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Synthesis of a polyamidoamine dendron-bearing lipid having sugar moieties and its use for preparation of nonviral gene vectors
Authors:Toshinari Takahashi  Eiji Yuba  Chie Kojima  Atsushi Harada  Kenji Kono
Affiliation:1. Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University, 1-1 Gakuen-cho, Naka-ku, Sakai, Osaka, 599-8531, Japan
2. Nanoscience and Nanotechnology Research Center, Research Institutes for Twenty First Century, 1-2 Gakuen-cho, Naka-ku, Sakai, Osaka, 599-8570, Japan
Abstract:We have so far developed a new type of cationic lipid that consists of an amine-terminated poly(amidoamine) dendron and two long alkyl chains. In this study, we designed a dendron-bearing lipid (DL) modified with sugar moieties as the ligand at the terminal groups of the dendron to improve the transfection activities. We combined lactobionic acid at the end of every dendritic branch of the DL to produce galactose moieties-attached DL (Gal-DL). The lipoplexes containing Gal-DL exhibited enhancement of transfection of HepG2 cells. Moreover, Gal-DL significantly promoted the transfection activity of the lipoplexes including poly(ethylene glycol)-attached dendron-bearing lipid (PEG-DL).
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