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Folate Receptor‐Mediated Gene Delivery Using Folate‐Poly(ethylene glycol)‐Poly( L ‐lysine) Conjugate
Author(s) -
Cho Kyung Chul,
Kim Sun Hwa,
Jeong Ji Hoon,
Park Tae Gwan
Publication year - 2005
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.200500018
Subject(s) - conjugate , lipofectamine , gene delivery , peg ratio , chemistry , biophysics , transfection , polylysine , ethylene glycol , zeta potential , folate receptor , microbiology and biotechnology , biochemistry , materials science , nanoparticle , biology , recombinant dna , organic chemistry , nanotechnology , cancer cell , gene , mathematical analysis , genetics , mathematics , finance , cancer , vector (molecular biology) , economics
Summary: For efficient receptor‐mediated gene transfection, a new and simple formulation method based on using PEI and FOLPEGPLL conjugate was presented. Luciferase plasmid DNA and PEI were complexed to form slightly positive‐charged nanoparticles, onto which FOL‐PEG‐PLL conjugate was surface coated. With increasing the coating amount of FOL‐PEG‐PLL conjugate, the FOL‐PEG‐PLL/PEI/DNA complexes exhibited increased surface zeta‐potential values with concomitantly increased diameters, indicating that the PLL part was physically anchored on the surface of preformed PEI/DNA complexes with FOL moieties being exposed on the outside. The formulated complexes exhibited a considerably higher transfection efficiency against FOL receptor over‐expressing KB cells than FOL receptor deficient A549 cells. This was caused by an enhanced cellular uptake of the resultant complexes via a receptor‐mediated endocytosis process. The formulated complexes showed a higher gene expression level, even in the presence of serum, than the PEI/DNA or Lipofectamine/DNA complexes. This was attributed to the PEG chains present on the surface of complexes that could work as a protective shield layer against aggregation caused by non‐specific protein adsorption. The FOL‐PEG‐PLL/PEI/DNA complexes also demonstrated better cell viability than the PEI/DNA complexes.1 H NMR spectrum of FOL‐PEG‐PLL conjugate.