Pharmacokinetics and antineoplastic effect of adriamycin (ADM) entrapped in multilamellar vesicles of liposomes composed of egg phosphatidylcholine (PC), cholesterol (Chol), and cholesterol sulfate (CholSO
4) in a molar ratio of 6:3:1 were studied. Upon its intravenous injection, the blood level of ADM remained higher for 24h than that of ADM entrapped in liposomes composed of PC, Chol, and sulfatide (CSE) in a molar ratio of 5:4:1 and than that of free ADM. Entrapment of ADM in liposomes containing either CholSO
4 or CSE reduced the concentration of ADM in the heart and kidney compared with free ADM. In the liver, however, the level of ADM, when the drug entrapped in CholSO
4-containing liposomes was injected, was similar to that of ADM injected in free form, while the drug markedly accumulated in this organ, when ADM was entrapped in CSE-containing liposomes. By using P388 leukemia of mice, we demonstrated that ADM entrapped in CholSO
4-containing liposomes has higher antineoplastic activity than free ADM.
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