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Folate Receptor Targeted Delivery of Polyelectrolyte Complex Micelles Prepared from ODN‐PEG‐Folate Conjugate and Cationic Lipids
Author(s) -
Kim Sun Hwa,
Jeong Ji Hoon,
Mok Hyejung,
Lee Soo Hyun,
Kim Sung Wan,
Park Tae Gwan
Publication year - 2007
Publication title -
biotechnology progress
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.572
H-Index - 129
eISSN - 1520-6033
pISSN - 8756-7938
DOI - 10.1021/bp060243g
Subject(s) - lipofectamine , transfection , folate receptor , peg ratio , conjugate , chemistry , cationic liposome , biophysics , endocytosis , receptor , gene delivery , ethylene glycol , micelle , oligonucleotide , microbiology and biotechnology , biochemistry , biology , cancer cell , recombinant dna , mathematics , genetics , cancer , vector (molecular biology) , mathematical analysis , dna , finance , aqueous solution , economics , gene , organic chemistry
Abstract 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.