Folate Receptor Targeted Delivery of Polyelectrolyte Complex Micelles Prepared from ODN-PEG-Folate Conjugate and Cationic Lipids

• Published in: Biotechnology progress Vol. 23; no. 1; pp. 232 - 237
• Main Authors: Kim, Sun Hwa, Jeong, Ji Hoon, Mok, Hyejung, Lee, Soo Hyun, Kim, Sung Wan, Park, Tae Gwan
• Format: Journal Article
• Language: English
• Published: USA American Chemical Society 2007
• Subjects: Carrier Proteins - metabolism; Cations; Cell Line, Tumor; Drug Carriers - chemistry; Drug Delivery Systems - methods; Electrolytes - chemistry; Folate Receptors, GPI-Anchored; Folic Acid - metabolism; Humans; KB Cells; Lipids - chemistry; Materials Testing; Micelles; Oligonucleotides - chemistry; Polyethylene Glycols - chemistry; Receptors, Cell Surface - metabolism
• ISSN: 8756-7938; 1520-6033
• DOI: 10.1021/bp060243g

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.