In Vitro Blood-Brain Barrier (BBB) Permeability Assay Service

Accelerate Neurotherapeutic Discovery with High-Fidelity BBB Models!

The blood-brain barrier (BBB) is a highly selective interface that limits CNS drug delivery. Approximately 98% of small molecules and nearly all large biologics fail to cross the BBB effectively. Leveraging recent breakthroughs in triculture co-culture systems, human iPSC-derived cells, and dynamic microfluidics, in vitro BBB models now offer predictive insights into brain permeability. Are you struggling with high CNS drug attrition, poor BBB predictability, or lack of reliable early-stage screening platforms? Creative Biolabs delivers next-generation BBB permeability assays validated by tight junction markers, transporter activity, and transendothelial electrical resistance (TEER).

We provide customizable, physiologically relevant in vitro BBB assay services for:

• Small Molecule & Biologic Screening: Assessing passive and active transport mechanisms.
• Permeability Coefficients (Papp): Quantification via real-time compound tracing.
• TEER Measurement & Tight Junction Profiling: Using impedance and imaging-based readouts.
• Efflux Transporter Assays: Evaluating compound susceptibility to P-gp and BCRP.
• Custom Model Development: Incorporating disease-relevant variables (e.g., inflammation, hypoxia, tumor-derived factors).

Our service delivers high-confidence BBB screening results that drive CNS-targeted drug development forward. With Creative Biolabs, clients receive:

• Reliable prediction of CNS drug penetration.
• Mechanistic insights into passive vs. active transport behavior.
• Disease-relevant model customization.
• Scalable, high-throughput capability.

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Strategies

Creative Biolabs integrates advanced BBB modeling strategies designed to closely mimic in vivo physiological and transport conditions:

• iPSC-Derived Endothelial Systems: Simulating human-specific transporter expression (e.g., GLUT1, P-gp, BCRP).
• Triculture Co-Culture Models: Combining endothelial cells, astrocytes, and pericytes for full neurovascular unit fidelity.
• 3D Spheroid and Chip-Based Models: Enabling complex barrier integrity and real-time transcytosis tracking.
• High-Throughput Screening Integration: Tailored to early-phase permeability and CNS drug profiling studies.

These approaches ensure translatable, reproducible, and cost-effective solutions for pharmaceutical and academic CNS research.

Workflow

Required Starting Materials

• Chemical identity, solubility, and concentration range of compound(s)
• Route of administration and intended CNS indication
• Specific interest in transporter or disease phenotype modulation

Highlights

Human-Relevant & Validated Models

Built with iPSC-derived cells, our models replicate the neurovascular unit with high TEER values and strong expression of tight junction and transporter proteins, offering reliable BBB permeability assessment.

Flexible Formats for Any Need

Choose from Transwell, microfluidic chip, or 3D spheroid models tailored to different throughput and compound classes, supporting everything from screening to mechanistic studies.

Pathology-Inclusive Models

Simulate disease-relevant conditions like inflammation or hypoxia to assess compound behavior in compromised BBB environments such as tumors or neurodegeneration.

High-Throughput Compatibility

Supports 96- and 384-well formats and automated workflows, enabling fast screening of large compound libraries during early-phase drug discovery.

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Publication

Drug permeability results reveal distinct transport characteristics across in vitro blood-brain barrier models established with human iPSC-derived brain microvascular endothelial cells. Compounds with high permeability, such as propranolol and caffeine, efficiently crossed the barrier, while low-permeability compounds like atenolol and inulin showed restricted passage. The data underscore the model's ability to discriminate between passive diffusion and restricted transport, aligning closely with known in vivo behavior. This highlights its utility for early-stage CNS drug screening, allowing accurate classification of compounds based on their BBB penetration potential.

Fig.1 Assessment of drug permeability.¹

Customer Reviews

• "Improved CNS Prediction Accuracy"
  Using Creative Biolabs' in vitro BBB assay in our research has significantly improved the predictability of our CNS candidate's permeability. The TEER and tight junction readouts gave us much-needed confidence in lead selection. March 2025, Dr. A***n
• "Accelerated BBB Screening Pipeline"
  Creative Biolabs helped us streamline our high-throughput permeability screening with their well-validated triculture model. We were able to quickly eliminate non-penetrant compounds and focus our efforts more efficiently. June 2025, Prof. K***i
• "Efflux Transport Insight"
  Using Creative Biolabs' BBB assay, we confirmed our compound's interaction with P-gp and adjusted our formulation accordingly. Their transporter inhibition data proved instrumental in overcoming our delivery barrier. April 2025, Dr. M***o

FAQs

Extended Services

Creative Biolabs also offers several complementary services to enhance your BBB permeability testing project.

Creative Biolabs provides cutting-edge, human-relevant BBB permeability assessment solutions tailored to support neuropharmaceutical innovation. From discovery to preclinical studies, we help you reduce risk, save time, and enhance translatability.

Contact Our Team for More Information and to Discuss Your Project

Reference

1. Ohshima, Makiko, et al. "Prediction of drug permeability using in vitro blood–brain barrier models with human induced pluripotent stem cell-derived brain microvascular endothelial cells." BioResearch open access 8.1 (2019): 200-209. DOI: 10.1089/biores.2019.0026. Distributed under Open Access license CC BY 4.0, without modification.