INIFTA   05425
INSTITUTO DE INVESTIGACIONES FISICO-QUIMICAS TEORICAS Y APLICADAS
Unidad Ejecutora - UE
artículos
Título:
Nanomolar cationic dendrimeric sulfadiazine as potential antitoxoplasmic agent
Autor/es:
M. J. PRIETO; D. BACIGALUPE; O.R. PARDINI; AMALVY, J.I.; VENTURINI, C.; M. J. MORILLA; E. L. ROMERO
Revista:
International Journal of Pharmaceutics
Referencias:
Año: 2006 p. 160 - 168
ISSN:
0378-5173
Resumen:
The high doses of sulfadiazine (SDZ), used in synergistic combination with pyrimethamine, are mainly responsible for severe side effects
and discontinuation of toxoplasmosis treatments. In the search for new strategies that improve the efficacy of treatments with reduced doses of
SDZ, we have determined the performance of cationic G4 (DG4) and anionic G4.5 (DG4.5) poly(amidoamine) (PAMAM) dendrimers to act as
SDZ nanocarriers. Both dendrimers could efficiently load SDZ (SDZDG4 and SDZDG4.5) up to a ratio of 30 molecules SDZ per dendrimer
molecule. The MTT assay on Vero and J774 cells showed no cytotoxicity for DG4.5 and its SDZ complex incubated between 0.03 and 33 M of
dendrimer concentration. On the other hand, DG4 and its SDZ complex resulted cytotoxic when incubated at dendrimer concentrations higher than
3.3M. Finally, complexes and empty dendrimers were in vitro tested against Vero cells infected with RH strain of Toxoplasma gondii along 4 h of
treatment. For SDZDG4.5 and DG4.5 to cause an infection decrease between 25 and 40%, respectively, a dendrimer concentration of 33 Mwas
required; however, SDZDG4 produced the highest infection decrease of 60% at 0.03 M. These preliminary results, achieved with nanomolar
doses of SDZDG4 as unique active principle, point to this complex as a suitable potential candidate for antitoxoplasmic therapy.
© 2006 Elsevier B.V. All rights reserved
treatment. For SDZDG4.5 and DG4.5 to cause an infection decrease between 25 and 40%, respectively, a dendrimer concentration of 33 Mwas
required; however, SDZDG4 produced the highest infection decrease of 60% at 0.03 M. These preliminary results, achieved with nanomolar
doses of SDZDG4 as unique active principle, point to this complex as a suitable potential candidate for antitoxoplasmic therapy.
© 2006 Elsevier B.V. All rights reserved
in vitro tested against Vero cells infected with RH strain of Toxoplasma gondii along 4 h of
treatment. For SDZDG4.5 and DG4.5 to cause an infection decrease between 25 and 40%, respectively, a dendrimer concentration of 33 Mwas
required; however, SDZDG4 produced the highest infection decrease of 60% at 0.03 M. These preliminary results, achieved with nanomolar
doses of SDZDG4 as unique active principle, point to this complex as a suitable potential candidate for antitoxoplasmic therapy.
© 2006 Elsevier B.V. All rights reserved