Design and evaluation of polyamidoamine dendrimer conjugate with PEG, α-cyclodextrin and lactose as a novel hepatocyte-selective gene carrier in vitro and in vivo
作者： Yuya Hayashi , Taishi Higashi , Keiichi Motoyama , Yoshimasa Mori , Hirofumi Jono
DOI: 10.3109/1061186X.2013.769105
关键词:
摘要: AbstractTo develop a novel hepatocyte-selective gene carrier, we prepared polyamidoamine starburst dendrimer (generation 3, G3) conjugates with three functional molecules, i.e. α-cyclodextrin, polyethylene glycol (PEG, molecular weight = 2170) and lactose (PEG-LαCs), evaluated delivery efficiency of these in vitro vivo. PEG-LαC (G3, degrees substitution the PEG moiety (DSP) 2.1) showed higher transfer activity than other PEG-LαCs DSP4.0, 6.2) HepG2 cells, expressing asialoglycoprotein receptor, decreased HeLa non-expressing receptor presence asialofetuin. High DSP2.1) was retained even 50% serum, although α-cyclodextrin/lactosylated (G3) conjugate (Lac-α-CDE (G3)), which is lacking moiety, severely 20% serum. provided negligible cytotoxicity up to charge ratio 50 (carri...
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