[A liposomal form of diamidine: reduced toxicity].

The research article focusses on the use of liposomal form of diamidine in the treatment of nuttaliosis in horses, emphasizing on its reduced toxicity as compared to free diamidine.

Objective of the research

• This research evaluates the use of liposomal forms of diamidine in treating nuttaliosis in horses induced by Nuttalia eque cultures.

Methodology

• The diamidine used here is an analog of imidocarb or imidozoline, and it was encapsulated in liposomes.
• The liposomes were prepared using a modified version of the phase inversion method, with lipids dissolved in a combination of freon-11 and chloroform.
• Gas liquid chromatography revealed that the presence of organic solvents in the preparation was less than 0.2%, showing significant purity in the encapsulation.
• The primary fraction of the liposome preparation consisted of particles ranging between 1.5 to 2.5 microns in size.

Observations and Results

• Tests were carried on animals of various species to understand the toxicity of the liposome-encapsulated diamidine.
• It was found that this encapsulated version had significantly reduced toxicity compared to using free diamidine in treatment.
• The lethal dose (LD50) – the dose that would kill 50% of the test population – for intravenous and intramuscular administration was found to be 52 and 6000 mg/kg for the encapsulated diamidine. In contrast, free diamidine’s LD50 was found to be much lower at 0.8 and 84 mg/kg, respectively.
• Additionally, in horses, intramuscular delivery of the encapsulated diamidine did not lead to death even at doses of 10mg/kg, whereas the same dose of free diamidine led to 100% fatality.

Conclusion

• The liposome-encapsulated diamidine demonstrated no adverse impact on the liver’s antitoxic and metabolic capabilities, further supporting the decreased toxicity findings.
• The researchers concluded with a hopeful note that the significantly lower toxicity of the encapsulated version could potentially lead to a higher chemotherapeutic index, providing a safer and more effective treatment for nuttaliosis in horses and other Nuttalia carriers.