@article{oai:nagasaki-u.repo.nii.ac.jp:00001536, author = {Suga, Tadaharu and Watanabe, Masanori and Sugimoto, Yuri and Masuda, Tomonari and Kuroda, Naotaka and Hagimori, Masayori and Kawakami, Shigeru}, journal = {Journal of Drug Delivery Science and Technology}, month = {Feb}, note = {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., Journal of Drug Delivery Science and Technology, 49, pp.668-673; 2019}, pages = {668--673}, title = {Synthesis of a high functionality and quality lipid with gp130 binding hydrophobic peptide for the preparation of human glioma cell-targeted PEGylated liposomes}, volume = {49}, year = {2019} }