Liposomes Prepared from Synthetic Amphiphiles. II. : Their Interaction with Ehrlich Ascites Tumor Cells and Tissue Distribution in Ehrlich Solid Tumor-Bearing Mice

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The interaction of ^<99m>Tc-labeled liposomes prepared from synthetic amphiphiles containing amino acid residues with Ehrlich ascites tumor cells in vitro and their tissue distribution in Ehrlich solid tumor-bearing mice were investigated. The amphiphiles used were N, N-didodecyl-N^a-[6-(trimethylammonio)hexanoyl]-L-alaninamide bromide (N^+C_5Ala2C_<12>), N, N-didodecyl-N^a-{6-[dimethyl(2-carboxyethyl)ammonio]hexanoyl}-L-alaninamide bromide (CAC_2N^+C_5Ala2C_<12>) and S-{1-carboxy-2-([2,3-bis(hexadecyloxy)propoxy]carbonyl)ethyl}homocysteine (HcyM^-G2C_<16>). Most of the radioactivity of N^+C_5Ala2C_<12> and CAC_2N^+C_5Ala2C_<12> liposomes was firmly bound to Ehrlich ascites tumor cells in vitro. On the other hand, the accumulation of three ^<99m>Tc-labeled liposomes in the tumor of Ehrlich solid tumor-bearing mice was low (about 1% dose per gram of tissue), and most of the liposomes were taken up highly in the liver and spleen of the tumor-bearing mice. However, the radioactivity of the liposomes in the tumor, especially that of N^+C_5Ala2C_<12> and CAC_2N^+C_5Ala2C_<12> liposomes, decreased more slowly with time than in the liver in up to 24 h after injection, suggesting that these liposomes were hard to separate from the tumor cells.
公益社団法人日本薬学会の論文
1990-10-25