BBB Penetration Assessment

The blood-brain barrier (BBB) is a structural and functional barrier between the interstitial fluid of the brain and the blood. On the one hand, it is a protective measure to maintain neural function and the homeostasis of the central nervous environment, on the other hand, it also poses challenges to the development of drugs for neurological diseases. The therapeutic potential of a neural drug candidate is not only related to its pharmacological target and biochemical activity, but also its effective dose when reaching the target. The ability of drugs to penetrate the blood-brain barrier is an important evaluation criterion in the development of neuropharmaceuticals, and it also directly determines whether enough effective molecules can cross the barrier to achieving a curative effect. At Creative Biolabs, we can achieve professional and first-class BBB penetration assessment with our cutting-edge technology and years of experience.

Background of BBB

The BBB is a highly selective semipermeable boundary composed of endothelial cells, astrocytes, pericytes, and a series of tightly linked proteins. The BBB lacks paracellular or transcellular pathways, so circulating molecules can only enter the brain interstitial fluid through one of two possible mechanisms: lipid-mediated free diffusion, or carrier- and receptor-mediated transport process. BBB only allows hydrophobic molecules and small molecules with a molecular weight of less than 400 and no more than 8 hydrogen bonds to pass through the barrier through lipid-mediated free diffusion, which means that without special design, all macromolecular drugs and most of the small-molecule drugs are excluded from the brain without a possible therapeutic effect.

Fig 1. Schematic of a simple BBB in vitro device. (Heymans, et al., 2018)

Drug delivery schemes targeting the BBB have been developed in recent years, including methods such as nanoparticles, liposomes, and cyclodextrins. These promising drug delivery means can deliver drugs to specific sites and protect them from being cleared by the circulatory system and can effectively control the dose and drug release.

Our BBB Penetration Assessment Services

The BBB prevents the brain from absorbing the vast majority of drugs, making many otherwise promising candidates for the central nervous system less effective when they are ongoing in vivo experiments. Creative Biolabs here provides stable, robust, and reproducible BBB penetration assessments for our worldwide clients, freeing you from tedious and time-consuming verification work, and devoting your time and energy to more important tasks. Whether you want to use a traditional in vitro BBB model or validate it directly in an animal model, we can develop a suitable experimental protocol for you and provide you with detailed and reliable data. If we can improve your project in any way or you have any further demands, please don't hesitate to contact us.

Reference

1. Heymans, M.; et al. Mimicking brain tissue binding in an in vitro model of the blood-brain barrier illustrates differences between in vitro and in vivo methods for assessing the rate of brain penetration. European Journal of Pharmaceutics and Biopharmaceutics. 2018, 127: 453-461.