title: Liposomes as carrier of methyl-GAG. Increased antitumor activity and reduced hypoglycemia in mice.
abstract: 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.
mesh_terms: 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
chemical_list: D008081:Liposomes; D008935:Mitoguazone