RESUMEN
Neratinib is a potent anticancer drug, used for the treatment of breast cancer. It is poorly soluble at higher pH, which tends to minimize the therapeutic effects in the lower GIT leads to its poor bioavailability. An attempt has been made to prepare and develop a novel gastro-retentive system of neratinib to improve the drug bioavailability in the GIT by enhancing the gastric retention time. The floating matrix tablets were prepared by various proportions of carbopol 940, micro-crystalline cellulose (MCC) and ethyl cellulose (EC), sodium bicarbonate (NaHCO3) as gas forming agent, by direct compression. The formulation mixture was assessed for pre and post compression test, lag time, in-vitro floating, FTIR, water uptake/swelling index, in vitro and kinetic release studies. The findings revealed that, the parameters of compression (pre and post) were within USP limits. The floating tablets swelled well and floated for more than 24h, with less than 120 seconds of buoyancy lag time. The optimized formulation F3 showed sustained release up to 12h; a non-Fickian mechanism. Therefore, all the results and findings have shown that developed neratinib floating matrix system is a promising approach as a drug delivery system and application in the treatment of breast cancer.
Asunto(s)
Antineoplásicos/administración & dosificación , Quinolinas/administración & dosificación , Resinas Acrílicas , Antineoplásicos/farmacocinética , Antineoplásicos/uso terapéutico , Celulosa/análogos & derivados , Humanos , Quinolinas/farmacocinética , Quinolinas/uso terapéutico , Bicarbonato de Sodio , Espectroscopía Infrarroja por Transformada de Fourier , Comprimidos/químicaRESUMEN
The objectives of this work was preparation and evaluation of the mucoadhesive elementary osmotic pump tablets of trimetazidine hydrochloride to achieve desired controlled release action and augmentation of oral drug absorption. The drug-loaded core tablets were prepared employing the suitable tableting excipients and coated with polymeric blend of ethyl cellulose and hydroxypropyl methylethylcellulose E5 (4:1). The prepared tablets were characterized for various quality control tests and in vitro drug release. Evaluation of drug release kinetics through model fitting suggested the Fickian mechanism of drug release, which was regulated by osmosis and diffusion as the predominant mechanism. Evaluation of mucoadhesion property using texture analyzer suggested good mucoadhesion potential of the developed osmotic systems. Solid state characterization using Fourier-transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffraction spectroscopy confirmed the absence of any physiochemical incompatibilities between drug and excipients. Scanning electron microscopy analysis showed the smooth surface appearance of the coated tablets with intact polymeric membrane without any fracture. In vivo pharmacokinetic studies in rabbits revealed 3.01-fold enhancement in the oral bioavailability vis-à-vis the marketed formulation (Vastarel MR®). These studies successfully demonstrate the bioavailability enhancement potential of the mucoadhesive elementary osmotic pumps as novel therapeutic systems for other drugs too.
Asunto(s)
Sistemas de Liberación de Medicamentos , Absorción Intestinal , Mucosa Intestinal/metabolismo , Trimetazidina/administración & dosificación , Vasodilatadores/administración & dosificación , Adhesividad , Animales , Disponibilidad Biológica , Celulosa/análogos & derivados , Celulosa/química , Preparaciones de Acción Retardada/administración & dosificación , Preparaciones de Acción Retardada/análisis , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Composición de Medicamentos , Liberación de Fármacos , Estabilidad de Medicamentos , Excipientes/química , Derivados de la Hipromelosa/química , Masculino , Presión Osmótica , Conejos , Reproducibilidad de los Resultados , Propiedades de Superficie , Comprimidos , Trimetazidina/análisis , Trimetazidina/química , Trimetazidina/farmacocinética , Vasodilatadores/análisis , Vasodilatadores/química , Vasodilatadores/farmacocinéticaRESUMEN
Arsenic (As) contamination of agricultural soil has become a major concern due to its adverse effects on plant growth and human health. Selenium nanoparticles (SeNPs), a novel selenium (Se) source, are characterised by their exceptional biocompatibility, degradability, and bioactivities. In the present study, SeNPs were biogenically synthesised and further characterised using UV-visible spectroscopy, XRD, FTIR, and TEM analysis. Different concentrations of the synthesised SeNPs were used to treat Spinacia oleracea L. (spinach) seeds to determine their impact on growth profile, gas exchange, photosynthetic pigments, oxidative stress, and antioxidant enzyme status upon arsenite (AsIII) treatment. The findings revealed that SeNP supplementation at a concentration of 100 µM (SeNPs100) led to a significant reduction in As accumulation by twofold in roots and 1.5-fold in leaves when compared to plants exposed to AsIII100 (µM) alone. Interestingly, the photosynthetic efficiency was also remarkably enhanced upon SeNPs100 treatment, associated with increased activities of the defence enzymes (ascorbate peroxidase, catalase, and glutathione peroxidase) in the AsIII + SeNP-exposed spinach plants as compared to AsIII treatment alone. Overall, the present study highlights the potential of biogenic SeNP supplementation in promoting plant growth and mitigating As toxicity in spinach under AsIII stress. This study could have significant implications for the use of SeNPs as a nanofertiliser in regions grappling with As-contaminated soils for sustainable agriculture and human health.
RESUMEN
Lead (Pb) is one of the most toxic elements on earth. The harmful effects of Pb at higher concentrations were seen on plant vegetation because plants are directly exposed towards it. Indian mustard, a well-known hyperaccumulator plant is the most promising crop for the environment, engaged in a variety of scenarios for ecological cleanup. In the present study, we used ethylene diamine tetraacetic acid (EDTA), a chelating agent that is of remarkable efficiency. The pot experiments were conducted in soil pretreated with 1000 mgkg-1 Pb with different concentrations of EDTA (2-10 mmol). All the growth parameters were reduced significantly in the plants treated with Pb and EDTA, however, a non-significant effect was observed in 5 mmol EDTA compared to Pb alone treatment. Photosynthetic pigments yield, nitrate reductase activity and NPK content were affected negatively; in contrast, superoxide dismutase and catalase activity was increased in Pb and Pb+EDTA treated in both the varieties. The Pb accumulation was elevated significantly by the augmentation of 5 mmol EDTA in both varieties. Accumulation of Pb in the shoot was higher in PM 25 than in P. Vijay, whereas root Pb accumulation showed the opposite, i.e., more Pb in roots of P. Vijay than PM 25. Moreover, The Pb accumulation per plant was observed more in P. Vijay as compared to PM 25. Hence, the present study implies that the augmentation of Pb-polluted soil with EDTA works well while dealing with B. juncea assisted phytoremediation and P. Vijay to be a stronger variety than PM 25. Further, 5 mmol of EDTA was optimum for phytoremediation of the soil polluted with up to 1000 mg Pb kg-1 soil.
Asunto(s)
Planta de la Mostaza , Contaminantes del Suelo , Ácido Edético/farmacología , Plomo/farmacología , Contaminantes del Suelo/análisis , Biodegradación Ambiental , Suelo/química , EtilenosRESUMEN
Since turning carbon neutral is regarded as a major macroeconomic agenda worldwide, this study examines whether financial globalization and good governance can help Brazil, Russia, India, China, South Africa, and Turkey in achieving carbon neutrality. Considering the period of analysis from 2000 to 2020 and utilizing robust econometric methods, it is observed that the environmental consequences vary across different components of financial globalization. In particular, the results validate the pollution haven hypothesis by confirming the carbon emission-boosting effect of de facto financial globalization indicators. In contrast, the pollution halo effect hypothesis is verified by the finding of the carbon emission-abating effect of de jure financial globalization indicators. Besides, promoting good governance is evidenced to impose carbon emission-mitigating impact in the long-run. The findings also authenticate the existence of the Environmental Kuznets Curve (EKC) hypothesis for the emerging countries of concern. Finally, for both the short and long runs, it is found that the non-renewable to renewable energy transition contributes to lower discharges of carbon dioxide, while urbanization results in the amplification of the carbon emission figures. Considering these critically important findings, it is necessary for these countries to impose restrictions on the influx of unclean foreign direct investment, facilitate and ease the investment process for foreign investors for investing in environment-friendly projects, promote good governance, and adopt green economic growth and sustainable urbanization policies by developing their respective renewable energy sectors.
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Contaminación Ambiental , Internacionalidad , Desarrollo Económico , Energía Renovable , Inversiones en Salud , Dióxido de Carbono/análisisRESUMEN
Recognizing the environmental development-related commitments made by the Next Eleven countries at 26th Conference of Parties (COP26), this study scrutinizes the repercussions accompanying good democratic governance, renewable energy transition, economic growth, and the ratification of the Kyoto Protocol on carbon emission figures of these emerging nations. In this regard, the period of analysis considered spans from 1990 to 2018 while the econometric analyses involve application of both parametric and non-parametric panel data estimators. Among the key findings, firstly, the outcomes from the parametric estimation methods verify that establishing better democratic governance and undergoing renewable energy transition, both independently and jointly, curb carbon emission levels, while higher economic growth and the signing of the Kyoto Protocol are responsible for boosting emissions the Next Eleven countries. Secondly, the findings derived using the non-parametric methods reveal a great deal of heterogeneity when compared with the results obtained from the parametric analysis. Notably, better democratic governance is seen to reduce carbon emissions in less and moderately polluted. Next Eleven nations, while renewable energy transition curbs emissions only in the moderately and highly polluted ones. Additionally, these variables jointly inhibit emissions only in the Next Eleven nations that are moderately polluted. Besides, better democratic governance is observed to mediate the renewable energy transition-carbon emissions nexus only for the less-polluted Next Eleven nations, while the environmental impacts of economic growth and the signing of the Kyoto Protocol vary across different emission quantiles. Accordingly, relevant policies are recommended for helping the Next Eleven countries to comply with their pledges made at the COP26.
Asunto(s)
Dióxido de Carbono , Energía Renovable , Dióxido de Carbono/análisis , Países en Desarrollo , Desarrollo Económico , CarbonoRESUMEN
The Kingdom of Saudi Arabia has recently declared its vision of turning carbon neutral by 2060. This declaration has motivated policymakers in this Arab nation to design policies that can green economic activities in Saudi Arabia so that environmentally sustainable growth can be ensured. Against this backdrop, this study models the independent and joint effects of financial development, globalization, and energy efficiency rates on green growth of the Saudi Arabian economy. In this regard, green growth in the Kingdom of Saudi Arabia is proxied by the difference between the nation's annual per capita growth rates of gross domestic product and carbon dioxide emission. Utilizing data from 1972 to 2018 and controlling for structural break-induced problems found in the data, the findings from the regression and causality analyses confirm the green growth-inhibiting impacts of financial development and trade globalization. In contrast, greater financial globalization is evidenced to drive green growth in the Kingdom of Saudi Arabia. Furthermore, more efficient uses of energy resources are found to not only directly boost green growth but also partially neutralize the long-run green growth-dampening impacts associated with the development of the financial sector. In addition, financial development and trade globalization are observed to jointly inhibit green growth attainment both in the short and long run. In line with these important findings, it is recommended that the government of Saudi Arabia conceptualizes new green growth policies so that the nation's annual per capita economic growth rate outpaces its annual per capita growth rate of carbon dioxide emissions.
Asunto(s)
Dióxido de Carbono , Desarrollo Económico , Arabia Saudita , Dióxido de Carbono/análisis , Producto Interno Bruto , Internacionalidad , Energía RenovableRESUMEN
Oman is committed to turning carbon neutral by 2040 whereby identifying the environmental sustainability-stimulating factors has become a critically important agenda for the nation. Against this backdrop, this study attempts to evaluate the marginal effects of economic growth, financial development, and low-carbon energy use on Oman's carbon footprint levels using quarterly frequency data spanning from 1984Q1 to 2018Q4. Controlling for structural break concerns in the data, the results from the empirical analysis verify the carbon footprint-related environmental Kuznets curve hypothesis for Oman in the long-run. In this regard, the threshold level of per capita real GDP level of Oman is predicted at around US $23,500 which is below the average and maximum per capita real GDP level of Oman during the period considered in this study. Besides, the development of the financial sector and scaling up consumption of low-carbon energy resources are evidenced to boost and curb Oman's short- and long-run carbon footprint figures, respectively. More importantly, the joint carbon footprint-mitigating impact of financial development and low-carbon energy use is also unearthed from the findings. In line with these major findings, a couple of relevant policy interventions are suggested to help Oman accomplish its 2040 carbon-neutrality agenda.
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Huella de Carbono , Desarrollo Económico , Carbono/análisis , Dióxido de Carbono/análisis , OmánRESUMEN
The traditional literature has explored various factors including, but not limited to, trade openness, financial development, energy consumption, foreign direct investment, globalization, and per capita income that significantly contribute to carbon emissions. However, the current study identifies aggregate domestic consumption spending as a novel driver of carbon dioxide, employing the data for the period of 1973-2018 in Pakistan. To this end, we develop the theoretical framework to illustrate the link between aggregate domestic consumption spending and carbon dioxide emissions and deploy autoregressive distributed lag (ARDL), asymmetric ARDL, and the threshold non-linear ARDL (NARDL) techniques. The results of the ARDL method suggest that only in the short run, aggregate domestic consumption spending significantly affects carbon dioxide emissions. Furthermore, the findings of the NARDL approach reveal that the positive and negative shocks significantly deteriorate and ameliorate the environmental quality by increasing and decreasing the pollution, respectively, in the short and long run. Even though the outcome of the threshold NARDL technique supports the results of the aforementioned approaches, the novelty of the current study is to find out the threshold in aggregate domestic consumption spending, which carries a significant role in determining the carbon emissions in both periods. Besides, we infer that fossil fuels energy and trade openness also degrade the Pakistani climate by boosting atmospheric pollution. Additionally, the application of the asymmetric Granger causality test validates the results by asserting the casual relationship between aggregate domestic consumption spending and carbon dioxide emissions. Based on the results, we suggest the authorities to start to promote the deployment of green products publicly to obtain green and sustainable development.