PLGA nanoparticles loaded with a new thiourea derivative: development, characterization and in vitro evaluation against Leishmania amazonensis

Leishmaniasis is a disease caused by protozoa of the genus Leishmania1. Current treatments are restricted to drugs that display side effects and potential for parasites to develop resistance2. The thiourea (LabTIF13) showed promising in vitro performance against Leishmania amazonensis3. To formulate LabTIF13 for oral administration, it was encapsulated into nanoparticles (NPs) to provide vectorizaded drug delivery4. NPs containing LabTIF13 were obtained through a nanoprecipitation methodology associated with solvent evaporation. They were characterized for particle size, zeta potential, encapsulation efficiency(EE%) and yield(%w/w). The in vitro antileishmanial activity of NPs was determined in the promastigotes and amastigotes of L. amazonensis and the cytotoxicity on macrophages of mice BALB/c. The results suggests that LabTIF13-NPs are sphericals, monodispersed with mean diameter <200nm and exhibited negative zeta potential (-30mV). They were obtained with higher yields (87%w/w) and %EE ranging from 30%w/w. NPs with LabTIF 13 showed an improved leishmanicidal activity (IC50=0.90±0.57µg/mL) with low cytotoxicity (CC50>100µg/mL).