Liposomes as carrier of methyl-GAG. Increased antitumor activity and reduced hypoglycemia in mice.
The encapsulation efficiency and the leakage on storage of various types of liposomes prepared from different lipid compositions containing the anticancer drug methyl-GAG (methylglyoxal-bis-guanylhydrazone) were investigated. Treatment with methyl-GAG in a q.d. 1-4 schedule resulted in the murine leukemias P 388 and L 1210 (i.v.) in nearly the same increase in life span as the corresponding dose in liposomes. In a q.d. 1, 3 schedule methyl-GAG containing liposomes revealed comparable effects as the 4-day treatment with the free drug. The hypoglycemic effect of 80 mg/kg methyl-GAG, q.d. 1-4, could be normalized when the drug was administered in reverse-phase evaporation vesicles. We conclude that the liposomal encapsulation of methyl-GAG leads to a depot effect with a slight relief of toxicity.
D000818:Animals; D005260:Female; D007003:Hypoglycemia / Q000139:chemically induced* / Q000517:prevention & control; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D008081:Liposomes / Q000008:administration & dosage*; D008175:Lung Neoplasms / Q000188:drug therapy*; D051379:Mice; D008810:Mice, Inbred C57BL; D008811:Mice, Inbred DBA; D008935:Mitoguazone / Q000008:administration & dosage / Q000627:therapeutic use* / Q000633:toxicity; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D013997:Time Factors
D008081:Liposomes; D008935:Mitoguazone