Abstract
A series of poly(maleic anhydride-alt-vinyl acetate) conjugates with alkylating agents were evaluated regarding antitumoral activity, biodistribution and organotropic effects. The synthesized conjugates exhibits a significant antitumoral activity expressed as ATR (average tumor retention). In addition the obtained macromolecular compounds show a prolonged half-life in sanguine serum and accumulation in tumoral tissue. The last effect is supposed to be enhanced by EPR (enhanced permeation and retention) effect. The analyzed compounds also exhibit some organotropic effects such as the increase of liver, spleen and kidney weight. The LD50 values of the alkylating agents and conjugated ones proved that the coupling reaction decrease the intrinsic toxicity of the alkylating agents. Keywords: poly(maleic anhydride-alt-vinyl acetate), antitumoral activity, EPR effect