A new medium-throughput screening design approach for the development of hydroxymethylnitrofurazone (NFOH) nanostructured lipid carrier for treating leishmaniasis.

Hydroxymethilnitrofurazone (NFOH) is a nitrofurazone derivative and has potential use in treating leishmaniasis. However, due to low water solubility and bioavailability, NFOH has failed in in vivo tests. Nanostructured lipid carrier (NLC) is an alternative to overcome these limitations by improving pharmacokinetics and modifying drug delivery. This work is focused on developing a novel NFOH-loaded NLC (NLC-NFOH) using a D-optimal mixture statistical design and high-pressure homogenization, for oral administration to treat leishmaniasis. The optimized NLC-NFOH consisted of Mygliol® 840, Gelucire® 50/13, and Precirol® ATO 5 as lipids. These lipids were selected using a rapid methodology Technobis Crystal 16 T M, microscopy, and DSC. Different tools for selecting lipids provided relevant scientific knowledge for the development of the NLC. NLC-NFOH presented a z-average of 198.6 ±â€¯5.4 nm, PDI of 0.11 ±â€¯0.01, and zeta potential of -13.7 ±â€¯0.7 mV. A preliminary in vivo assay was performed by oral administration of NLC-NFOH (2.8 mg/kg) in one healthy male Wistar rat (341 g) by gavage. Blood from the carotid vein was collected, and the sample was analyzed by HPLC. The plasma concentration of NFOH after 5 h of oral administration was 0.22 µg/mL. This same concentration was previously found using free NFOH in the DMSO solution (200 mg/kg), which is an almost 100-fold higher dose. This study allowed a design space development approach of the first NLC-NFOH with the potential to treat leishmaniasis orally.

Estudo da interação entre células endoteliais humanas e biomateriais utilizados em cirurgia buco-maxilo-facial / Interaction of human endothelial cells with biomaterials applied on maxillo-facial surgery

Neste estudo procuramos analisar a interação entre células endoteliais humanas e biomateriais utilizados em cirurgia oral, através de análises histológicas e ensaios imunocitoquímicos. Culturas primárias foram isoladas de veias de cordões umbilicais humanos. As células foram semeadas, em densidade determinada, sobre secções circulares de membrana colágena, placas de titânio e controles; foram mantidas por 1, 7 ou 14 dias. As células proliferaram, atingiram confluência e após 14 dias formaram camada plana e uniforme. Os resultados demonstraram que os materiais estudados permitem a proliferação e a adesão das células endoteliais. Esta adesão é mediada pela interação de integrinas e proteínas.With the present investigation, we examined the behavior of endothelial cells on two different biomaterials, using histological and immunocitochemical methods. The endothelial cells were isolated from umbilical cord veins. Cells, after two passages, were seeded in a standard density on a collagen membrane, on commercially pure titanium in the form of plates and on control surfaces. Then these were maintained for 1, 7 or 14 days. After 14 days, we could observe a confluent monolayer of cells. Our results showed that both studied materials support endothelial cells growth and attachment and this is most related to the binding through integrins and proteins...