Macrophages are prospective targets for therapeutic agents containing carbohydrates due to the presence of C-type lectins. Targeting macrophage mannose receptors for drug delivery is being paid more and more attention. Creative Biolabs has organized a staff of outstanding scientists who have engaged in mannosylated liposome design and development for many years. We are glad to serve our global clients with professionalism and expertise in this field.

Targeting Macrophage Mannose Receptor

Macrophage mannose receptor (MR), also known as CD206 or MRC1, is a highly glycosylated type I transmembrane protein that belongs to the C-type lectin receptor (CLEC) family and a member of the polylectin mannose receptor family. It was first identified in rabbit alveolar macrophages in the 1970s and is predominantly distributed on the surface of macrophages, dendritic cells (DCs) and avascular endothelial cells. As a marker for M2-type macrophages, its expression is regulated by cytokines such as IL-4, IL-13, IL-10 and dexamethasone.

Fig.1 Structure of the mannose receptor (MR) and the overview of its cellular functions.^1,3

MR consists of the following extracellular structural domains:

• CR structural domain: Bind sulfonyl glycan chains.
• FNII structural domain: Bind collagen.
• 8 C-type lectin structural domains (CTLD): Recognize sugars such as mannose, fucose, N-acetylglucosamine (GlcNAc).
• Transmembrane domains and cytoplasmic tail: The cytoplasmic tail is short and lacks typical signaling motifs, suggesting that it is dependent on other receptors for signaling.

Some interesting studies are associated with the use of mannosylated liposomes for the delivery of therapeutic agents. Mannose-modified nanoparticles (e.g., liposomes, chitosan) target macrophages via MR-mediated endocytosis to deliver siRNA or anti-inflammatory drugs for the treatment of metabolic diseases. Mannosylated delivery system induces the conversion of M1-type macrophages to M2-type and attenuates pathological damage such as inflammatory bowel disease.

Drug Delivery by Targeting Mannose Receptors at Creative Biolabs

Studies have shown that mannose residues have the highest receptor affinity for macrophage mannose receptors. Moreover, mannose is an inexpensive and readily accessible reagent. Thus, active targeting of macrophage mannose receptors can be considered as an efficient strategy for the design of targeted delivery systems. With an experienced team of experts in the development of macrophage-targeted liposome drug delivery systems, Creative Biolabs has accumulated rich experience in mannosylated liposome design and development.

We provide delivery system design and technical solutions for targeting MR.

Table 1 Delivery system design and technical solutions for targeting MR.

We typically cover the full chain of development services.

• Receptor ligand screening and validation: Assessment of ligand binding affinity to MR using surface plasmon resonance (SPR) or flow cytometry. Validation of target specificity by gene editing.
• Carrier synthesis and functionalization: Chemical synthesis or bioengineering.
• In vitro/in vivo validation.

MR-targeted drug delivery development services provide efficient and safe solutions for infectious disease, cancer and immunomodulatory therapies through precise ligand design, multifunctional vector construction and rigorous in vitro and in vivo validation. By integrating customized technology platforms and rich experience, we help our clients break through the limitations of traditional delivery systems.

Related Products

As a leading service provider focusing on the development of drug delivery systems targeting macrophages MR, we are committed to providing specialized and customized solutions to our customers. In doing so, we have a deep understanding of the challenges faced by researchers when conducting macrophage research. Therefore, we also provide our clients with a range of macrophage research tools to support their needs in both basic and applied research.

Our research tools include cells and assay kis. Whether it is the development of drug delivery systems targeting macrophages or the provision of various macrophage research tools for researchers, we look forward to working with you.

Service Features

Cross-disciplinary Integration

Combining immunology, nanotechnology, and research needs to provide a one-stop service from target validation to preclinical validation.

Specificity Advantage

MR is highly expressed in pathogens and tumor microenvironments, while normal tissues have low expression, reducing off-target effects.

Flexibility

Small molecule chemotherapeutic agents, nucleic acids or immunomodulators can be loaded to meet different development needs.

Publications

Igor D. Zlotnikov et al. synthesized a series of mannosylated carriers based on mannan, polyethyleneimine (PEI) and cyclodextrin (CD) and studied the molecular structure. Depending on the type of carrier, particle sizes range from as small as 10-50 nm to as large as 500 nm and may be suitable for creating a variety of drug forms. Non-specific capture of cells was achieved with increased selectivity for CD206+ macrophages.

Fig. 2 Scheme of synthesis of mannan-amCD and mannan-spermine-HPCD.^2,3

It was found that pathogen localization sites can be accessed through polymeric mannosylation systems that circulate in the body for longer periods of time and penetrate more readily into the lungs - alveolar macrophages.

Scientific Resources

Learn More Macrophages in Diseases

Download Macrophage Recruitment and Chemotaxis

Learn More Development of Fine Liposome Nanoplatforms for Macrophage Clearance

Learn More Isolation and Identification of Macrophages

Q & A

Q: What does your custom development service model include?

A: We provide full-process customization services, covering modules including needs analysis and vector design, process development and optimization, and preclinical study support. Customers can choose modularized services (e.g., carrier design only) or all-inclusive development, with project cycle and cost flexibly adjusted according to demand.

Q: What is the typical development cycle of a project?

A: The development cycle of a project usually varies depending on the specific requirements. If complex customization requirements are involved, such as the design of a specific drug or carrier, this may extend the development time. Our R&D team will work closely with our customers to ensure that their expectations are fully understood and met during the development process.

References

1. Paurević, Marija, Martina Šrajer Gajdošik, and Rosana Ribić. "Mannose ligands for mannose receptor targeting." International journal of molecular sciences 25.3 (2024): 1370. https://doi.org/10.3390/ijms25031370
2. Zlotnikov, Igor D., et al. "Mannosylated Systems for Targeted Delivery of Antibacterial Drugs to Activated Macrophages." International Journal of Molecular Sciences 23.24 (2022): 16144. https: //doi.org/10.3390/ijms232416144
3. Under Open Access license CC BY 4.0, without modification.