Diminazene aceturate-sodium oleate complex for the treatment of trypanosomiasis in animal models

Abstract

The aim of this study is to improve the efficacy of diminazene aceturate via complex formation with sodium oleate. The complex was subjected to various in vitro and in vivo tests to assess its properties, toxicity and efficacy against Trypanosoma brucei brucei infections in comparison to pure drug. Results revealed that the complex was four times more lipophilic than the pure drug and the LD₅₀ is > 5000 mg/kg. FTIR results showed that the functional groups in the pure drug were retained in the complex and that the complexation was via hydrogen bonding between the amino group of the pure drug and the oleic moiety of sodium oleate. There was no significant increase in the serum levels of hepatic enzymes or reduction in haematological indices upon administration of the complex or pure drugto mice as compared to their states before treatment. The complex was many times more active than the pure drug onin vitro cultures of T. bruceibrucei and it was still active in vivo. Thus, complexation of the drug could be a good way of improving its efficacy.

Keywords: diminazene aceturate-sodium oleate complex, properties, toxicity, effectiveness in trypanosomiasis