Journal
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 123, Issue -, Pages 153-161Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2018.07.036
Keywords
Mannose; Lipid; Serine-glycine repeat spacer; Macrophage; Liposome
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Funding
- JSPS KAKENHI [18H03535]
- Takeda Science Foundation
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The mannose receptor, which is responsible for tumor invasion, proliferation, and metastasis in the tumor microenvironment, is overexpressed in tumor-associated macrophages. Mannose is commonly applied to PEGylated liposomes in macrophage-targeted cancer therapy. To develop a high functionality and quality (HFQ) lipid for macrophage-targeted liposomes, we designed a novel mannosylated lipid with improved mannose receptor binding affinity using serine-glycine repeats (SG)(n). We synthesized Man(S)-(SG)(5)-SSK-K(Pal)(2) using only a fluorenylmethyloxycarbonyl (Fmoc) protecting group solid-phase peptide synthesis method, which produced a high-quality lipid at a moderately good yield. We then prepared Man-(SG)(5)/PEGylated liposomes using a post-insertion technique to insert Man(S)-(SG)(5)-SSK-K(Pal)(2 )into the PEGylated liposomes. In vitro cell investigations revealed that the Man-(SG)(5)/PEGylated liposomes effectively associated with mouse peritoneal macrophages by interacting with the mannose receptors. The results suggest that we produced a novel high-quality, highly functional mannosylated lipid that is suitable for clinical drug delivery applications.
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