Inhibition of tumor cell growthin vitroandin vivoby 2‐methyl 9‐hydroxyellipticinium entrapped within phospholipid vesicles

摘要

AbstractEncapsulation in liposomes of the antitumoral drug 2‐methyl 9‐hydroxyellipticinium and the consequences of its cytoxicityin vitroon L1210 leukemia cells and on its antitumoral activityin vivoon leukemic mice inoculated with L1210 cells are described. Provided the drugs is dissolved in the buffer below its critical micelle concentration (10−4M), it can be encapsulated in lipid vesicles with a very good yield in the form of a very stable combination with the lipids. Thein vitroexperiments show that 2‐CH39‐OH‐ellipticinium is less cytotoxic against L1210 cells when entrapped than when free in solution. Thein vivoexperiments on tumor‐bearing mice show that encapsulation of the drug reduces its toxicity. Encapsulation maintains the antitumoral activity of the drug or increases it if the leukemia is delayed (104cells injected per mouse instead of 105cel