Advances in drug research depend not only on high-throughput screening to evaluate large numbers of compounds but also on the development of in vitro models that can mimic human tissues in terms of permeability and functions. Potential failures, such as poor permeability or interaction with efflux drug transporters, can influence the drug candidate's progression onto the next stages of the drug development process.
Most drugs need to pass through at least one cellular membrane to reach the intended target. Although tight binding of a drug molecule to its intended target is important for efficacy, poor membrane permeability often means poor or nonexistent efficacy in vivo. Therefore, membrane permeability is a key property to consider during drug design, especially when dealing with small molecules with intracellular targets, since their efficacy highly depends on their ability to cross the membrane. At the same time, permeability is an important factor affecting oral absorption, blood-brain barrier permeation, and transport of drugs into tissues and across cell membranes. The permeability of a drug across a membrane is dependent on the passive permeability as well as the susceptibility of the drug to efflux or uptake by drug transporter proteins.
Creative Bioarray offers a wide range of complementary in vitro models to evaluate drug permeability and predict drug absorption and distribution.
With decades of operational experience, Creative Bioarray is able to provide the following analytical services based on our permeability models:
- Predict various permeability processes (paracellular, transcellular)
- Estimate different intracellular concentrations (membrane, cytosol, lysosome)
- Assess impact of experimental variability on the predicted outcomes
- Analysis of measured in vitro permeability data
All absorption and permeability assays are available in standard human and animal model systems, and can be ordered individually, combined or as a selection of key services in our candidate assessment packages to provide cost savings.
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