MICELLAR DELIVERY SYSTEM FOR DEQUALINIUM - A LIPOPHILIC CATIONIC DRUGWITH ANTICARCINOMA ACTIVITY

Delocalized lipophilic cations (DLC) such as dequalinium (DQA) compris e a novel class of antitumor agents. They are more selectively toxic t o carcinoma cells in comparison to non-transformed epithelial cells. I n addition, DLC's have also been shown to enhance the efficacy of exis ting anticancer modalities such as radiation and photodynamic therapie s. A severe drawback of these attractive novel anticancer agents is th eir limited solubility in aqueous solutions. To overcome this obstacle , we tried to incorporate DQA into liposomes and micelles. We found th at incorporation in liposomes does not seem to be possible at physiolo gical salt concentrations. However, we succeeded in preparing micelles made of polyethylene glycol derivatives of phosphatidylethanolamine ( PEG-PE) which stably bind up to 30 mol % DQA.