Liposomes as Carrier of Methyl-GAG

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.