Avaliação da eficácia e farmacocinética de nanocápsulas poliméricas de quinina em ratos infectados com plasmodium berghei

摘要: Efficacy and pharmacokinetics of polymeric nanoparticles containing quinine in Plamodium berghei infected rats Objectives: The aims this study were to develop characterize nanocapsules (NC) (QN) evaluate their efficacy vivo as well the pharmacokinetic profile nanoencapsulated drug. Methodology: NC-QN prepared by nanoprecipitation with different drug concentration 2 (NC2QN), 3 (NC3-QN) 4 mg/mL (NC4-QN). All formulations characterized terms encapsulation efficacy, loading, zeta potential, particle size, polydispersion index, pH. stability suspensions evaluated during 30 days. An experimental malaria model Plasmodium was used Wistar rats. Different doses tested for each formulation. evaluation performed dose NC–QN which presented 100 % model. NC2-QN or QN free administrated i.v. route (25 mg/kg) health Blood samples collected at pre-determinated time points quantified an HPLC validated method. Animal protocols approved UFRGS Ethics Research Committee (# 2005477). Results discussion: adequate monodisperse population, negative content efficiency higher than 90 %. formulation (75 mg/kg/day) q8h daily 7-9 days post-infection cured all For NC2-QN, 60 mg/kg/day, q8h, 28.6 85.7 survival observed, respectively. significant decrease t1⁄2 compared (32.9 ± 8.9 min 69.8 44.6 min, respectively), (α = 0,05). This occurs due tendency increase CLtotal (7.1 3.3 9.9 2.1 L/h/kg, respectively). increased encapsulated group. Conclusion: Nanoencapsulation reduced effective animals. Theses results indicate that is a potential strategy be investigated treatment. KEY-WORDS: quinine, nanocapsules, antimalarial berghei, pharmacokinetics.