In search of the Holy Grail: Folate-targeted nanoparticles for cancer therapy

Alfonso Garcia-Bennett, Matthias Nees, Bengt Fadeel (Corresponding Author)

Research output: Contribution to journalArticleScientificpeer-review

95 Citations (Scopus)


Targeted drug therapy or “smart” drug delivery, potentially combined with simultaneous imaging modalities to monitor the delivery of drugs to specific tissues, is arguably the “holy grail” of pharmacology. Therapeutic approaches that exploit nanoparticles to deliver drugs selectively to cancer cells are currently considered one of the most promising avenues in the area of cancer therapeutics and imaging. The potential to deliver active chemotherapeutic drugs in the vicinity or directly within specific tumors via receptor mediated pathways, and to image tumors through the use of nanoparticles has been conceptually and experimentally shown for several classes of nanoparticles. Nanoparticles functionalized with the vitamin folic acid are of particular interest as a variety of malignant tumors are known to overexpress the folate receptor(s). Indeed, several nanoparticle architectures with improved retention time, administration route, biocompatibility, absorption, and clearance are being proposed and are in late stage clinical development. This commentary highlights some of the most important concepts related to nanoparticles and folate-mediated drug delivery and imaging in cancer research.
Original languageEnglish
Pages (from-to)976-984
Number of pages8
JournalBiochemical Pharmacology
Issue number8
Publication statusPublished - 2011
MoE publication typeA1 Journal article-refereed


  • Nanoparticle
  • folic acid
  • targeted delivery
  • toxicity


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