Folate receptor mediated intracellular protein delivery using PLL-PEG-FOL conjugate

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To develop a receptor-mediated intracellular delivery system that can transport therapeutic proteins or other bioactive macromolecules into a specific cell, a di-block copolymer conjugate, poly(L-lysine)-polyethylene glycol)-folate (PLL-PEG-FOL), was synthesized. The PLL-PEG-FOL conjugate was physically complexed with fluorescein isothiocyanate conjugated bovine serum albumin (FITC-BSA) in an aqueous phase by ionic interactions. Cellular uptake of PLL-PEG-FOL/FITC-BSA complexes was greatly enhanced against a folate receptor over-expressing cell line (KB cells) compared to a folate receptor deficient cell line (A549 cells). The presence of an excess amount of free folate (1 mM) in the medium inhibited the intracellular delivery of PLL-PEG-FOL/FITC-BSA complexes. This suggests that the enhanced cellular uptake of FITC-BSA by KB cells in a specific manner was attributed to folate receptor-mediated endocytosis of the complexes having folate moieties on the surface. The PLL-PEG-FOL di-block copolymer could be potentially applied for intracellular delivery of a wide range of other biological active agents that have negative charges on the surface. (c) 2005 Elsevier B.V All rights reserved.
Publisher
Elsevier Science Bv
Issue Date
2005-04
Language
English
Article Type
Article
Keywords

POLYION COMPLEX MICELLES; ENTRAPPING ENZYME MOLECULES; DRUG-DELIVERY; BLOCK-COPOLYMER; ANTISENSE OLIGONUCLEOTIDE; GENE DELIVERY; TARGETED DRUG; CELLS; PEPTIDE; SYSTEM

Citation

JOURNAL OF CONTROLLED RELEASE, v.103, no.3, pp.625 - 634

ISSN
0168-3659
DOI
10.1016/j.jconrel.2004.01.006
URI
http://hdl.handle.net/10203/13111
Appears in Collection
BS-Journal Papers(저널논문)
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