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1.
Antimicrob Agents Chemother ; 68(5): e0091523, 2024 May 02.
Article in English | MEDLINE | ID: mdl-38517190

ABSTRACT

Primaquine is the mainstream antimalarial drug to prevent Plasmodium vivax relapses. However, this drug can induce hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency. Nanostructure formulations of primaquine loaded with D-galactose were used as a strategy to target the drug to the liver and decrease the hemolytic risks. Nanoemulsion (NE-Pq) and nanochitosan (NQ-Pq) formulations of primaquine diphosphate containing D-galactose were prepared and characterized by their physicochemistry properties. Pharmacokinetic and biodistribution studies were conducted using Swiss Webster mice. A single dose of 10 mg/kg of each nanoformulation or free primaquine solution was administered by gavage to the animals, which were killed at 0.5, 1, 2, 4, 8, and 24 hours. Blood samples and tissues were collected, processed, and analyzed by high-performance liquid chromatography. The nanoformulation showed sizes around 200 nm (NE-Pq) and 400 nm (NQ-Pq) and physicochemical stability for over 30 days. Free primaquine solution achieved higher primaquine Cmax in the liver than NE-Pq or NQ-Pq at 0.5 hours. However, the half-life and mean residence time (MRT) of primaquine in the liver were three times higher with the NQ-Pq formulation than with free primaquine, and the volume distribution was four times higher. Conversely, primaquine's half-life, MRT, and volume distribution in the plasma were lower for NQ-Pq than for free primaquine. NE-Pq, on the other hand, accumulated more in the lungs but not in the liver. Galactose-coated primaquine nanochitosan formulation showed increased drug targeting to the liver compared to free primaquine and may represent a promising strategy for a more efficient and safer radical cure for vivax malaria.


Subject(s)
Antimalarials , Chitosan , Galactose , Liver , Primaquine , Primaquine/pharmacokinetics , Primaquine/chemistry , Animals , Mice , Liver/metabolism , Liver/drug effects , Galactose/chemistry , Chitosan/chemistry , Antimalarials/pharmacokinetics , Nanoparticles/chemistry , Tissue Distribution , Nanostructures/chemistry , Male
2.
Sci Rep ; 7(1): 7132, 2017 08 02.
Article in English | MEDLINE | ID: mdl-28769088

ABSTRACT

Electromagnetically induced transparency (EIT) is an optical phenomenon which allows a drastic modification of the optical properties of an atomic system by applying a control field. It has been largely studied in the last decades and nowadays we can find a huge number of experimental and theoretical related studies. Recently a similar phenomenon was also shown in quantum dot molecules (QDM), where the control field is replaced by the tunneling rate between quantum dots. Our results show that in the EIT regime, the optical properties of QDM and the atomic system are identical. However, here we show that in the strong probe field regime, i.e., "coherent population trapping" (CPT) regime, it appears a strong discrepancy on the optical properties of both systems. We show that the origin of such difference relies on the different decay rates of the excited state of the two systems, implying in a strong difference on their higher order nonlinear susceptibilities. Finally, we investigate the optical response of atom/QDM strongly coupled to a cavity mode. In particular, the QDM-cavity system has the advantage of allowing a better narrowing of the width of the dark state resonance in the CPT regime when compared with atom-cavity system.

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