The blood/brain barrier (BBB) is formed by the brain endothelial cells and is identified as a structural and chemical barrier between the brain and systemic circulation. BBB studies are prerequisite for explaining preclinical efficacy and toxicology results. On the other hand, overcoming the obstacles of delivering therapeutic drugs to specific sites of the brain has become a main challenge of treating most brain diseases. With years of operational experience, Creative Biolabs now provides BBB study services using qualitative measurements of drug exposure, to evaluate your new therapeutic agents.

Blood/Brain Barrier (BBB)

The blood/brain barrier (BBB) is highly selective semipermeable membrane barrier, which is defined as a physical and metabolic barrier that separates the circulating blood from the brain and extracellular fluid in the central nervous system (CNS). The blood/brain barrier is formed of brain capillary endothelium. It permits water, some gases, and lipid-soluble molecules to pass by passive diffusion, and also allows the selective transport of molecules such as glucose and amino acids that are essential to neural function. Moreover, it prevents the entrance of lipophilic potential neurotoxins by means of the P-glycoprotein-mediated active transport mechanism. Astrocytes have been supposed to be necessary to set up the blood-brain barrier. However, a few regions in the brains do not have a blood/brain barrier, such as the circumventricular organs.

The illustration of the blood-brain barrier (BBB). Fig.1. The illustration of the blood-brain barrier (BBB). (Liu, et al., 2012)

Blood/Brain Barrier (BBB) Permeability

Drug delivery across the BBB is challenging, predominantly due to the physical restriction of paracellular diffusion between the endothelial cells which constitute the microvessels of the BBB, as well as the activity of efflux transporters which speedily expel back into the capillary lumen turning into a wide range of xenobiotics. The BBB creates an obstacle to drug delivery that prevents essentially 100% of large-molecule drugs (e.g., monoclonal antibodies, antisense drugs) and more than 98% of small molecule drugs from entering the brain under normal circumstance. Consequently, it is of significant importance to characterize the BBB permeability of candidate drugs as early as possible in drug discovery.

Our Advantages

  • A team of scientists who are proficient in BBB studies;
  • Extensive experience with various administration routes, including IV, IP, PO, IM, IN, SC, and ICV, as well as short- or long-term continuous infusions;
  • Combination of BBB studies and bioanalytical method.

What We Offer

Creative Biolabs is recognized as a world leader in the industry of drug discovery, providing standard and customized in vivo pharmacokinetic assays with the largest and most diverse portfolio. Our scientists specialized in BBB studies will work with you to characterize the properties of your drug candidate to develop a dosing and sample collection strategy that will offer the most meaningful data for your research. BBB studies in Creative Biolabs can be conducted with both standard or custom bioanalytical methods, to provide a complete pharmacokinetic profile for your drug candidate.

Additionally, Creative Biolabs now offers a set of in vivo pharmacokinetic assay services in addition to cassette dosing studies, including:

Besides, you might be also interested in other in vivo PK studies listed below:

If you have any special needs in in vivo pharmacokinetic assays or be interested in learning more about Creative Biolabs’ pharmacokinetic assay services, please contact us for more information.


  1. Liu, T. B.; et al. Molecular mechanisms of cryptococcal meningitis. Virulence. 2012, 3(2): 173.

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