New lipid formulation of octenidine dihydrochloride

Abstract

Octenidine dihydrochloride is an effective antiseptic compound which mode of action is based on destabilization plasma membrane of microorganisms. This ensures that microorganisms cannot develop the drug resistance in a straightforward way, as the entire cellular structure, rather than specific molecular target is affected. Since the octenidine is a hydrophobic compound, it requires organic solvent such as phenoxyethanol in order to be effectively administered. However, the presence of phenoxyethanol has strong irritating effect, particularly when applied on open wounds and mucous membranes. Phospholipids are known as neutral excipients free of side effects and in their aggregated form may serve as solvent for octenidine. In this article, we propose a new antiseptic formulation composed of equimolar ratio of lipids and octenidine. The resulting particles are ∼4 nm in diameter showing that their topology is different from that known for liposomes. The new formulation has proven to be equally effective as octenidine dihydrochloride formulation marketed under the name of Octenisept®. The main advantage of the new formulation is that it does not contain phenoxyethanol, which opens new possibilities for broader application spectrum of octenidine, including treatments of mucous membranes and open wounds.

Keywords: Octenidine dihydrochloride; antiseptics; lipid aggregate; particulate antiseptics; phenoxyethanol.