Search results for: Eloísa S. S. Vieira

Authors: Leslie Raphael de M. Ferraz, Salvana Priscylla M. Costa, Tarcyla de A. Gomes, Giovanna Christinne R. M. Schver, Cristóvão R. da Silva, Magaly Andreza M. de Lyra, Danilo Augusto F. Fontes, Larissa A. Rolim, Amanda Carla Q. M. Vieira, Miracy M. de Albuquerque, Pedro J. Rolim-Neto

Abstract:

Efavirenz (EFV) is a drug used as first-line treatment of AIDS. However, it has poor aqueous solubility and wettability, presenting problems in the gastrointestinal tract absorption and bioavailability. One of the most promising strategies to improve the solubility is the use of solid dispersions (SD). Therefore, this study aimed to characterize SD EFZ with the polymers: PVP-K30, PVPVA 64 and SOLUPLUS in order to find an optimal formulation to compose a future pharmaceutical product for AIDS therapy. Initially, Physical Mixtures (PM) and SD with the polymers were obtained containing 10, 20, 50 and 80% of drug (w/w) by the solvent method. The best formulation obtained between the SD was selected by in vitro dissolution test. Finally, the drug-carrier system chosen, in all ratios obtained, were analyzed by the following techniques: Differential Scanning Calorimetry (DSC), polarization microscopy, Scanning Electron Microscopy (SEM) and spectrophotometry of absorption in the region of infrared (IR). From the dissolution profiles of EFV, PM and SD, the values of area Under The Curve (AUC) were calculated. The data showed that the AUC of all PM is greater than the isolated EFV, this result is derived from the hydrophilic properties of the polymers thus favoring a decrease in surface tension between the drug and the dissolution medium. In adittion, this ensures an increasing of wettability of the drug. In parallel, it was found that SD whom had higher AUC values, were those who have the greatest amount of polymer (with only 10% drug). As the amount of drug increases, it was noticed that these results either decrease or are statistically similar. The AUC values of the SD using the three different polymers, followed this decreasing order: SD PVPVA 64-EFV 10% > SD PVP-K30-EFV 10% > SD Soluplus®-EFV 10%. The DSC curves of SD’s did not show the characteristic endothermic event of drug melt process, suggesting that the EFV was converted to its amorphous state. The analysis of polarized light microscopy showed significant birefringence of the PM’s, but this was not observed in films of SD’s, thus suggesting the conversion of the drug from the crystalline to the amorphous state. In electron micrographs of all PM, independently of the percentage of the drug, the crystal structure of EFV was clearly detectable. Moreover, electron micrographs of the SD with the two polymers in different ratios investigated, we observed the presence of particles with irregular size and morphology, also occurring an extensive change in the appearance of the polymer, not being possible to differentiate the two components. IR spectra of PM corresponds to the overlapping of polymer and EFV bands indicating thereby that there is no interaction between them, unlike the spectra of all SD that showed complete disappearance of the band related to the axial deformation of the NH group of EFV. Therefore, this study was able to obtain a suitable formulation to overcome the solubility limitations of the EFV, since SD PVPVA 64-EFZ 10% was chosen as the best system in delay crystallization of the prototype, reaching higher levels of super saturation.

Keywords: characterization, dissolution, Efavirenz, solid dispersions

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Authors: Beatriz Rebocho, Elisabete Valente, Carla Palma, Andreia Guilherme, Filipa Bessa, Paula Sobral

Abstract:

The global accumulation of plastic in the oceans is a growing problem. Plastic is transported from its source to the oceans via rivers, which are considered the main route for plastic particles from land-based sources to the ocean. These plastics undergo physical and chemical degradation resulting in microplastics. The i-Plastic project aims to understand and predict the dispersion, accumulation and impacts of microplastics (5 mm to 1 µm) and nano plastics (below 1 µm) in marine environments from the tropical and temperate land-ocean interface to the open ocean under distinct flow and climate regimes. Seasonal monitoring of the fluxes of microplastics was carried out in (three) coastal areas in Brazil, Portugal and Spain. The present work shows the first results of in-situ seasonal monitoring and mapping of microplastics in ocean waters between Ovar and Vieira de Leiria (Portugal), in which 43 surface water samples and 43 water column samples were collected in contrasting seasons (spring and autumn). The spring and autumn surface water samples were collected with a 300 µm and 150 µm pore neuston net, respectively. In both campaigns, water column samples were collected using a conical mesh with a 150 µm pore. The experimental procedure comprises the following steps: i) sieving by a metal sieve; ii) digestion with potassium hydroxide to remove the organic matter original from the sample matrix. After a filtration step, the content is retained on a membrane and observed under a stereomicroscope, and physical and chemical characterization (type, color, size, and polymer composition) of the microparticles is performed. Results showed that 84% and 88% of the surface water and water column samples were contaminated with microplastics, respectively. Surface water samples collected during the spring campaign averaged 0.35 MP.m-3, while surface water samples collected during autumn recorded 0.39 MP.m-3. Water column samples from the spring campaign had an average of 1.46 MP.m-3, while those from the autumn recorded 2.54 MP.m-3. In the spring, all microplastics found were fibers, predominantly black and blue. In autumn, the dominant particles found in the surface waters were fibers, while in the water column, fragments were dominant. In spring, the average size of surface water particles was 888 μm, while in the water column was 1063 μm. In autumn, the average size of surface and water column microplastics was 1333 μm and 1393 μm, respectively. The main polymers identified by Attenuated Total Reflectance (ATR) and micro-ATR Fourier Transform Infrared (FTIR) spectroscopy from all samples were low-density polyethylene (LDPE), polypropylene (PP), polyethylene terephthalate (PET), and polyvinyl chloride (PVC). The significant difference between the microplastic concentration in the water column between the two campaigns could be due to the remixing of the water masses that occurred that week due to the occurrence of a storm. This work presents preliminary results since the i-Plastic project is still in progress. These results will contribute to the understanding of the spatial and temporal dispersion and accumulation of microplastics in this marine environment.

Keywords: microplastics, Portugal, Atlantic Ocean, water column, surface water

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Authors: Fernanda Piculo, Giovana Vesentini, Gabriela Marini, Debora Cristina Damasceno, Angelica Mercia Pascon Barbosa, Marilza Vieira Cunha Rudge

Abstract:

Introduction: Women with previous gestational diabetes mellitus (GDM) were significantly more likely to have urinary incontinence (UI) and pelvic floor muscle dysfunction compared to non-diabetic women two years after a cesarean section. Additional results demonstrated that induced diabetes causes detrimental effects on pregnant rat urethral muscle. These results indicate the need for exploration of the mechanistic role of a recovery factor in female UI. Chemokine ligand 7 (CCL7) was significantly over expressed in rat serum, urethral and vaginal tissues immediately following induction of stress UI in a rat model simulating birth trauma. CCL7 over expression has shown potency for stimulating targeted stem cell migration and provide a translational link (clinical measurement) which further provide opportunities for treatment. The aim of this study was to investigate the CCL7 levels profile in diabetic pregnant women with urinary incontinence during pregnancy over the first year postpartum. Methods: This study was conducted in the Perinatal Diabetes Research Center of the Botucatu Medical School/UNESP, and was approved by the Research Ethics Committee of the Institution (CAAE: 20639813.0.0000.5411). The diagnosis of GDM was established between 24th and 28th gestational weeks, by the 75 g-OGTT test according to ADA’s criteria. Urinary incontinence was defined according to the International Continence Society and the CCL7 levels was measured by ELISA (R&D Systems, Catalog Number DCC700). Two hundred twelve women were classified into four study groups: normoglycemic continent (NC), normoglycemic incontinent (NI), diabetic continent (DC) and diabetic incontinent (DI). They were evaluated at six-time-points: 12-18, 24-28 and 34-38 gestational weeks, 24-48 hours, 6 weeks and 6-12 months postpartum. Results: At 12-18 weeks, it was possible to consider only two groups, continent and incontinent, because at this early gestational period has not yet been the diagnosis of GDM. The group with GDM and UI (DI group) showed lower levels of CCL7 in all time points during pregnancy and postpartum, compared to normoglycemic groups (NC and NI), indicating that these women have not recovered from child birth induced UI during the 6-12 months postpartum compared to their controls, and that the progression of UI and/or lack of recovery throughout the first postpartum year can be related with lower levels of CCL7. Instead, serum CCL7 was significantly increased in the NC group. Taken together, these findings of overexpression of CCL7 in the NC group and decreased levels in the DI group, could confirm that diabetes delays the recovery from child birth induced UI, and that CCL7 could potentially be used as a serum marker of injury. Conclusion: This study demonstrates lower levels of CCL7 in the DI group during pregnancy and postpartum and suggests that the progression of UI in diabetic women and/or lack of recovery throughout the first postpartum year can be related with low levels of CCL7. This provides a translational potential where CCL7 measurement could be used as a surrogate for injury after delivery. Successful controlled CCL7 mediated stem cell homing to the lower urinary tract could one day introduce the potential for non-operative treatment or prevention of stress urinary incontinence.

Keywords: CCL7, gestational diabetes, pregnancy, urinary incontinence

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