Synthesis of high functionality and quality mannose-grafted lipids to produce macrophage-targeted liposomes

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Masayori HagimoriShigeru Kawakami

Abstract

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.

Citations

Jan 18, 2020·Current Cancer Drug Targets·Kuldeep Rajpoot
Mar 21, 2020·Frontiers in Immunology·Clara I ColinoCarmen Gutierrez-Millan
Dec 1, 2020·Biochemistry·Xizheng SunTakeshi Mori
Apr 17, 2021·Drug Delivery·Siwei SongYang Jin
Jul 16, 2021·Molecular Pharmaceutics·Despo ChatzikleanthousRoberto Adamo

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