Liposomes produced by reverse phase evaporation: in vitro and in vivo efficacy of diminazene aceturate against Trypanosoma evansi.
This study aimed to develop and test the in vitro and in vivo effectiveness of diminazene aceturate encapsulated into liposomes (L-DMZ) on Trypanosoma evansi. To validate the in vitro tests with L-DMZ, the efficacy of a commercial formulation of diminazene aceturate (C-DMZ) was also assessed. The tests were carried out in culture medium for T. evansi, at concentrations of 0.25, 0.5, 1, 2 and 3 μg mL(-1) of L-DMZ and C-DMZ. A dose-dependent effect was observed for both formulations (L-DMZ and C-DMZ), with the highest dose-dependent mortality of trypomastigotes being observed at 1 and 3 h after the onset of tests with L-DMZ. The results of in vivo tests showed the same effects in the animals treated with L-DMZ and C-DMZ in single doses of 3.5 mg kg(-1) and for 5 consecutive days (3.5 mg kg(-1) day(-1)). It was possible to conclude that T. evansi showed greater in vitro susceptibility to L-DMZ when compared with C-DMZ. In vivo tests suggest that treatment with the L-DMZ and C-DMZ showed similar efficacy in vivo. The potential of the formulation developed in this study was clearly demonstrated, as it increased the efficacy of the treatment against trypanosomosis, but more studies are needed to increase the effectiveness in vivo.
Department of Microbiology and Parasitology, Universidade Federal de Santa Maria (UFSM), Brazil.
Camila Belmonte
CB
Oliveira
Department of Production and Control of Medicines, Faculty of Pharmacy, Universidade Federal do Rio Grande do Sul, Brazil.
Lucas Almeida
LA
Rigo
Department of Microbiology and Parasitology, Universidade Federal de Santa Maria (UFSM), Brazil.
Luciana Dalla
LD
Rosa
Department of Microbiology and Parasitology, Universidade Federal de Santa Maria (UFSM), Brazil.
Lucas Trevisan
LT
Gressler
Department of Microbiology and Parasitology, Universidade Federal de Santa Maria (UFSM), Brazil.
Carine Eloise Prestes
CE
Zimmermann
Department of Production and Control of Medicines, Faculty of Pharmacy, Universidade Federal do Rio Grande do Sul, Brazil.
Aline Ferreira
AF
Ourique
Department of Animal Science, Universidade do Estado de Santa Catarina - UDESC, Brazil.
Aleksandro Schafer
AS
DA Silva
Department of Animal Production, Universidade do Estado de Santa Catarina, Lages, SC, Brazil.
Luiz C
LC
Miletti
Department of Production and Control of Medicines, Faculty of Pharmacy, Universidade Federal do Rio Grande do Sul, Brazil.
Ruy Carlos Ruver
RC
Beck
Department of Microbiology and Parasitology, Universidade Federal de Santa Maria (UFSM), Brazil.
Silvia Gonzalez
SG
Monteiro
D000818:Animals; D002626:Chemistry, Pharmaceutical; D004133:Diminazene / Q000008:administration & dosage / Q000031:analogs & derivatives; D008081:Liposomes; D008297:Male; D036103:Nanotechnology; D017208:Rats, Wistar; D014344:Trypanocidal Agents / Q000008:administration & dosage*; D014345:Trypanosoma / Q000187:drug effects*; D014352:Trypanosomiasis / Q000188:drug therapy* / Q000469:parasitology
D008081:Liposomes; D014344:Trypanocidal Agents; C003915:diminazene aceturate; D004133:Diminazene