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. 2002 Nov-Dec;13(6):1220-5.
doi: 10.1021/bc025569z.

Efficient intracellular delivery of oligonucleotides formulated in folate receptor-targeted lipid vesicles

Wen Zhou  1 , Xing Yuan, Annette Wilson, Lijuan Yang, Michael Mokotoff, Bruce Pitt, Song Li
Affiliations

Efficient intracellular delivery of oligonucleotides formulated in folate receptor-targeted lipid vesicles

Wen Zhou et al. Bioconjug Chem. 2002 Nov-Dec.

Abstract

In this study, a novel lipid vector has been developed for targeted delivery of oligodeoxynucleotides (ODN) to tumors that overexpress folate receptor. This is based on a method developed by Semple et al. (1), which utilizes an ionizable aminolipid (1,2-dioleoyl-3-(dimethylammonio)propane, DODAP) and an ethanol-containing buffer system for encapsulating large quantities of polyanionic ODN in lipid vesicles. Folate is incorporated into the lipid vesicles via a distearoylphosphatidylethanolamine-poly(ethylene glycol) (DSPE-PEG) spacer. These vesicles are around 100-200 nm in diameter with an ODN entrapment efficiency of 60-80%. Folate mediated efficient delivery of ODN to KB cells that overexpress folate receptor. Uptake of folate-targeted lipidic ODN by KB cells is about 8-10-fold more efficient than that of lipidic ODN without a ligand or free ODN. This formulation is resistant to serum. Thus, targeted delivery of ODN via this novel lipid vector may have potential in treating tumors that overexpress folate receptors.

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