of transcutaneous cisterna magna puncture for cerebrospinal fluid sampling in rats

“…Numerous in vivo models are available to measure the drug transport to the brain using different animal species (de Boer and Gaillard, 2005). In the pharmaceutical industry, various in vitro methods were also used, however in vitro-in vivo correlations are weaker when using in vitro cell based BBB transport assays to predict in vivo B/P ratio due to the presence of various confounding variables (Garberg et al, 2005).…”