J Vet Sci.  2011 Dec;12(4):303-307. 10.4142/jvs.2011.12.4.303.

Biodynamic parameters of micellar diminazene in sheep erythrocytes and blood plasma

• Staroverov SA
• Sidorkin V
• Fomin AS
• Shchyogolev SY
• Dykman LA

• KMID: 1365012
• DOI: http://doi.org/10.4142/jvs.2011.12.4.303

Abstract

In this work, we used a preparation of diminazene, which belongs to the group of aromatic diamidines. This compound acts on the causative agents of blood protozoan diseases produced by both flagellated protozoa (Trypanosoma) and members of the class Piroplasmida (Babesia, Theileria, and Cytauxzoon) in various domestic and wild animals, and it is widely used in veterinary medicine. We examined the behavior of water-disperse diminazene (immobilized in Tween 80 micelles) at the cellular and organismal levels. We assessed the interaction of an aqueous and a water-disperse preparation with cells of the reticuloendothelial system. We compared the kinetic parameters of aqueous and water-disperse diminazene in sheep erythrocytes and plasma. The therapeutic properties of these two preparations were also compared. We found that the surface-active substances improved intracellular penetration of the active substance through interaction with the cell membrane. In sheep blood erythrocytes, micellar diminazene accumulated more than its aqueous analog. This form was also more effective therapeutically than the aqueous analog. Our findings demonstrate that use of micellar diminazene allows the injection dose to be reduced by 30%.

Keyword

babesia; biodynamic; diminazene; kinetic; micelles

MeSH Terms

Animals
Babesiosis/drug therapy/veterinary
Diminazene/metabolism/*pharmacokinetics
Dose-Response Relationship, Drug
Female
Macrophages, Peritoneal/cytology/metabolism
Male
Micelles
Polysorbates
Rats
Sheep/*blood
Sheep Diseases/drug therapy
Trypanocidal Agents/*pharmacokinetics

Figure

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  Fig. 1 Rat peritoneal cells cultured with FITC-labeled SAS micelles (green). ×400.

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  Fig. 2 Rat peritoneal cells cultured in the presence of micellar diminazene. ×400.

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  Fig. 3 Rat peritoneal cells cultured in the presence of aqueous diminazene. ×400.

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  Fig. 4 Kinetic parameters of intramuscularly injected aqueous and micellar diminazene in sheep plasma.

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  Fig. 5 Kinetic parameters of intramuscularly injected aqueous and micellar diminazene in sheep blood erythrocytes.

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