OhioMod2013:Methods/folate

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Folate-PEG-amine Synthesis

The folate receptor is overexpressed in cancer cells, especially with ovarian malignancies. This can attributed to the need for the cancer cells to take in more folic acid, otherwise known as vitamin B9, eessential for rapid cell division. Therefore there seems to be potential to attaching folate to our nanoparticles to increase their selectivity towards the Folate Receptor expressing cancer cells. We also know that this sort of targeting has shown to be more effective when the folate is coupled with a PEG spacer. Since we are using PEG to coat the CPNPs, it is consistent for us to try the same strategy. Much of this protocol comes from W.E. Hennink's lab in the Netherlands[1] and from Xiaboin Zhao's thesis in Dr. Robert Lee's lab from Ohio State.

Materials

• Folic acid dihydrate
• polyethylene glycose bis-amine
• Discuccinimidyl suberate(DSS)
• Dimethyl Sulfoxide

scheme 1

1. van Steenis JH, van Maarseveen EM, Verbaan FJ, Verrijk R, Crommelin DJ, Storm G, and Hennink WE. Preparation and characterization of folate-targeted pEG-coated pDMAEMA-based polyplexes. J Control Release. 2003 Feb 21;87(1-3):167-76. DOI:10.1016/s0168-3659(02)00361-9 |