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•Curcumin-nicotinamide cocrystal was formed.•Cocrystallization was performed with carbon dioxide as supercritical solvent.•Cocrystal showed 2 times greater dissolution rate in water ...than pure curcumin.•Cocrystal presented greater antinociceptive activity than curcumin.
Curcumin is a bioactive polyphenol, which presents several medicinal benefits such as antinociceptive, anti-inflammatory, anti-carcinogenic, antimalarial, and antioxidant activity. Despite the benefits, the main barrier in curcumin use by pharmaceutical industry is its low solubility in water medium and hence low bioavailability. The cocrystallization process is characterized by the incidence of molecular interactions between the active pharmaceutical ingredient and coformer that enables improvements in physicochemical properties such as solubility and bioavailability. The main objective of this work is to produce a curcumin-nicotinamide cocrystal by Cocrystallization with Supercritical Solvent (CSS) technique in order to increase curcumin water dissolution rate as well as antinociceptive/anti-inflammatory activities. Curcumin-nicotinamide cocrystal dissolution rate were about 2 times greater than pure curcumin in water medium. The cocrystallization process increased curcumin antinociceptive/anti-inflammatory potency probably due to alterations in its bioavailability. These results open new possibilities of use for curcumin cocrystals in pharmaceutical industries.
Microcapsules containing Lactobacillus paracasei BGP-1 were produced by co-extrusion technology using alginate and alginate-shellac blend as wall materials. Sunflower oil and coconut fat were used as ...vehicles to incorporate BGP-1 into the microcapsules. The microcapsules were evaluated with regard the particle size, morphology, water activity and survival of probiotics after 60days of storage at room temperature. Fluidized bed and lyophilization were used to dry the microcapsules and the effect of these processes on probiotic viability was also evaluated. Next, dried microcapsules were exposed to simulated gastrointestinal fluids to verify the survival of BGP-1. Microcapsules dried by fluidized bed had spherical shape and robust structures, whereas lyophilized microcapsules had porous and fragile structures. Dried microcapsules presented a medium size of 0.71–0.86mm and aw ranging from 0.14 to 0.36, depending on the drying process. When comparing the effects of drying processes on BGP-1 viability, the fluidized bed was less aggressive than lyophilization. The alginate-shellac blend combined with coconut fat as core effectively protected the encapsulated probiotic under simulated gastrointestinal conditions. Thus, the production of microcapsules by co-extrusion followed by drying using the fluidized bed is a promising strategy for protection of probiotic cells.
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•Co-extrusion of alginate-shellac and coconut fat was effective on protecting encapsulated BGP-1.•Approximately 93% of encapsulated BGP-1 survived to fluidized bed drying.•After 60days of storage at room temperature, >90% of encapsulated BGP-1 were viable.•Over 95% of encapsulated BGP-1 survived under simulated gastrointestinal conditions.•Microcapsules loaded with BGP-1 may be applied in chocolate, cereal bars and mixed nuts.
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•Curcumin+N-acetylcysteine cocrystals were prepared by cocrystallization with supercritical solvent technique (CSS).•Cocrystals were produced by solvent-free technique.•By DSC, XRD ...and FTIR it has been evidenced that the cocrystals were formed.•Cocrystallization provided cocrystals exhibiting a dissolution rate about 2 times higher than pure curcumin crystals.
Cocrystallization is a method that enables an improvement in physicochemical properties such as solubility, bioavailability, dissolution rate and stability. Curcumin (CUR) is bioactive ingredient known for its wide variety of medicinal benefits, such as anti-inflammatory, anti-carcinogenic, antimalarial and antioxidant activity, however its low solubility in water medium and hence low bioavailability represents a barrier in its use in food and pharmaceutical industry. This work aims to produce curcumin cocrystals by Cocrystallization with Supercritical Solvent (CSS) technique in order to improve curcumin water dissolution rate. N-acetylcysteine (NAC) was chose as coformer by previous screening using Liquid Assisted Grinding (LAG) technique. The cocrystals formations were confirmed through characterizations by Differential Scanning Calorimetry, Powder X-Ray Diffraction, Fourier Transform-Infrared Spectroscopy and Scanning Electron Microscopy. Cocrystals dissolution rate were about 2.2 times greater than pure curcumin dissolution in water medium, which opens new possibilities of use for these cocrystals in pharmaceutical and food industries.
•Microparticle was formed by GAS antisolvent.•The efficiency of encapsulation better than 99%.•Inhibition of peroxide formation was improved in encapsulated resveratrol.•Resveratrol properties have ...been improved with encapsulation.
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In this study, poly(ε-caprolactone) particles containing resveratrol were developed employing the GAS antisolvent technique. A central composite design 22 evaluated the influence of polymer, resveratrol mass ratio (2:1, 1:1, 1:2), and pressure (100, 120, 140 bar) on encapsulation percentage, and efficiency. The values obtained for encapsulation efficiency and percentage of encapsulation at the best conditions attained were 99.34% and 65.31%. In addition, the statistical analysis showed that only the mass ratio had significantly affected the percentage of encapsulation, but neither variable significantly affected efficiency. Microparticles produced demonstrably heterogeneous characteristics and irregular morphology. However, this process did not change either the compound chemical structures or the resveratrol antioxidant activity. Microparticles maintained constant release for 48 h, and in thermal oxidative analysis, the difference between samples and control was 2.57 times smaller than the difference between pure resveratrol and the control sample.
•Curcumin+resveratrol cocrystal was prepared using supercritical technology.•Cocrystal exhibited higher water solubility compared to raw compounds.•Antioxidant activity and dissolution rate were ...improved after cocrystallization.•Cocrystal presented greater antinociceptive activity than raw components.
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Bioactive compounds curcumin and resveratrol have been appointed to have potential for prevention and treatment of several diseases, replacing synthetic compounds with limited action. However, both present low aqueous solubility and bioavailability. Cocrystallization aims to modify physicochemical properties of active compounds by occurrence of intermolecular forces between them and possible modifications in the crystalline matrix. This research aimed to synthesize a curcumin-resveratrol cocrystal by the Cocrystallization with Supercritical Solvent (CSS) technique intending to improve the components solubility and dissolution rate. Characterization by Differential Scanning Calorimetry, X-Ray Powder Diffraction and Fourier Transform-Infrared Spectroscopy confirmed cocrystal formation. Comparing to raw components, cocrystal antioxidant activity was improved as well as dissolution rate. Curcumin and resveratrol solubility were improved 1.5 and 2 times, respectively. Behavioral tests in mice showed that curcumin-resveratrol antinociceptive/anti-inflammatory potency was increased probably due to alterations in its bioavailability, which gives the cocrystal good potential of use in the pharmaceutical industry.
Wastewater treatment is of great concern in the textile industries because dyes, which are released into wastewater, are stable due to their structures and that some of the existing conventional ...techniques are not effective for aqueous removal of dyes. Among the advanced techniques for treatment of industrial effluents, adsorption is one of the most effective processes for removal of dyes from industrial wastewater. Similarly, activated carbons from different sources have been successfully applied as adsorbents for dye removal from aqueous solutions. In this context, this research evaluated the performance of activated carbon produced from peach pit (APC-1.0) for removal of a textile dye, Procion Red MX-5B (PR-5B), through batch adsorption process. The characteristic features of the peach activated carbon were obtained through Fourier transforms infrared spectroscopy, and scanning electron microscopy. The effectiveness of the activated to remove PR-5B from aqua system was compared with that of commercial activated carbon (CAC). In the kinetic study, the contact time was evaluated between 0 and 480 min using two different initial concentrations. Adsorption isotherms of PR-5B onto the two adsorbents were investigated in six different temperatures (298–326 K). The thermodynamic parameters of the process indicated spontaneous and exothermic adsorption. Equilibrium data were best described by Liu isotherm model with maximum removal capacities of 297.2 and 174.0 mg g
−1
for APC-1.0 and CAC, respectively.
Human papillomavirus (HPV) is the causative agent of human cervical cancer and has been associated with oropharyngeal squamous cell carcinoma development. Although prophylactic vaccines have been ...developed, there is a need to develop new targeted therapies for individuals affected with malignant infected lesions in these locations, which must be tested in appropriate models. Cutaneous beta HPV types appear to be involved in skin carcinogenesis. Virus oncogenicity is partly achieved by inactivation of retinoblastoma protein family members by the viral E7 gene. Here we show that the E7 protein of cutaneous beta HPV5 binds pRb and promotes its degradation. In addition, we described an in vivo model of HPV-associated disease in which artificial human skin prepared using primary keratinocytes engineered to express the E7 protein is engrafted onto nude mice. Expression of E7 in the transplants was stably maintained for up to 6 months, inducing the appearance of lesions that, in the case of HPV16 E7, histologically resembled human anogenital lesions caused by oncogenic HPVs. Moreover, it was confirmed through biomarker expression analysis via immunodetection and/or quantitative PCR from mRNA and miRNA that the 16E7-modified engrafted skin shares molecular features with human HPV-associated pretumoral and tumoral lesions. Finally, our findings indicate a decrease of the in vitro capacity of HPV5 E7 to reduce pRb levels in vivo, possibly explaining the phenotypical differences when compared with 16E7-grafts. Our model seems to be a valuable platform for basic research into HPV oncogenesis and preclinical testing of HPV-associated antitumor therapies.
The upper Valanginian – lower Aptian Centenario Formation is a significant producer of oil and gas in the Neuquén Basin, western Argentina. This formation is located exclusively in the subsurface of ...the eastern and northeastern Neuquén Basin, and is 450–1000 m thick. The Centenario Formation laterally interfingers with the Agrio Formation. Previous studies addressing the paleogeographic history of the Centenario Formation are scarce, and a comprehensive geological model has yet to be put forward.
The current study scrutinizes the Centenario Formation, especially its lower member, within the northeastern Neuquén Basin. The study area includes the Cerro Hamaca Oeste, Señal Cerro Bayo, and Volcán Auca Mahuida oilfields operated by Yacimientos Petrolíferos Fiscales (YPF). Sedimentological and ichnological core data, geophysical well logs, and petrographic thin sections have been utilized to construct a geological model. Eleven sedimentary facies and three facies associations have been identified from the core dataset, providing insights into the paleoenvironmental settings and their stresses on infaunal colonization. Basin-margin deposits from the northeastern part of the study region were formed in continental environments, comprising ephemeral fluvial channel complexes and floodplains, and are ichnologically represented by rare Skolithos and common rhizoliths. The central part of the study area is interpreted as recording deposition in ephemeral lakes, river-dominated lake deltas, and coastal lagoons and sabkhas, and is represented by a combination of stressed expressions of both the Skolithos and Scoyenia Ichnofacies. River-dominated, storm-influenced delta deposits are located towards the southwestern limit of the study area, and are ichnologically represented by the Skolithos and depauperate Cruziana Ichnofacies. Deltaic deposits gradually transition into the basinal facies of the Agrio Formation to the west. Overall sedimentologic characteristics suggest semi-arid to arid climatic conditions during deposition.
•The Centenario Formation is a significant producer of oil and gas in the Neuquén Basin, Argentina.•Sedimentological, ichnological, petrographical, and petrophysical analyses refined the paleodepositional interpretations.•The Centenario Formation was deposited in continental, marginal-marine, and deltaic depositional settings.
Over the last few years, the effects of steroid hormones on the brain have been intensively discussed. It has been demonstrated that ATP (acting as a neurotransmitter) is hydrolyzed to adenosine in ...the synaptic cleft by the conjugated action of ectonucleotidases, which include an enzyme of the E-NTPDase family (NTPDase3, apyrase, EC 3.6.1.5) and a 5′-nucleotidase (EC 3.1.3.5). The 5′-nucleotidase enzyme is able to hydrolyze AMP as well as other monophosphate nucleotides. The importance of this enzyme in the central nervous system is to participate in the adenosine formation, a nucleoside with neuroprotective properties and modulatory effects. However, several questions have been raised about the mechanisms of steroid hormones and the possible neuroprotective effects of estrogen. Thus, we examined the effects of gonadal steroid hormone deprivation, induced by ovary removal (OVX) and estradiol replacement therapy, on the ectonucleotidase activities in synaptosomes from hippocampus and cerebral cortex of adult rats. ATP and ADP hydrolysis in synaptosomes from cerebral cortex and hippocampus did not change as a function of OVX and results demonstrated an increase in AMP hydrolysis (82%) in the animals submitted to OVX in cerebral cortex, but not in hippocampus, when compared to control and sham-operated groups. Estradiol replacement therapy reversed this effect. RT-PCR analysis showed that the enhancement of enzyme activity in cerebral cortex could be explained by the higher expression of 5′-nucleotidase, following OVX. The hormones 17β-estradiol (cyclodextrin-encapsulated 17β-estradiol), DHEAS, and pregnenolone (1.0, 2.5, and 5.0
μM) did not alter the nucleotide hydrolysis, in vitro, in synaptosomes from cortex and hippocampus of female adult rats. Results presented, herein, should be considered relevant for hormone replacement therapy, since much controversy exists surrounding this area and the relationship between adenosine and sex steroids is still poorly understood.
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