title: Pyrimethamine-loaded lipid-core nanocapsules to improve drug efficacy for the treatment of toxoplasmosis.
abstract: We propose an innovative product based on the nanoencapsulation of pyrimethamine (PYR), aiming an improvement of drug efficacy for the treatment of toxoplasmosis. The in vitro cytotoxicity effect of encapsulated PYR and PYR-colloidal suspension was concomitantly evaluated against LLC-MK2 lineage and mouse peritoneal macrophage showing that the cells had similar tolerance for both PYR encapsulated or in the aqueous suspension. CF1 mice acutely infected with tachyzoites of Toxoplasma gondii RH strain treated with different doses (5.0-10 mg/kg/day) of PYR-nanocapsules had survival rate higher than the animals treated with the same doses of non-encapsulated PYR. Thus, encapsulation of PYR improved the efficacy of this drug against an acute model of toxoplasmosis in mice and can be considered an alternative for reducing the dose of PYR, which, in turn, could also reduce the side effects associated to the treatment.
authors.affiliation: Laboratório de Ultraestrutura Celular Hertha Meyer, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil, k.pissinate@gmail.com.
authors.forename: Kenia
authors.initials: K
authors.lastname: Pissinate
authors.forename: Érica
authors.initials: É
authors.lastname: dos Santos Martins-Duarte
authors.forename: Scheila Rezende
authors.initials: SR
authors.lastname: Schaffazick
authors.forename: Catiúscia Padilha
authors.initials: CP
authors.lastname: de Oliveira
authors.forename: Rossiane Cláudia
authors.initials: RC
authors.lastname: Vommaro
authors.forename: Sílvia Stanisçuaski
authors.initials: SS
authors.lastname: Guterres
authors.forename: Adriana Raffin
authors.initials: AR
authors.lastname: Pohlmann
authors.forename: Wanderley
authors.initials: W
authors.lastname: de Souza
mesh_terms: D000818:Animals; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D003049:Coccidiostats / Q000008:administration & dosage* / Q000627:therapeutic use / Q000633:toxicity; D005260:Female; D008055:Lipids; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000502:physiology; D051379:Mice; D053769:Nanocapsules; D011739:Pyrimethamine / Q000008:administration & dosage* / Q000627:therapeutic use / Q000633:toxicity; D014122:Toxoplasma / Q000187:drug effects*; D014124:Toxoplasmosis, Animal / Q000188:drug therapy* / Q000469:parasitology
chemical_list: D003049:Coccidiostats; D008055:Lipids; D053769:Nanocapsules; D011739:Pyrimethamine