It is critical to understand a drug’s potential for partitioning in situations where the test drug has a high Log P (lipophilic). In this case, a large portion of the drug may be taken up and held by red blood cells (RBCs). For this reason, more informative data describing drug distribution in the blood can be obtained by measuring both the blood partitioning ratios and direct protein binding. When the comprehensive knowledge of protein binding and blood partitioning is understood, investigators can make a better determination about appropriate biological fluid, either whole blood, plasma, or serum should be collected to analyze the pharmacokinetic behavior of the drug.
Since certain compounds show specific binding to blood cells, choosing the most appropriate concentration to measure blood partitioning is crucial. If the concentration is too high, binding sites in the blood will be saturated and the partitioning cannot be effectively observed; if it is too low, the detection issues start to become apparent and the physiologically relevant range is missed. In addition, RBCs contain a variety of enzymes that can metabolize many drugs. Thus, the processing of blood samples should be done in accord with a protocol that is based on the results of previous studies, establishing the interaction between RBCs and the drug being developed. Sample protocols should specify the centrifugation time, temperature, and pH conditions, as well as need for addition of enzyme inhibitors. At Creative Bioarray, the red blood cell partitioning assay provides a specific and robust approach to assess these parameters using fresh blood from human and preclinical species.
- Fresh whole blood
- Rodent and non-rodent species upon request
- Blood/plasma ration
The Application of Red Blood Cell Partitioning
- This assay is used to determine the blood-to-plasma partitioning coefficient of a test compound in mice, rats, dogs, monkeys, or humans in vitro.
- Blood-to-plasma ratio is an important parameter, in conjunction with other ADME and physicochemical properties, for predicting whole body pharmacokinetics.
- A high blood-to-plasma ratio indicates the potential for drug accumulation in red blood cells and the risk of subsequent hematoxicity.
The Additional Benefits of the Interaction between Drugs and RBCs
- Rationally derived and physiologically correct reference concentration of the drug for computing organ clearances.
- Estimating the in vivo distribution of new cationic drugs.
- As an alternative method to determine plasma protein binding of drugs, particularly highly lipophilic drugs.
- Determining the desirable and undesirable effects of drugs on RBCs early.
Creative Bioarray has an experienced team of experts dedicated to providing customers with the most reliable and highest quality services. The red blood cell partitioning is one of our in vitro ADME screening services. Please contact us for further information.
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