Folate-mediated targeting of antineoplastic drugs, imaging agents, and nucleic acids to cancer cells

J Control Release. 1998 Apr 30;53(1-3):39-48. doi: 10.1016/s0168-3659(97)00236-8.


The receptor for the vitamin, folic acid, is overexpressed on a number of human tumors, including cancers of the ovary, kidney, uterus, testis, brain, colon, lung, and myelocytic blood cells. Conjugates of folic acid linked via its gamma-carboxyl to either a single drug molecule or assembly of molecules can bind to and enter receptor-expressing cancer cells via folate receptor-mediated endocytosis. Because the affinity of folate conjugates for cell surface folate receptors is high (KD approximately 10(-10) M), folic acid derivatization allows the selective delivery of diagnostic and therapeutic agents to cancer cells in the presence of normal cells. This review will summarize studies aimed at folate-mediated targeting of protein toxins, imaging agents, antisense oligodeoxynucleotides, genes, and liposomes specifically to cancer cells in vitro and in vivo.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacokinetics*
  • Carrier Proteins / metabolism
  • Contrast Media / administration & dosage
  • Contrast Media / pharmacokinetics*
  • Endocytosis
  • Folate Receptors, GPI-Anchored
  • Folic Acid / metabolism*
  • Genetic Therapy
  • Humans
  • Hydrogen-Ion Concentration
  • Microscopy, Electron
  • Nucleic Acids / administration & dosage
  • Nucleic Acids / pharmacokinetics*
  • Receptors, Cell Surface*


  • Antineoplastic Agents
  • Carrier Proteins
  • Contrast Media
  • Folate Receptors, GPI-Anchored
  • Nucleic Acids
  • Receptors, Cell Surface
  • Folic Acid