EFFECTS OF ADMINISTERED ROUTE ON TISSUE DISTRIBUTION AND ANTITUMOR-ACTIVITY OF POLYETHYLENEGLYCOL-COATED LIPOSOMES CONTAINING ADRIAMYCIN

Tissue distribution, antitumor activity and side effects after intrape ritoneal administration of polyethyleneglycol-coated liposomes contain ing adriamycin (PEG-LADR) were examined and compared to that after int ravenous treatment. Plain liposomes (PLADR) and PEG-LADR appeared to m aintain blood circulation by intraperitoneal injection and suggested u sefulness in passive targeting. Because of the accumulation of ADR in the pancreas found after intraperitoneal treatment, this administered route of PLADR and PEG-LADR was expected to be useful as a method of t argeting the pancreas. The side effects of ADR in the heart and liver were suppressed by the liposomalization and PEG-modification. The anti tumor effect of ADR was increased by the liposomalization, and PEG-mod ification after intraperitoneal administration was superior to that af ter intravenous administration. The slowly disappearing pattern of PLA DR and PEG-LADR from the abdominal cavity was similar. It is suggested that PLADR and PEG-LADR were absorbed intact from the abdominal cavit y and transferred into the blood circulation. (C) 1997 Elsevier Scienc e Ireland Ltd.