Folate Targeted

Drug Delivery

Folate receptors are cellular surface markers for numerous solid tumors and
myeloid leukemias. Avanti now offers a derivative, DSPE-PEG-folate, which
can be incorporated into liposomes as a targeting ligand.

DSPE-PEG(5000)Folate
Avanti Number 880123
49

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Folate Receptors
1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[folate(polyethylene glycol)-2000]
(ammonium salt)
Avanti Number 880124

Folate Receptor-Mediated Drug Targeting: From Therapeutics to Diagnostics

Hilgenbrink A.R., Low P.S. Department of Chemistry, Purdue University, West Lafayette, Indiana 47907

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.
2005 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 94:21352146, 2005
References

1. Chiu, S.J., S. Liu, D. Perrotti, G. Marcucci, and R.J. Lee. (2006). Efficient delivery of a Bcl-2-specific antisense

oligodeoxyribonucleotide (G3139) via transferrin receptor-targeted liposomes. J Control Release 112:199-207.
2. Wu, J., Q. Liu, and R.J. Lee. (2006). A folate receptor-targeted liposomal formulation for paclitaxel.

Int J Pharm 316:148-53.
3. Shiokawa, T., Y. Hattori, K. Kawano, Y. Ohguchi, H. Kawakami, K. Toma, and Y. Maitani. (2005). Effect of polyeth

ylene glycol linker chain length of folate-linked microemulsions loading aclacinomycin A on targeting ability

and antitumor effect in vitro and in vivo. Clin Cancer Res 11:2018-25.
4. Zhang, Y., L. Guo, R.W. Roeske, A.C. Antony, and H.N. Jayaram. (2004). Pteroyl-gamma-glutamate-cysteine

synthesis and its application in folate receptor-mediated cancer cell targeting using folate-tethered liposomes.

Anal Biochem 332:168-77.
5. Gabizon, A., A.T. Horowitz, D. Goren, D. Tzemach, F. Mandelbaum-Shavit, M.M. Qazen, and S. Zalipsky. (1999).

Targeting folate receptor with folate linked to extremities of poly(ethylene glycol)-grafted liposomes: in vitro

studies. Bioconjug Chem 10:289-98.

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