Micellar Delivery System for Dequalinium—A Lipophilic Cationic Drug with Anticarcinoma Activity

Abstract

Delocalized lipophilic cations (DLC) such as dequalinium (DQA) comprise a novel class of antitumor agents. They are more selectively toxic to carcinoma cells in comparison to non-transformed epithelial cells. In addition, DLC’s have also been shown to enhance the efficacy of existing anticancer modalities such as radiation and photodynamic therapies. A severe drawback of these attractive novel anticancer agents is their limited solubility in aqueous solutions. To overcome this obstacle, we tried to incorporate DQA into liposomes and micelles. We found that incorporation in liposomes does not seem to be possible at physiological salt concentrations. However, we succeeded in preparing micelles made of polyethylene glycol derivatives of phosphatidy-lethanolamine (PEG-PE) which stably bind up to 30 mol % DQA.

Keywords::

• Micelles
• Liposomes
• Drug Carriers
• Dequalinium
• Bolaamphiphiles