Synthesis of a high functionality and quality lipid with gp130 binding hydrophobic peptide for the preparation of human glioma cell-targeted PEGylated liposomes
In: Journal of Drug Delivery Science and Technology, Jg. 49 (2019-02-01), Heft 1, S. 668-673
Online
serialPeriodical
Zugriff:
We developed high functionality and quality (HFQ) lipids for facile and rapid preparation of ligand-grafted PEGylated liposomes. Because HFQ lipids are designed to exhibit good water dispersibility, ligand-grafted PEGylated liposomes can be easily prepared using the post-insertion method. The aim of this study is to develop novel VTWTPQAWFQWV (VTW) peptide-HFQ lipid to target human glioma cells. In order to disperse in water, VTW-(SG)5-lipid derivatives containing various amino acid residues with different charges were synthesized. Based on our previous work, (SG)5, a serine-glycine repeated peptide with a discrete molecular weight, was used as a spacer between the VTW and lipid. Of the derivatives tested, VTW-K3-(SG)5-lipid with three lysine residues showed the highest dispersibility in water, and VTW-K3-(SG)5/PEGylated liposomes can be prepared using the post-insertion method. The sizes of PEGylated liposomes and VTW-K3-(SG)5/PEGylated liposomes were 69.5 ± 4.4 and 74.4 ± 5.0 nm, respectively. In addition, the zeta potentials of PEGylated liposomes and VTW-K3-(SG)5/PEGylated liposomes were −2.7 ± 1.6 and −1.3 ± 0.3 mV, respectively. We found that VTW-K3-(SG)5/PEGylated liposomes selectively associated with human glioma U251MG cells. We succeeded in developing water-dispersible VTW-K3-(SG)5-lipids for the preparation of VTW-grafted PEGylated liposomes for glioma cell targeting.
Titel: |
Synthesis of a high functionality and quality lipid with gp130 binding hydrophobic peptide for the preparation of human glioma cell-targeted PEGylated liposomes
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Autor/in / Beteiligte Person: | Suga, Tadaharu ; Watanabe, Masanori ; Sugimoto, Yuri ; Masuda, Tomonari ; Kuroda, Naotaka ; Hagimori, Masayori ; Kawakami, Shigeru |
Link: | |
Zeitschrift: | Journal of Drug Delivery Science and Technology, Jg. 49 (2019-02-01), Heft 1, S. 668-673 |
Veröffentlichung: | 2019 |
Medientyp: | serialPeriodical |
ISSN: | 1773-2247 (print) |
DOI: | 10.1016/j.jddst.2018.12.037 |
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