Journal
TETRAHEDRON
Volume 64, Issue 9, Pages 2233-2240Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2007.12.027
Keywords
heterobifunctional PEG; TentaGel (R) resin; perfluoroalkylated amphiphile; DNA nanoparticles; dimerizable cationic detergents; non-viral gene delivery; synthetic viruses; folic acid
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A very efficient, versatile as well as simple to perform procedure was developed in order to prepare a heterobifunctional amphiphilic PEG-NH(2) derivative which can be used for conjugation to a targeting ligand (such as folic acid). This method proceeds by a mixed solid-liquid phase strategy using a TentaGel (R) PAP resin, a copolymer consisting of a polystyrene matrix on which a PEG (M(w) 3400 Da) terminated by an amino function has been grafted. Solid phase chemistry was used for the conjugation of a highly hydrophobic moiety. After release from the resin, the amphiphilic PEG-OH conjugate was converted into its corresponding amphiphilic PEG-NH(2) derivative (four steps in 77% overall yields). This procedure allowed the preparation of similar to 330 mg batches. This derivative was then coupled to folic acid, a ligand that is used for the targeting of drug (gene) carrier and delivery systems to cells over-expressing the folate receptor. The low and high molecular weight of folic acid and its amphiphilic PEG-folate conjugate, respectively, allowed easy purification by dialysis and led to the targeted compound with high recovery. (C) 2007 Elsevier Ltd. All rights reserved.
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