901 resultados para Bioavailability


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Schistosomiasis is still an endemic disease in many regions, with 250 million people infected with Schistosoma and about 500,000 deaths per year. Praziquantel (PZQ) is the drug of choice for schistosomiasis treatment, however it is classified as Class II in the Biopharmaceutics Classification System, as its low solubility hinders its performance in biological systems. The use of cyclodextrins is a useful tool to increase the solubility and bioavailability of drugs. The aim of this work was to prepare an inclusion compound of PZQ and methyl-beta-cyclodextrin (MeCD), perform its physico-chemical characterization, and explore its in vitro cytotoxicity. SEM showed a change of the morphological characteristics of PZQ:MeCD crystals, and IR data supported this finding, with changes after interaction with MeCD including effects on the C-H of the aromatic ring, observed at 758 cm(-1). Differential scanning calorimetry measurements revealed that complexation occurred in a 1:1 molar ratio, as evidenced by the lack of a PZQ transition temperature after inclusion into the MeCD cavity. In solution, the PZQ UV spectrum profile in the presence of MeCD was comparable to the PZQ spectrum in a hydrophobic solvent. Phase solubility diagrams showed that there was a 5.5-fold increase in PZQ solubility, and were indicative of a type A(L) isotherm, that was used to determine an association constant (K(a)) of 140.8 M(-1). No cytotoxicity of the PZQ:MeCD inclusion compound was observed in tests using 3T3 cells. The results suggest that the association of PZQ with MeCD could be a good alternative for the treatment of schistosomiasis.

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Background, aim, and scope Contaminated sediments are a worldwide problem, and mobilization of contaminants is one of the most critical issues in environmental risk assessment insofar as dredging projects are concerned. The investigation of how toxic compounds are mobilized during dredging operations in the channel of the Port of Santos, Brazil, was conducted in an attempt to assess changes in the bioavailability and toxicity of these contaminants.Materials and methods Bulk sediment samples and their interstitial waters and elutriates were subjected to chemical evaluation and ecotoxicological assessment. Samples were collected from the channel before dredging, from the dredge's hopper, and from the disposal site and its surroundings.Results The results indicate that the bulk sediments from the dredging site are contaminated moderately with As, Pb, and Zn and severely with Hg, and that polycyclic aromatic hydrocarbon (PAH) concentrations are relatively high. Our results also show a 50% increase in PAH concentrations in suspended solids in the water collected from the hopper dredge. This finding is of great concern, since it refers to the dredge overflow water which is pumped back into the ecosystem. Acute toxicity tests on bulk sediment using the amphipod Tiburonella viscana showed no toxicity, while chronic tests with the sea urchin Lytechinus variegatus showed toxicity in the interstitial waters and elutriates. Results are compared with widely used sediment quality guidelines and with a sediment quality assessment scheme based on various lines of evidence.Conclusions The data presented here indicate that the sediments collected in this port show a certain degree of contamination, especially those from the inner part of the channel. The classification established in this study indicated that sediments from the dredged channel are impacted detrimentally and that sea disposal may disperse contaminants. According to this classification, the sediments are inappropriate for disposal at sea. It should be emphasized that the poor quality of fine sediments discharged from the hopper dredge in the overflow process can recontaminate the environment.Recommendations and perspectives These findings will help to underpin improved planning of management strategies for dredging operations and sediment disposal in Brazil and other countries.

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Background: Assessing the chemical or bacterial contamination in marine waters and sediments is a very common approach to evaluate marine pollution and associated risks. However, toxicity and organic pollution of beach sands have not yet been considered, except in adjacent waters. In the present study, the toxicity and the chemical contamination of natural beach sands collected 20 m from the shoreline at two sites located on the Mediterranean Sea (Marseille and La Marana, Corsica) were studied. Results: Up to 16.93% (net percentage) abnormal or dead larvae was observed in elutriates prepared from the urban beach sand sample (Marseille); no significant toxicity was observed in the sample collected from the reference beach in La Marana. Results of Fourier transform infrared spectroscopy analyses revealed that no microplastics were present in either of the samples. Several polycyclic aromatic hydrocarbons [PAHs] in both samples and a larger number of individual PAHs in the urban sample than in the sample collected from the reference beach were detected. In addition, the antioxidant dioctyldiphenylamine was detected in both beach sand samples, whereby a higher concentration was found in La Marana than in Marseille. Calculated PAH concentrations in elutriates were generally higher than measured ones. Conclusions: The results of this preliminary study provide evidence of toxicity and the presence of organic trace contaminants in beach sands from France. According to our results, monitoring using a combination of biotests and chemical analyses is recommended, especially of sediments from beaches abandoned to urban and industrial areas.

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Proton-pump inhibitors (PPIs) are one of the most active ingredients prescribed in Spain. In recent decades there has been an overuse of these drugs in both outpatient clinics and hospitals that has lead to a significant increase in healthcare spending and to an increase in the risk of possible side effects. It is important for health professionals to know the accepted indications and the correct doses for the use of these drugs. On the market there are different types of PPI: omeprazole, pantoprazole, lansoprazole, rabeprazole and esomeprazole. Omeprazole is the oldest and most used PPI, being also the cheapest. Although there are no important differences between PPIs in curing diseases, esomeprazole, a new-generation PPI, has proved to be more effective in eradicating H. pylori and in healing severe esophagitis compared to other PPIs. In recent years the use of generic drugs has spread; these drugs have the same bioavailability than the original drugs. In the case of PPIs, the few comparative studies available in the literature between original and generic drugs have shown no significant differences in clinical efficacy.

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Introduction: Large nutritional surveys in Peru have identified the magnitude and location of the different types of malnutrition. The chronic type is the most prevalent one. However, although rates may be considered as alarming (even more in rural areas), only one of these studies contains information about intake characteristics, using 24-hour recalls (R24). That is, it lacks some other systems, adapted to the gastronomical characteristics of their regions and to the bioavailability of food in each area, in order to locate the origin of this situation and, thus, propose truly effective and efficient solutions. Aim: To determine the nutritional value of the main dishes consumed by the residents of a slum in Peruvian Amazon. Methods: Ninety-eight participants completed three 24-h recalls. Based on these data, we selected the 25 most commonly eaten dishes and evaluated their nutritional composition. We took note of the homemade recipes, weights and measures. In addition, we observed preparation and cooking. The mean nutritional composition of each dish was calculated per 100 g using the Nutriplato 4.6. software. We also calculated gains or losses resulting from culinary treatments. Results: Within those which include milk, the highest energy density is the mingado de arroz. In the group of fish, the most energetic is pescado frito, while within meat-based recipes tallarín con pollo, res asada and chancho frito are the most energetic ones. Regarding prepared dishes, the juane is the highest energy density of all recipes. Inside garnish, using bananas as the main ingredient, plátano frito and madurito are the most energetic. Fats are higher in fried dishes and those which contribute most fat ratio. The same thing happens with garnish as 100 grams of plátano frito or madurito contain more than 70% of the RDA. Res asada and juane present the highest sodium level. Conclusions: If we wish to offer healthier dishes, it is necessary to change their composition and/or cooking methods, reducing the consumption of fried foods. Sodium intake should also be reduced. Two foods could be important to that aim: menudencia de pollo, rich in B vitamins and low in fat, and frijol hervido, which is rich in vegetable protein and, with rice dishes ubiquitous in this area, increases the biological value of ingested proteins.

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Dissertação de mestrado, Qualidade em Análises, Faculdade de Ciências e Tecnologia, Universidade do Algarve, 2014

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With the advances in medicine, life expectancy of the world population has grown considerably in recent decades. Studies have been performed in order to maintain the quality of life through the development of new drugs and new surgical procedures. Biomaterials is an example of the researches to improve quality of life, and its use goes from the reconstruction of tissues and organs affected by diseases or other types of failure, to use in drug delivery system able to prolong the drug in the body and increase its bioavailability. Biopolymers are a class of biomaterials widely targeted by researchers since they have ideal properties for biomedical applications, such as high biocompatibility and biodegradability. Poly (lactic acid) (PLA) is a biopolymer used as a biomaterial and its monomer, lactic acid, is eliminated by the Krebs Cycle (citric acid cycle). It is possible to synthesize PLA through various synthesis routes, however, the direct polycondensation is cheaper due the use of few steps of polymerization. In this work we used experimental design (DOE) to produce PLAs with different molecular weight from the direct polycondensation of lactic acid, with characteristics suitable for use in drug delivery system (DDS). Through the experimental design it was noted that the time of esterification, in the direct polycondensation, is the most important stage to obtain a higher molecular weight. The Fourier Transform Infrared (FTIR) spectrograms obtained were equivalent to the PLAs available in the literature. Results of Differential Scanning Calorimetry (DSC) showed that all PLAs produced are semicrystalline with glass transition temperatures (Tgs) ranging between 36 - 48 °C, and melting temperatures (Tm) ranging from 117 to 130 °C. The PLAs molecular weight characterized from Size Exclusion Chromatography (SEC), varied from 1000 to 11,000 g/mol. PLAs obtained showed a fibrous morphology characterized by Scanning Electron Microscopy (SEM)

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Tese de Doutoramento, Química, Especialização em Química Orgânica, Faculdade de Ciências e Tecnologia, Universidade do Algarve, 2016

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Purpose: To compare oral bioavailability and pharmacokinetic parameters of different lornoxicam formulations and to assess similarity in plasma level profiles by statistical techniques. Methods: An open-label, two-period crossover trial was followed in 24 healthy Pakistani volunteers (22 males, 2 females). Each participant received a single dose of lornoxicam controlled release (CR) microparticles and two doses (morning and evening) of conventional lornoxicam immediate release (IR) tablet formulation. The microparticles were prepared by spray drying method. The formulations were administered again in an alternate manner after a washout period of one week. Pharmacokinetic parameters were determined by Kinetica 4.0 software using plasma concentration-time data. Moreover, data were statistically analyzed at 90 % confidence interval (CI) and Schuirmann’s two one-sided t-test procedure. Results: Peak plasma concentration (Cmax) was 20.2 % lower for CR formulation compared to IR formulation (270.90 ng/ml vs 339.44 ng/ml, respectively) while time taken to attain Cmax (tmax) was 5.25 and 2.08 h, respectively. Area under the plasma drug level versus time (AUC) curve was comparable for both CR and IR formulations. The 90 % confidence interval (CI) values computed for Cmax, AUC0-24, and AUC0-∞ , after log transformation, were 87.21, 108.51 and 102.74 %, respectively, and were within predefined bioequivalence range (80 - 125 %). Conclusion: The findings suggest that CR formulation of lornoxicam did not change the overall pharmacokinetic properties of lornoxicam in terms of extent and rate of lornoxicam absorption.

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Purpose: To enhance the solubility and dissolution rate of the antidiabetic drug repaglinide by solid dispersion (SD) technique Method: The solid dispersion of repaglinide was prepared by solvent evaporation method using the hydrophilic carrier, polyethylene glycol 4000 (PEG 4000) in three drug:PEG 4000 ratios (1:1, 1:3, 1:5). For comparison, physical mixtures of repaglinide and PEG 4000 in the same ratios were also prepared. The formulations were characterized by Fourier transformed infrared spectroscopy (FTIR), x-ray diffractometry (XRD) and differential scanning colorimetry (DSC). Phase solubility study of pure repaglinide, physical mixture and solid dispersion was performed in distilled water. Dissolution studies were carried out in pH 7.4 phosphate buffer. Results: DSC and XRD results indicate that repaglinide exists in amorphous form in solid dispersion. FT-IR analysis demonstrated the presence of intermolecular hydrogen bonding between repaglinide and PEG 4000 in the solid dispersion. The solubility of pure repaglinide was enhanced from 22.5± 5.0 to 235.5± 5.0 µg/mL in distilled water at 37 0C. Rapid burst release (80 - 86 %) from the solid dispersion formulations was observed within 15 min. Conclusion: The solubility and dissolution rate of repaglinide are enhanced by formulating SDs of repaglinide with PEG 4000. This will likely lead to increase in bioavailability which would be beneficial for better glucose control in diabetic patients.

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Purpose: To investigate the interaction between quinine and Garcinia kola using an in vitro adsorption study. Methods: In vitro interaction between quinine and G. kola was conducted at 37 ± 0.1 °C. Adsorption of quinine (2.5 - 40 μg/ml) to 2.5 % w/v G. kola suspension was studied. Thereafter, quinine desorption process was investigated. The amount of quinine adsorbed and desorbed was quantified using HPLC. A Freundlich isotherm was constructed to describe the resulting data and percentage of quinine desorbed was determined from the desorption data. Results: An adsorption isotherm of the data gave a Freundlich constant (K) of 52.66 μg/g, with a slope of 0.69 indicating a high capacity and affinity of G. kola to adsorb quinine at a concentration smaller than 2.41 μg/g of G. kola. However the adsorptive capacity of G. kola for quinine at 37 ± 0.1 °C appears to be a saturable process as observed from the isotherm. Quinine desorption from G. kola peaked at 1 hour (37.51 %) and decreased to a constant amount (about 35 %) over the remaining sampling time. Conclusion: Quinine is adsorbed on G. kola in vitro. This suggests that concurrent administration of quinine and G. kola should be avoided, to prevent potential drug interaction and decreased drug bioavailability.

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Purpose: To prepare and evaluate floating microspheres of curcumin for prolonged gastric residence and to study their effect on alloxan-induced diabetic rats. Methods: Floating microsphere were prepared by emulsion-solvent diffusion method, using hydroxylpropyl methylcellulose, chitosan and Eudragit S 100 polymer in varying proportions. Ethanol/dichloromethane blend was used as solvent in a ratio of 1:1. The floating microspheres were evaluated for flow properties, particle size, incorporation efficiency, as well as in-vitro floatability and drug release. The anti-diabetic activity of the floating microspheres of batch FM4 was performed on alloxaninduced diabetic rats. Result: The floating microspheres had particle size, buoyancy, drug entrapment efficiency and yield in the ranges of 255.32 - 365.65 μm, 75.58 - 89.59, 72.6 - 83.5, and 60.46 - 80.02 %, respectively. Maximum drug release after 24 h was 82.62 % for formulation FM4 and 73.879, 58.613 and 46.106 % for formulations FM1, FM2, and FM3 respectively. In-vivo data obtained over a 120-h period indicate that curcumin floating microspheres from batch FM4 showed the better glycemic control than control and a commercial brand of the drug. Conclusion: The developed floating curcumin delivery system seems economical and effective in diabetes management in rats, and enhances the bioavailability of the drug.

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Introduction: The In vitro-in vivo pharmacokinetic correlation models (IVIVC) are a fundamental part of the drug discovery and development process. The ability to accurately predict the in vivo pharmacokinetic profile of a drug based on in vitro observations can have several applications during a successful development process. Objective: To develop a comprehensive model to predict the in vivo absorption of antiretroviral drugs based on permeability studies, in vitro and in vivo solubility and demonstrate its correlation with the pharmacokinetic profile in humans. Methods: Analytical tools to test the biopharmaceutical properties of stavudine, lamivudine y zidovudine were developed. The kinetics of dissolution, permeability in caco-2 cells and pharmacokinetics of absorption in rabbits and healthy volunteers were evaluated. Results: The cumulative areas under the curve (AUC) obtained in the permeability study with Caco-2 cells, the dissolution study and the pharmacokinetics in rabbits correlated with the cumulative AUC values in humans. These results demonstrated a direct relation between in vitro data and absorption, both in humans and in the in vivo model. Conclusions: The analytical methods and procedures applied to the development of an IVIVC model showed a strong correlation among themselves. These IVIVC models are proposed as alternative and cost/effective methods to evaluate the biopharmaceutical properties that determine the bioavailability of a drug and their application includes the development process, quality assurance, bioequivalence studies and pharmacosurveillance.

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Dissertação (mestrado)—Universidade de Brasília, Instituto de Ciências Biológicas, Programa de Pós-Graduação em Nanociência e Nanobiotecnologia, 2016.

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Iron oxides and arsenic are prevalent in the environment. With the increase interest in the use of iron oxide nanoparticles (IONPs) for contaminant remediation and the high toxicity of arsenic, it is crucial that we evaluate the interactions between IONPs and arsenic. The goal was to understand the environmental behavior of IONPs in regards to their particle size, aggregation and stability, and to determine how this behavior influences IONPs-arsenic interactions. A variety of dispersion techniques were investigated to disperse bare commercial IONPs. Vortex was able to disperse commercial hematite nanoparticles into unstable dispersions with particles in the micrometer size range while probe ultrasonication dispersed the particles into stable dispersions of nanometer size ranges for a prolonged period of time. Using probe ultrasonication and vortex to prepare IONPs suspensions of different particle sizes, the adsorption of arsenite and arsenate to bare hematite nanoparticles and hematite aggregates were investigated. To understand the difference in the adsorptive behavior, adsorption kinetics and isotherm parameters were determined. Both arsenite and arsenate were capable of adsorbing to hematite nanoparticles and hematite aggregates but the rate and capacity of adsorption is dependent upon the hematite particle size, the stability of the dispersion and the type of sorbed arsenic species. Once arsenic was adsorbed onto the hematite surface, both iron and arsenic can undergo redox transformation both microbially and photochemically and these processes can be intertwined. Arsenic speciation studies in the presence of hematite particles were performed and the effect of light on the redox process was preliminary quantified. The redox behavior of arsenite and arsenate were different depending on the hematite particle size, the stability of the suspension and the presence of environmental factors such as microbes and light. The results from this study are important and have significant environmental implications as arsenic mobility and bioavailability can be affected by its adsorption to hematite particles and by its surface mediated redox transformation. Moreover, this study furthers our understanding on how the particle size influences the interactions between IONPs and arsenic thereby clarifying the role of IONPs in the biogeochemical cycling of arsenic.