Evaluation of antitumor effect of tumor-associated macrophage-targeting liposomes

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We investigated the possibility of whether depletion of tumor-associated macrophages (TAMs) by zoledronic acid (ZOL) entrapped in folate-linked liposome (FL-ZOL) could inhibit tumor angiogenesis and consequently tumor growth. FL-ZOL showed high cytotoxicity for FR-positive KB and murine macrophage RAW264.7 cells, but not for FR-negative Colon 26 cells, suggested that FL-ZOL was selectively taken up via FR-mediated endocytosis. However, injections of FL-ZOL did not induce antitumor activities for KB and Colon 26 tumor-bearing mice, and had a lethal effect by high toxicity. From these findings, the severe in vivo toxicity of liposomal ZOL limited its utility for in vivo TAM targeting, although FL-ZOL could selectively induce in vitro cytotoxicity via FR.