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Protein Precoating Of Polylactide Microspheres Containing A Lipophilic Immunopotentiator For Enhancement Of Macrophage Phagocytosis And Activation

Y. Tabata, Y. Ikada
Published 2004 · Chemistry, Medicine

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Biodegradable microspheres containing a lipophilic muramyl dipeptide, MDP-B30, were prepared from a L-lactic acid–glycolic acid copolymer. The effect of precoating the microspheres with water-soluble polymers including proteins on the antitumor activity of mouse peritoneal macrophages (Mφ) was investigated. Macrophages activated by phagocytosis of the microspheres exhibited growth inhibitory activity toward Meth-A tumor cells. The activity correlated with the extent of Mφ phagocytosis of the microspheres. Mφ phagocytosis was greatly augmented by gelatin precoating of the microspheres, resulting in a significant increase of in vitro antitumor activity of Mφ by the microspheres. However, potentiation of Mφ activity by gelatin precoating was minimal after intraperitoneal injection of the microspheres, but cross-linking of the coated gelatin with glutaraldehyde afforded potentiation of the antitumor activity in vivo.
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