Blood Brain Barrier Permeability Test Services for Radiopharmaceuticals
Rdcthera is dedicated to supporting the radiopharmaceutical industry by providing the latest CRO services. The tests offered are executed at a high professional level with key areas of expertise focused on BBB permeability tests, the most imperative of which are for radiopharmaceuticals targeted at brain tissues.
Understanding the Blood-Brain Barrier
The blood-brain barrier is a highly selective permeability barrier that shields the brain from probable toxic substances but allows essential molecules, including oxygen and nutrients. Thus, crossing this barrier is crucial for radiopharmaceuticals targeting brain targets. A huge number of radiopharmaceuticals are incapable of passing through the BBB, either due to low solubility in the membrane bilayer or recognition and consequent efflux by efflux pumps like P-glycoprotein and breast cancer resistance protein. Therefore, the developmental steps of these compounds are reputed to be critical in evaluating permeability across the BBB.
Fig. 1. In vitro microfluidic-integrated BBB models. (Choi JH, et al., 2019)
Our Comprehensive In Vitro BBB Permeability Test Services
At Rdcthera, we offer state-of-the-art in vitro blood-brain barrier permeability test services. Our experienced team utilizes sophisticated BBB models to evaluate the permeation of radiopharmaceuticals through the layers of cells without being affected by efflux pumps. We conduct cell-based assays to assess the susceptibility of compounds to efflux pumps and use in silico scoring systems to predict the likelihood of successful BBB penetration.
- In vitro permeability assays to evaluate the ability of compounds to traverse the BBB
- Efflux pump interaction studies to determine susceptibility to P-glycoprotein and breast cancer resistance protein.
- Physicochemical property analysis to assess key attributes like logP, polar surface area, hydrogen donor count, and pKa.
Our In Vitro Blood Brain Barrier Models
We make use of advanced in-vitro BBB models that physiologically represent the human brain. Our models are designed to
- Mimic passive diffusion from the blood, apical side to brain, basolateral side.
- Elucidate the role and impact of efflux pumps on drug permeation.
- Offer a robust platform for lead optimization and initial screening of drug candidates.
| Our In Vitro BBB Models |
- Epithelial cells over-expressing
|
|
- Transwell monoculture model
|
|
- Dynamic in vitro (DIV) model
|
|
Experimental Methods
The experimental methods are designed with good care to ensure proper and reproducible results.
- Cell-Based Assays - Test interactions with efflux pumps
- Permeability Assays - Using advanced in-vitro BBB models.
- Physicochemical Property Measurements - Using techniques such as shake flask, HPLC, and NMR.
Data and Insights
Our services provide a wealth of data and insights, including
- Permeability coefficients.
- Interaction profiles with efflux pumps.
- Physicochemical property data.
- Predictive scores for BBB penetration.
Applications of In Vitro BBB Permeability Test
It is in such information, if derived from blood-brain barrier permeability testing, that can be of essence in the optimization of radiopharmaceutical design and in vivo behavior predictions, also in the selection of promising candidates for further development. Make informed decisions and accelerate the progress of your drug discovery projects through our services.
- High throughput screening of early stage drug candidates.
- Development of drug formulations with an optimized BBB penetration potential.
- Regulatory submissions and compliance.
Feel free to contact us for more information regarding our services related to blood-brain barrier permeability testing and how we can further support radiopharmaceutical development.
Reference
- Choi JH, Santhosh M, Choi JW. (2019). In vitro Blood-Brain Barrier-Integrated Neurological Disorder Models Using a Microfluidic Device. Micromachines (Basel). 11(1):21.
For research use only. Not intended for any clinical use.
Related Service
