Peptide Drugs Blood-brain Barrier Permeability Test Platform

* Please kindly note that our products and services can only be used to support research purposes (Not for clinical use).

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As a professional biomedical company, Creative Peptides focuses on the research and development of new peptides, and are committed to providing customers with a comprehensive blood-brain barrier permeability test platform and related services. Our platform combines advanced technology and extensive experience to accelerate the development and clinical translation of new drugs.

Blood-brain barrier permeability test procedure

What is the blood-brain barrier?

The blood-brain barrier (BBB), a delicate structure located at the interface between the endothelium and glial cells in the brain vessel, and at the interface between plasma and cerebrospinal fluid in the choroid plexus, plays a crucial gatekeeper role. It delicately screens and allows vital substances such as oxygen, glucose, essential amino acids and small molecules of fat-soluble substances to enter the brain, while effectively blocking foreign substances including many drugs, maintaining the stability of the brain environment and the healthy functioning of nerve cells. This high degree of selective permeability, although a cornerstone of central nervous system health, also constitutes a major obstacle to the development of drugs for the treatment of brain diseases, especially for peptide drugs with large molecular weights and specific polarity, whose natural permeability is limited, greatly limiting the potential application in the treatment of central nervous system diseases.

Can peptides cross the blood-brain barrier?

As a therapeutic drug, peptides have great potential due to their high specificity and potency. However, their ability to cross the blood-brain barrier is inherently limited by their size, hydrophilicity, and susceptibility to enzymatic degradation. In the face of this challenge, researchers have embarked on a variety of strategies aimed at overcoming the limitations of the blood-brain barrier to peptide drugs and broadening their application in the treatment of brain diseases.

Chemical modification strategy: Through the introduction of non-natural amino acids such as β-enyl amino acid, not only enhanced the binding ability of peptide molecules to specific receptors, improved enzyme stability, but also significantly improved its ability to penetrate the blood-brain barrier.

Yin-yang balance design: Through carefully designed chemical modifications on both ends of the peptide, such as n-terminal guanidylation and C-terminal aromatic cyclic chlorination, the fine regulation of molecular charge was achieved, significantly enhancing the efficiency of the peptide crossing the blood-brain barrier.

Carrier and receptor-mediated delivery: The use of carrier systems or receptor-specific binding methods, such as the access of oligo-arginine sequences at both ends of the peptide, although it may affect the direct affinity of the drug to the target, but significantly improve the efficiency of brain drug delivery through indirect mechanisms.

Transmembrane peptide fusion: The integration of sequences with known transmembrane ability into peptide drugs directly facilitates the crossing of peptide molecules across the blood-brain barrier, significantly enhancing intracranial delivery efficiency.

Our blood-brain barrier permeability testing services

We offer a full range of blood-brain barrier permeability testing services for peptide drug discovery on our professional and advanced biomedical services platform, designed to accelerate your research and development process and increase the success rate of your project.

Preliminary evaluation of blood-brain barrier permeability assay in vitro

We rely on advanced in vitro models to simulate the complex physiological structure and function of the blood-brain barrier, and use primary brain endothelial cells, astrocytes and pericytes to co-culture and construct a highly simulated co-culture system. This strategy creates a tightly controlled and highly repeatable experimental environment for the study of blood-brain barrier permeability, which is particularly suitable for early drug screening and helps researchers efficiently select promising candidate compounds. Key features include:

High simulation co-culture model: human brain endothelial cells, astrocytes and pericytes were integrated to ensure the physiological relevance and prediction accuracy of the model.

Application of Transwell system: The Transwell system was used to establish a single-layer endothelial cell model, accurately divide the upper and lower compartments, simulate the environment on both sides of blood and brain tissue, and measure the transmembrane resistance (TEER) to evaluate the single-layer integrity.

Precision permeability measurement: The permeability quantification of labeled molecules is used to accurately evaluate the permeability of candidate peptides.

In-depth in vivo model validation

For further verification and optimization, we used animal models such as mice and rats, combined with microdialysis technology and imaging technology (MRI, CT), to investigate the distribution of peptide drugs in the central nervous system in detail, and evaluate their pharmacokinetic characteristics and targeting efficiency in vivo.

Other services

High throughput screening and precise quantification: Rapid evaluation of a large number of candidate peptides with a high-throughput screening platform and precise quantitative analysis through cutting-edge technologies such as LC-MS/MS to ensure accurate and reliable data.

Data interpretation and reporting: Our team of experts provide detailed data analysis and reporting to help you understand the penetration and potential central nervous system availability of peptide drugs.

Personalized analysis and mechanism exploration: Provide customized services to meet specific research needs, explore peptide transport mechanisms in depth, and identify key factors affecting permeability.

Optimization and validation: Improve peptide formulations and delivery strategies to enhance blood-brain barrier penetration.

Cutting-edge and innovative platform technology

Our test bed incorporates cutting-edge technologies to maximize analysis accuracy and reliability.

Dynamic blood flow simulation: By simulating the hemodynamics within the blood-brain barrier, the shear stress under real physiological conditions is reproduced to improve the physiological relevance of the model.

Three-dimensional (3D) culture technology: The use of 3D culture systems to build a more realistic cell microenvironment, significantly enhancing the usefulness of predictive models.

Real-time monitoring and analysis: Integrated live cell imaging and impedance measurement technology to achieve real-time monitoring of the dynamic changes of the blood-brain barrier and the transport process of peptides, providing immediate feedback for research.

Through these comprehensive services and technologies, we are committed to providing comprehensive and in-depth blood-brain barrier permeability testing solutions, promoting the development of peptide drugs, and opening up new paths for the treatment of central nervous system diseases.


1. What is the purpose of testing the blood-brain barrier (BBB) permeability of peptide drugs?

Testing the BBB permeability of peptide drugs is essential to determine their ability to reach the central nervous system (CNS). This evaluation helps in understanding whether the therapeutic peptides can effectively cross the BBB to exert their intended pharmacological effects in the brain.

2. What types of peptide drugs can be tested using your platform?

Our platform is capable of testing a wide range of peptide drugs, including small peptides, cyclic peptides, peptidomimetics, and peptide-based conjugates. We can also accommodate modified peptides designed to enhance BBB penetration.

3. How do you simulate the blood-brain barrier in your assays?

We use advanced in vitro models that replicate the BBB's structure and function. This includes co-culture systems with human brain endothelial cells, astrocytes, and pericytes, as well as dynamic flow systems to mimic physiological blood flow conditions.

4. What specific assays are included in your BBB permeability testing services?

  • Transendothelial electrical resistance (TEER) measurement: To assess the integrity of the endothelial cell monolayer.
  • Permeability assays: Using marker molecules and peptide drugs to measure their transport across the BBB.
  • Real-time monitoring: Employing live-cell imaging and impedance-based techniques to continuously monitor BBB integrity and permeability.

5. How are the results of BBB permeability tests analyzed?

Results are analyzed using a combination of quantitative techniques such as LC-MS/MS for precise peptide quantification and computational models to interpret transport mechanisms. We provide detailed reports with comprehensive data analysis and insights into the peptide's BBB permeability.

6. Can your platform be used for high-throughput screening of multiple peptide candidates?

Yes, our platform supports high-throughput screening, allowing the evaluation of numerous peptide candidates in parallel. This accelerates the drug discovery process by quickly identifying peptides with favorable BBB permeability profiles.

7. What are the key advantages of using your BBB permeability test platform?

  • Physiologically relevant models: Advanced in vitro models that closely mimic the human BBB.
  • Customization: Tailored assays to meet specific research needs.
  • Comprehensive Analysis: Detailed data interpretation and reporting.
  • Advanced technologies: Use of dynamic flow systems, 3D culture models, and real-time monitoring.

8. Can you help with the development and optimization of peptide formulations to enhance BBB permeability?

Yes, we offer services for the development and optimization of peptide formulations. This includes chemical modifications, encapsulation strategies, and other approaches to improve BBB penetration and stability.

* Please kindly note that our products and services can only be used to support research purposes (Not for clinical use).
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