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Protein Precoating of Polylactide Microspheres Containing a Lipophilic Immunopotentiator for Enhancement of Macrophage Phagocytosis and Activation

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Abstract

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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Tabata, Y., Ikada, Y. Protein Precoating of Polylactide Microspheres Containing a Lipophilic Immunopotentiator for Enhancement of Macrophage Phagocytosis and Activation. Pharm Res 6, 296–301 (1989). https://doi.org/10.1023/A:1015942306801

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  • DOI: https://doi.org/10.1023/A:1015942306801

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