Targeted Drug Delivery Systems Utilizing Folate Receptor Modulation
Summary
Folate receptors (FRs), notably the alpha and beta isoforms, are highly expressed on a range of tumour cells and on activated macrophages within the tumour microenvironment. Exploiting this differential expression enables selective delivery of therapeutic and diagnostic agents, minimising systemic toxicity and improving treatment efficacy. Strategies involve conjugating folic acid to small‐molecule drugs, antibodies or nanocarriers to create targeted constructs that bind FRs with high affinity and undergo receptor‐mediated endocytosis. Advances span from small molecule–drug conjugates and antibody–drug conjugates to multifunctional nanoparticles and liposomal vehicles incorporating folate ligands for enhanced tumour penetration. Photothermal and photodynamic approaches have harnessed folate‐decorated nanoparticles that release cytotoxic payloads or generate heat upon light activation. Gene therapy vectors modified with folate moieties afford selective transfection of both tumour cells and tumour‐associated macrophages, reshaping the immune microenvironment. Collectively, these systems demonstrate the global significance of FR modulation in improving the precision and safety of anticancer regimens, while offering platforms for combination therapies, real‐time imaging and personalised medicine.
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Targeted Drug Delivery Systems Utilizing Folate Receptor Modulation publication trend
The graph below shows the total number of articles in targeted drug delivery systems utilizing folate receptor modulation across all publications each year (not limited to Nature Index journals).
Technical terms
Folate receptor: A glycosylphosphatidylinositol-anchored cell‐surface protein that binds folic acid and mediates its internalisation via endocytosis.
Small molecule–drug conjugate: A therapeutic agent in which a cytotoxic or imaging payload is chemically linked to a low-molecular-weight targeting ligand such as folic acid.
Antibody–drug conjugate: A monoclonal antibody bound to a cytotoxic drug, combining the specificity of the antibody with the potency of the drug for targeted cell killing.
Liposome: A spherical vesicle composed of one or more phospholipid bilayers used to encapsulate and deliver therapeutic molecules selectively to target cells.
Photothermal therapy: A treatment modality that uses light‐absorbing agents to convert laser energy into localized heat, inducing tumour cell death.
Tumour‐associated macrophages: Macrophages within the tumour microenvironment that can support tumour growth and are targeted to modulate immune responses or deliver therapeutics.
References
- Nanosecond Laser Pulses Facilitating Efficient and Specific Cell Killing with Doxorubicin‐Loaded Gold Nanoparticles Targeted to the Folate Receptor. Small Science (2024).
- Targeting folate receptor β positive tumor-associated macrophages in lung cancer with a folate-modified liposomal complex. Signal Transduction and Targeted Therapy (2020).
- Formulation Strategies for Folate-Targeted Liposomes and Their Biomedical Applications. Pharmaceutics (2019).
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