Bioorganic & Medicinal Chemistry Letters 2007-06-01

A tetra(L-lysine)-grafted poly(organophosphazene) for gene delivery.

Yong Joo Jun, Jung Hee Kim, Su Jin Choi, Hwa Jeong Lee, Moo Jin Jun, Youn Soo Sohn

Index: Bioorg. Med. Chem. Lett. 17 , 2975-2978, (2007)

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Abstract

In order to develop a new gene delivery vector, a novel cationic poly(organophosphazene) was synthesized by stepwise nucleophilic substitutions of poly(dichlorophosphazene) with a hydrophilic methoxy-poly(ethylene glycol) (MPEG) as a shielding group and a branched tetra(L-lysine), LysLys(LysEt)(2), as a cationic moiety. The cationic polymer has shown to form a polyplex by DNA condensation and very low in vitro cytotoxicity probably due to the shielding effect of MPEG, which provides a basis for improving the low gene transfection yield of cationic polyphosphazenes.