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Dual-ligand modification of PEGylated liposomes shows better cell selectivity and efficient gene delivery

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Title: Dual-ligand modification of PEGylated liposomes shows better cell selectivity and efficient gene delivery
Authors: Kibria, Golam Browse this author
Hatakeyama, Hiroto Browse this author →KAKEN DB
Ohga, Noritaka Browse this author
Hida, Kyoko Browse this author
Harashima, Hideyoshi Browse this author
Keywords: Targeted delivery
PEGylated liposome
RGD motif
Cell penetrating peptide
Gene expression
Issue Date: 30-Jul-2011
Publisher: Elsevier
Journal Title: Journal of Controlled Release
Volume: 153
Issue: 2
Start Page: 141
End Page: 148
Publisher DOI: 10.1016/j.jconrel.2011.03.012
PMID: 21447361
Abstract: The objective of this study was to develop an efficient dual-ligand based PEGylated liposomal delivery system that had target specificity as well as properties that would enhance cellular uptake. PEGylated liposomes (PEG-LP) were prepared by the lipid film hydration method by adding distearoyl phosphoethanolamine-polyethylene-glycol-2000 conjugate (DSPE-PEG2000) to a lipid mixture. The cyclic RGD (Arg-Gly-Asp) peptide, a specific ligand with affinity for Integrin αvβ3 was coupled to the distal end of the PEG on the PEG-LP (RGD-PEG-LP). Stearylated octaarginine (STR-R8) was incorporated on the surface of the RGD-PEG-LP as dual-ligand (R8/RGD-PEG-LP) that functions as a cell penetrating peptide (CPP). RGD-PEG-LP and R8/RGD-PEG-LP were preferentially taken up by caveolae-mediated and clathrin-mediated endocytosis pathways, respectively. Compared to PEG-LP, R8/RGD-PEG-LP showed an enhanced cellular uptake as well as a higher transfection efficiency in Integrin αvβ3 expressing cells. However, the amount of cellular uptake or gene expression by the single ligand versions was negligible, even in Integrin αvβ3 expressing cells. No remarkable difference in cellular uptake or gene expression was observed for cells in which the expression of targeted receptors was absent. It can be concluded that dual-ligand modified PEG-LP possesses a strong capability for the efficient internalization of PEG-LP and consequently would be an effective tool for the targeted delivery of macromolecules or chemotherapeutics through accelerated cellular uptake.
Type: article (author version)
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 畠山 浩人

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