Folate receptor targeted delivery of polyelectrolyte complex micelles prepared from ODN-PEG-folate conjugate and cationic lipids.
A polyelectrolyte complex micelle (PECM)-based delivery system for targeting folate (FOL) receptor overexpressing tumor cells is demonstrated using poly(ethylene glycol) (PEG)-conjugated oligonucleotide (ODN). The tumor targeting property was conferred to the PECM by tethering a folate moiety to the distal end of the PEG segment in an anti-sense green fluorescent protein (GFP) ODN-PEG conjugate. Nanoscale PECMs were spontaneously produced from ionic interactions between the ODN-PEG-FOL conjugate and a cationic lipid, lipofectamine (Lf). When treated with FOL receptor overexpressing cells (KB), the PCEMs caused a significant reduction in GFP expression in a dose-dependent manner. This effect was not observed in FOL receptor deficient cells (A549). The enhanced transfection of ODN-PEG-FOL/Lf PECMs to KB cells was caused by FOL receptor mediated endocytosis. The efficiency of target-specific gene suppression by ODN-PEG-FOL/Lf PECMs was maintained even in the presence of 10% fetal bovine serum in the transfection medium.
Kim
Sun Hwa
SH
Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon 305-701, South Korea.
Jeong
Ji Hoon
JH
Mok
Hyejung
H
Lee
Soo Hyun
SH
Kim
Sung Wan
SW
Park
Tae Gwan
TG
D002352:Carrier Proteins / Q000378:metabolism*; D002412:Cations; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D004573:Electrolytes / Q000737:chemistry; D058973:Folate Receptors, GPI-Anchored; D005492:Folic Acid / Q000378:metabolism*; D006801:Humans; D007624:KB Cells; D008055:Lipids / Q000737:chemistry*; D008422:Materials Testing; D008823:Micelles; D009841:Oligonucleotides / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D011956:Receptors, Cell Surface / Q000378:metabolism*
D002352:Carrier Proteins; D002412:Cations; D004337:Drug Carriers; D004573:Electrolytes; D058973:Folate Receptors, GPI-Anchored; D008055:Lipids; D008823:Micelles; D009841:Oligonucleotides; D011956:Receptors, Cell Surface; D011092:Polyethylene Glycols; D005492:Folic Acid