Development of tumor associated macrophages-selective DDS and its application to tumor therapy

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Tumor-associated macrophages (TAM) exhibit an M2 phenotype that promotes tumor progression, and conversion of M2 TAM toward a tumouricidal M1 phenotype is a promising anti-cancer therapy. However, little has been reported on TAM-selective drug delivery because a specific ligand is lacked. Mannosylated carriers would be an effective approach, but they can be distributed to all of macrophages that highly expressed mannose receptors in the body. In this study, we succeeded to develop a mannosylated bubble lipoplex and ultrasound irradiation to tumor site for TAM-selective delivery of nucleic acid.