In Vitro and In Vivo Trypanocidal Activity of H(2)bdtc-Loaded Solid Lipid Nanoparticles

Autor(es)

Carneiro, Zumira A. ^[1] ; Maia, Pedro I. da S. ^[2] ; Sesti-Costa, Renata ^[3] ; Lopes, Carla D. ^[4] ; Pereira, Tatiana A. ^[5] ; Milanezi, Cristiane M. ^[6] ; da Silva, Marcelo A. Pereira ^[7] ; Lopez, Renata F. V. ^[8] ; Silva, Joao S. ^[9] ; Deflon, Victor M. ^[10]

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo. Fac Ciencias Farmaceut Ribeirao Preto

^[2] Univ Sao Paulo. Inst Quim Sao Carlos

^[3] Univ Sao Paulo. Sch Med

^[4] Univ Sao Paulo. Sch Med

^[5] Univ Sao Paulo. Fac Ciencias Farmaceut Ribeirao Preto

^[6] Univ Sao Paulo. Sch Med

^[7] Univ Sao Paulo. Inst Fis Sao Carlos

^[8] Univ Sao Paulo. Fac Ciencias Farmaceut Ribeirao Preto

^[9] Univ Sao Paulo. Sch Med

^[10] Univ Sao Paulo. Inst Quim Sao Carlos

• Tipo de documento: Artigo Científico
• Fonte: PLoS Neglected Tropical Diseases; v. 8, n. 5 MAY 2014.
• Citações Web of Science: 1

Resumo

The parasite Trypanosoma cruzi causes Chagas disease, which remains a serious public health concern and continues to victimize thousands of people, primarily in the poorest regions of Latin America. In the search for new therapeutic drugs against T. cruzi, here we have evaluated both the in vitro and the in vivo activity of 5-hydroxy-3-methyl-5-phenyl-pyrazoline-1-(S-benzyl dithiocarbazate) (H(2)bdtc) as a free compound or encapsulated into solid lipid nanoparticles (SLN); we compared the results with those achieved by using the currently employed drug, benznidazole. H(2)bdtc encapsulated into solid lipid nanoparticles (a) effectively reduced parasitemia in mice at concentrations 100 times lower than that normally employed for benznidazole (clinically applied at a concentration of 400 mu mol kg(-1) day(-1)); (b) diminished inflammation and lesions of the liver and heart; and (c) resulted in 100% survival of mice infected with T. cruzi. Therefore, H(2)bdtc is a potent trypanocidal agent. (AU)

• Processo FAPESP: 10/20610-0 - "Avaliação de atividade tripanocida in vitro e in vivo do composto 5-hidroxi-3-metil-5-fenil-pirazolina-1-(S-benzilditiocarbazato) em meio aquoso e em sistema de liberação de droga."
• Beneficiário: Zumira Aparecida Carneiro
• Linha de fomento: Bolsas no Brasil - Doutorado