Liposomes prepared from synthetic amphiphiles. II. Their interaction with Ehrlich ascites tumor cells and tissue distribution in Ehrlich solid tumor-bearing mice.
The interaction of 99mTc-labeled liposomes prepared from synthetic amphiphiles containing amino acid residues with Ehrlich ascites tumor cells in vitro and their tissue distributions in Ehrlich solid tumor-bearing mice were investigated. The amphiphiles used were N,N-didodecyl-N alpha-[6-(trimethylammonio)hexanoyl]-L-alaninamide bromide N+C5Ala2C12), N,N-didodecyl-N alpha-(6-[dimethyl(2-carboxyethyl)ammonio]hexanoyl)-L- alaninamide bromide (CAC2N+C5Ala2C12) and S-[1-carboxy-2- ([2,3-bis(hexadecyloxy)propoxy]carbonyl)ethyl]homocysteine (HcyM-G2C1 6). Most of the radioactivity of N+C5Ala2C12 and CAC2N+C5Ala2C12 liposomes was firmly bound to Ehrlich ascites tumor cells in vitro. On the other hand, the accumulation of three 99mTc-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+C5Ala2C12 and CAC2N+C5Ala2C12 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.
Goto
R
R
Department of Radiobiochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Japan.
Kubo
H
H
Daicho
Y
Y
Okada
S
S
D000818:Animals; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism*; D008081:Liposomes / Q000493:pharmacokinetics*; D051379:Mice; D008815:Mice, Inbred Strains; D004369:Pentetic Acid; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured / Q000378:metabolism
D008081:Liposomes; D004369:Pentetic Acid