SAMANTA ETEL TREIGER BORBOREMA

SAMANTA ETEL TREIGER BORBOREMA

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Pharmacokinetics of neutron-irradiated meglumine antimoniate in Leishmania amazonensis-infected BALB/c mice
2019 - BORBOREMA, SAMANTA E.T.; OSSO JUNIOR, JOAO A.; ANDRADE JUNIOR, HEITOR F. de; NASCIMENTO, NANCI do
Background: Cutaneous leishmaniasis (CL) is a parasitic disease caused by the protozoan Leishmania spp. Pentavalent antimonial agents have been used as an effective therapy, despite their side effects and resistant cases. Their pharmacokinetics remain largely unexplored. This study aimed to investigate the pharmacokinetic profile of meglumine antimoniate in a murine model of cutaneous leishmaniasis using a radiotracer approach. Methods: Meglumine antimoniate was neutron-irradiated inside a nuclear reactor and was administered once intraperitoneally to uninfected and L. amazonensis-infected BALB/c mice. Different organs and tissues were collected and the total antimony was measured. Results: Higher antimony levels were found in infected than uninfected footpad (0.29% IA vs. 0.14% IA, p = 0.0057) and maintained the concentration. The animals accumulated and retained antimony in the liver, which cleared slowly. The kidney and intestinal uptake data support the hypothesis that antimony has two elimination pathways, first through renal excretion, followed by biliary excretion. Both processes demonstrated a biphasic elimination profile classified as fast and slow. In the blood, antimony followed a biexponential open model. Infected mice showed a lower maximum concentration (6.2% IA/mL vs. 11.8% IA/mL, p = 0.0001), a 2.5-fold smaller area under the curve, a 2.7-fold reduction in the mean residence time, and a 2.5-fold higher clearance rate when compared to the uninfected mice. Conclusions: neutron-irradiated meglumine antimoniate concentrates in infected footpad, while the infection affects antimony pharmacokinetics.
Pharmacokinetic of meglumine antimoniate encapsulated in phosphatidylserine-liposomes in mice model
2018 - BORBOREMA, SAMANTA E.T.; OSSO JUNIOR, JOAO A.; TEMPONE, ANDRE G.; ANDRADE JUNIOR, HEITOR F. de; NASCIMENTO, NANCI do
Visceral leishmaniasis (VL) is a fatal parasitic disease caused by the protozoan Leishmania spp. Meglumine antimoniate (MA) is the main treatment and has demonstrated a promising efficacy in a VL-model when encapsulated into negatively charged liposomes. Considering the current concept for the evaluation of pharmacokinetic parameters at early phases of drug discovery, we developed a formulation of MA-encapsulated into phosphatidylserine liposomes (MA-LP) and analyzed the in vitro antileishmanial activity, physicochemical properties, and pharmacokinetic profile in a mice model. The liposomal formulation had an internal mean diameter of 114 nm and a high stability in plasma. MA-LP was 23-fold more in vitro effective against Leishmania infantum-infected macrophages than the free drug, with a selectivity index higher than 220. The pharmacokinetic studies demonstrated that the liposomes increased the uptake of the drug by the liver and spleen and promoted sustained levels. MA-LP was first eliminated through renal excretion, followed by biliary excretion. In the blood, MA-LP followed a biexponential open model. This work emphasizes the importance of liposomes as potential drug delivery systems for visceral leishmaniasis.
Antimonial drugs entrapped into phosphatidylserine liposomes: physicochemical evaluation and antileishmanial activity
2016 - BORBOREMA, SAMANTA E.T.; OSSO JUNIOR, JOAO A.; ANDRADE JUNIOR, HEITOR F. de; NASCIMENTO, NANCI do
Synthesis and antieshmanial activities of novel 3 substituted quinolines
2005 - TEMPONE, ANDRE G.; SILVA, ANA C.M.P.; BRANDT, CARLOS A.; MARTINEZ, FERNANDA S.; BORBOREMA, SAMANTA E.T.; SILVEIRA, MARIA A.B.; ANDRADE JUNIOR, HEITOR F.
Uptake and antileishmanial activity of meglumine antimoniate-containing liposomes in Leishmania (leishmania) major-infected macrophages
2011 - BORBOREMA, SAMANTA E.T.; SCHWENDENER, RETO A.; OSSO JUNIOR, JOAO A.; ANDRADE JUNIOR, HEITOR F. de; NASCIMENTO, NANCI
Biodistribution of meglumine antimoniate in healthy and Leichmania (Leishmania) infantum chagasi-infected BALB/c mice
2013 - BORBOREMA, SAMANTA E.T.; OSSO JUNIOR, JOAO A.; ANDRADE JUNIOR, HEITOR F. de; NASCIMENTO, NANCI do