Drug Distribution & Binding

  • Overview
  • Services
  • Capabilities
  • Features
  • Applications
  • Explore Other Options

In the preclinical stage of drug development, a clear understanding of a compound's distribution profile and its affinity for plasma proteins, tissues, and biological barriers is essential for evaluating candidate potential. These interactions strongly influence pharmacokinetic (PK) and pharmacodynamic (PD) behavior, shaping systemic exposure, target engagement, and overall safety. For example, high plasma protein binding may prolong half-life but reduce the unbound, pharmacologically active fraction, while the ability to cross specialized barriers such as the blood–brain barrier (BBB) is a decisive factor for the success of CNS-directed therapeutics.

Creative Bioarray offers a range of in vitro and in vivo assays to understand how drug molecules are distributed, bound, and exposed in systemic and target tissues, supporting data-driven development and regulatory filings.

Key Services

Plasma Protein Binding Assay

Measures drug binding to plasma proteins using equilibrium dialysis and LC-MS/MS to predict free drug availability and distribution.

Blood-Plasma Partitioning Assay

Determines blood-to-plasma ratio using fresh whole blood to assess erythrocyte distribution and correct PK calculations.

Brain Tissue Binding Assay

Quantifies unbound drug fraction in brain homogenate via equilibrium dialysis for CNS penetration assessment.

Microsomal Binding Assay

Evaluates drug binding to liver microsomes to predict metabolic stability and clearance using LC-MS/MS.

Quantitative Tissue Distribution

Tracks radiolabeled compounds across tissues via QWBA to map organ-specific exposure and retention.

Target Tissue Exposure Analysis

Uses MALDI-MSI for cellular-level drug quantification in target organs (e.g., tumors).

Blood-Brain Barrier Penetration

Evaluates the ability of a drug to cross the BBB, crucial for CNS-targeted therapeutics.

Our Capabilities

Platform

  • LC-MS/MS – High-sensitivity quantification of drugs and metabolites.
  • Quantitative Whole-Body Autoradiography (QWBA) – Spatially resolved tissue distribution analysis.
  • MALDI-MSI – Cellular-level drug imaging in tissues.
  • ICP-MS – Sensitive quantification of trace metals and elements in biological matrices.

Model

In Vivo Models

Mice, rats, guinea pigs, canine, minipigs, and non-human primates, covering disease models for diverse research needs.

In Vitro Models

Hepatocytes, microvascular endothelial cells, brain homogenate, liver microsomes, and more for metabolism, toxicity studies, and early BBB permeability assessment.

Why Choose Us?

End-to-End Solutions

Covering in vitro binding assays through in vivo tissue distribution.

Advanced Technologies

LC-MS/MS, QWBA, MALDI-MSI, and proprietary software.

Customizable Designs

Species, time points, dosing routes, and disease models.

Expertise in CNS & Oncology

Specialized BBB and tumor penetration assays.

Applications

PK/PD Modeling

Enhance prediction accuracy of drug efficacy and safety.

Dose Optimization

Guide dose selection and optimization based on tissue-specific exposure.

CNS Drug Development

Assess brain penetration for neurological and psychiatric drugs.

Toxicology and Safety

Assess and mitigate risks of tissue accumulation.

Explore Other Options

For research use only. Not for any other purpose.