Unlocking Drug Potential: Precision Permeability Analysis by Creative Biolabs

Understanding and evaluating intestinal permeability is therefore essential in the early stages of drug development to predict how a drug will behave in the human body. One of the most widely recognized in vitro models for studying drug transport and permeability is the Caco-2 cell line. Derived from a human colon adenocarcinoma, the Caco-2 cell line is unique because, when cultured under appropriate conditions, it undergoes spontaneous differentiation to form a monolayer of polarized cells. This endogenous model closely mimics the epithelial lining of the human small intestine. This model is used to measure the transepithelial electrical resistance (TEER) as an indicator of tight junction integrity and to evaluate the transport of compounds from the apical (intestinal lumen side) to the basolateral (blood side) chambers.

The utility of the Caco-2 cell model lies in its ability to provide insights into the passive diffusion, active transport, and efflux of compounds. For instance, the model can be used to identify substrates for efflux transporters such as P-glycoprotein (P-gp), which can limit drug absorption by pumping drugs back into the intestinal lumen. Similarly, it can help in the identification of compounds that are actively transported into the cells, enhancing their absorption. Our assay employs HPLC-MS/MS detection to accurately measure the peak area response, providing detailed and reliable data on the permeability characteristics of drug candidates.

Our permeability analysis services encompass a variety of advanced methodologies to meet diverse research needs:

• Caco-2 Cell Line Assay
  • Cell Type: Human Caco-2 cells, resembling the epithelial lining of the human small intestine, are used for this assay.
  • Assay Type: Functional, cell-based assay.
  • Detection Method: HPLC-MS/MS is employed to measure peak area response, providing accurate quantification of drug permeability.
  • Procedure: The assay involves culturing Caco-2 cells on permeable supports to form a monolayer, mimicking the intestinal barrier. Compounds are introduced, and their transport across the monolayer is measured, offering insights into their permeability characteristics.
• High-Throughput Permeability Screening
  • Automated Systems: High-throughput screening using automated liquid handling systems to assess large compound libraries efficiently.
  • Procedure: Compounds are arrayed in microtiter plates, and incubated with Caco-2 cells, and permeability is analyzed using HPLC-MS/MS, enabling rapid identification of promising drug candidates.
• Tailored Permeability Profiling
  • Tailored assays to meet specific research objectives and compound properties.
  • Custom assays are developed to evaluate the permeability of compounds under various conditions, providing detailed permeability profiles and mechanistic insights.

Applications

• Drug Development: Evaluating the permeability of drug candidates to optimize formulations and enhance bioavailability.
• Lead Optimization: Screening and identifying compounds with favorable permeability characteristics for further development.
• Regulatory Compliance: Generating data to support regulatory submissions and demonstrate drug efficacy and safety.

Advantages

• Precision and Reliability: Our assays provide accurate and reproducible data, ensuring confidence in the results.
• Comprehensive Solutions: Offering a range of assays to address diverse research needs and drug development stages.
• Expertise and Innovation: Leveraging advanced technologies and scientific expertise to deliver cutting-edge solutions.

Through permeability screening using the Caco-2 model, researchers can classify drug candidates according to their permeability characteristics, predict their oral absorption potential, and identify potential absorption-related challenges early in the drug development process. This approach at Creative Biolabs helps in optimizing drug candidates for better bioavailability, ultimately leading to more effective and safer therapeutic agents. Contact us today to learn how we will accelerate your research and development processes.

For Research Use Only | Not For Clinical Use

Related Services

• Parallel Artificial Membrane Permeability Determination Service