Folate receptor-mediated drug targeting: From therapeutics to diagnostics

Andrew R. Hilgenbrink, Philip Low

Research output: Contribution to journalShort surveypeer-review

568 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)2135-2146
Number of pages12
JournalJournal of Pharmaceutical Sciences
Issue number10
StatePublished - Jan 1 2005


  • Arthritis
  • Cancer chemotherapy
  • Folate conjugate
  • Folate receptor
  • Imaging methods
  • Inflammatory disease
  • Liposomes
  • Nano-particles
  • Targeted drug delivery

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science


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