Folate Receptor and Targeting Strategies

  • Bhagyashri Joshi
  • Sukhada S. Shevade
  • Prajakta Dandekar
  • Padma V. DevarajanEmail author
Part of the AAPS Advances in the Pharmaceutical Sciences Series book series (AAPS, volume 39)


The folate receptor (FR) is essential for intracellular transport of folic acid, a vital enzymatic cofactor required for cell survival and growth. FR exists in four isoforms termed as α, β, γ, and δ having variable affinity for folate ligand and exhibit differential expression in normal tissues. The receptors are known to amplify in a broad spectrum of cancers and therefore have been extensively explored to treat as well as to diagnose various cancers. This chapter presents an overview of the receptor family, ligands explored, pathophysiological features, importance of FR in therapeutics and diagnostics, different FR-mediated delivery systems, and clinical studies relying on FR targeting.


Folate Cancer Infectious disease Macrophage Targeting Photodynamic therapy Theranostics 



5 Methyl tetrahydrofolate




human lung adenocarcinoma cell line




Acute lymbhoblastic leukemia


Acute myelogenous leukemias




Clusters of differentiation




Chronic lymphocytic leukemia


Chronic myelogenous leukemias


Computed tomography


Deoxyribonucleic acid


Dipalmitoyl phosphatidylethanolamine





EPR effect

Enhanced permeation and retention effect


Folic acid


Folic acid–polyethyleneglycol/polyethyleneoxide-poly(Ɛ-caprolactone)


Folic acid–polyethylene glycol–doxorubicin


Folic acid–polyethylene glycol–polylactic acid


Fluorescein isothiocyanate


Folate receptor


Glutamic acid




Glycosyl phosphatidylinositol


High density lipid


Cervical cancer cell lines


Hepatocellular carcinoma cell line



HT 29

A human colorectal adenocarcinoma cell line


A human fibrosarcoma cell line


Human antigen R


Inhibitory concentration 50



JEG-3 and JAR

Placental choriocarcinoma cell lines


Line KB is now known to be a subline of the ubiquitous KERATIN-forming tumor cell line HeLa



mab 343

A monoclonal antibody to FR-α

mab 909

A monoclonal antibody to FR-β




Gastric cancer cell line


Magnetic resonance imaging


Messenger RNA


Near infra red


nanostructured lipid carriers






Polyethylene glycol


Polyethylene oxide-polypropylene oxide-poly(Ɛ-caprolactone)


Positron emission tomography






Poly lactic-co-glycolic acid






Reduced folate carrier


Ribonucleic acid




Small interfering RNA


Ovarian cancer cell line


Solid lipid nanoparticles


Tumor-associated macrophages








Ultraviolet A




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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Bhagyashri Joshi
    • 1
  • Sukhada S. Shevade
    • 1
  • Prajakta Dandekar
    • 2
  • Padma V. Devarajan
    • 2
    Email author
  1. 1.Department of Pharmaceutical Sciences & TechnologyInstitute of Chemical TechnologyMumbaiIndia
  2. 2.Department of Pharmaceutical SciencesInsitute of Chemical Technology, Deemed University, Elite Status and Centre of Excellence, Government of MaharashtraMumbaiIndia

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