Folate receptor-mediated drug targeting: from therapeutics to diagnostics

J Pharm Sci. 2005 Oct;94(10):2135-46. doi: 10.1002/jps.20457.


Folate targeted drug delivery has emerged as an alternative therapy for the treatment and imaging of many cancers and inflammatory diseases. Due to its small molecular size and high binding affinity for cell surface folate receptors (FR), folate conjugates have the ability to deliver a variety of molecular complexes to pathologic cells without causing harm to normal tissues. Complexes that have been successfully delivered to FR expressing cells, to date, include protein toxins, immune stimulants, chemotherapeutic agents, liposomes, nanoparticles, and imaging agents. This review will summarize the applications of folic acid as a targeting ligand and highlight the various methods being developed for delivery of therapeutic and imaging agents to FR-expressing cells.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / therapeutic use
  • Biomarkers, Tumor / metabolism*
  • Carrier Proteins / metabolism*
  • Drug Delivery Systems*
  • Folate Receptors, GPI-Anchored
  • Folic Acid / administration & dosage*
  • Folic Acid / chemistry
  • Humans
  • Immunotherapy
  • Liposomes
  • Nanostructures
  • Neoplasms / diagnostic imaging
  • Neoplasms / drug therapy
  • Neoplasms / metabolism*
  • Neoplasms / therapy*
  • Radionuclide Imaging
  • Radiopharmaceuticals
  • Receptors, Cell Surface / metabolism*
  • Toxins, Biological / administration & dosage
  • Toxins, Biological / therapeutic use


  • Antineoplastic Agents
  • Biomarkers, Tumor
  • Carrier Proteins
  • Folate Receptors, GPI-Anchored
  • Liposomes
  • Radiopharmaceuticals
  • Receptors, Cell Surface
  • Toxins, Biological
  • Folic Acid