期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 521, 期 1-2, 页码 361-364出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2017.02.041
关键词
Liposomes; Targeting; PEG; Drug delivery; HER2
资金
- JSPS KAKENHI [16108862]
- Shinnihon Foundation of Advanced Medical Treatment Research
- Novartis Pharma Research Grant
- Grants-in-Aid for Scientific Research [16K18862] Funding Source: KAKEN
Ligand peptide-grafted PEGylated liposomes have been widely studied for targeted drug delivery systems. Because ligand peptides are commonly grafted using PEG as a spacer on the surface of PEGylated liposomes, the interaction between ligand peptides and their corresponding receptors can be interrupted by steric hindrance of the PEG layer. Therefore, we aimed to develop ligand peptide-lipid derivatives to enhance the targeting efficiency of ligand peptide-grafted PEGylated liposomes, and designed a new ligand peptide-lipid derivatives having serine-glycine repeats (SG)(n) as a spacer based on the peptide length calculated by PyMol (v0.99). We selected KCCYSL (KCC) as the ligand peptide for binding to human epidermal growth factor receptor-2 (HER2). We synthesized new KCC-(SG) n-lipid derivatives (n = 3, 5, 7) and evaluated their cellular association in breast cancer cells. KCC-(SG) n/PEGylated liposomes dramatically increased cellular association on HER2-positive breast cancer cells. The results suggest that KCC can be grafted on the surface of KCC-(SG) n/PEGylated liposomes prepared from KCC-(SG) n-lipid derivatives (n = 3, 5, 7). In summary, we succeeded in developing KCC-(SG) n-lipid derivatives for the preparation of ligand peptide-grafted PEGylated liposomes. (C) 2017 Elsevier B.V. All rights reserved.
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