Active halogen compounds and proteinaceous material: Loss of activity of topical anti-infectives by halogen consumption

Abstract

Objectives The activity of oxidants, such as halogens and active halogen compounds, decreases generally in the presence of proteinaceous material. A quantification of consumption effects was performed to judge the suitability of different representatives as antiseptics and their compatibility with pharmaceutical additives. Methods An iodometric approach served to assess the temporal loss of oxidation capacity in the presence of peptone and fetal calf serum (FCS). The tested agents comprised active halogen compounds, well-known and in particular novel chloramine-based agents indicated for the topical treatment of infections. Key findings The decrease in oxidation capacity was higher in the presence of FCS than of peptone and correlated with the reactivity of the oxidants in both cases. The highest consumption rates were for active bromine compounds followed by hypochlorous acid and heterocyclic chlorimides, such as dichloro-isocyanuric acid, while N-chlorotaurine and related amine-based analogues were least consumed. The pH dependence was only remarkable for chloramine T. Conclusions The observed consumption effects are the result of the differing oxidizing (chlorinating) potencies. Since consumption and irritation are founded on the very same reactions, representatives with low reactivity (N-chloro amino acids) are regarded as more tolerable and retain more oxidative capacity, which provides a more sustained antimicrobial activity. © 2012 Royal Pharmaceutical Society.