Long term improvement in the treatment of canine leishmaniosis using an antimony liposomal formulation

Vet Parasitol. 2001 May 9;97(1):15-21. doi: 10.1016/s0304-4017(01)00389-2.

Abstract

Pharmacokinetic and clinical effectiveness of liposome-encapsulated N-methylglucamine antimoniate (LMA) was performed in dogs suffering from experimental leishmaniosis. LMA was compared with N-methylglucamine antimoniate (MGA), the same drug in its free form. Sb plasma concentrations for LMA were always higher than those for MGA. Mean residence time (MRT), half-life time (t(1/2)) and clearance (Cl) showed that Sb was eliminated slower after liposome administration. The high volume of distribution (Vd) obtained with LMA suggests that Sb could achieve therapeutic concentrations in parasite-infected tissues. Average plasma concentration at steady state (Css(ave)) shows that Sb body concentrations after LMA treatment (9.8 mg/kg Sb, each 24h) would be effective in Leishmania infantum canine infection. Comparing LMA with MGA in a 1-year follow-up we observed no relapses for LMA and total protein and gammaglobulin concentrations were within normal range, while for MGA both began to rise 3 months after treatment. Use of antimonial liposomal formulations may restore effectiveness to an existing drug and reduce toxicity.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimony / administration & dosage
  • Antimony / pharmacokinetics
  • Antimony / therapeutic use*
  • Delayed-Action Preparations
  • Dog Diseases / drug therapy*
  • Dogs
  • Leishmaniasis / drug therapy
  • Leishmaniasis / veterinary*
  • Liposomes*
  • Male

Substances

  • Delayed-Action Preparations
  • Liposomes
  • Antimony