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1.
Anal Sci ; 2024 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-38554251

RESUMO

Despite the high medicinal value of tiopronin, there are substantial adverse effects such as yellow skin, yellow eyes, muscle aches, etc. Therefore, there is a huge necessity to identify tiopronin using advanced sensors in provided samples. Recently, the preference for graphene quantum dots (GQDs) and inorganic nanomaterial-based fluorescent sensors for the detection of pharmaceuticals has been extensively documented due to their plentiful advantages. Therefore, in this work, the cobalt-doped GQDs decorated vanadium pentoxide nanosheet-based fluorescence switch 'Off-On' sensor (Co-GQDs@V2O5-NS) was designed for highly sensitive and selective detection of tiopronin. Briefly, the green synthesis of highly fluorescent Co-GQDs was carried out using a hydrothermal method. Meanwhile, the synthesis of V2O5-NS was synthesized using the liquid exfoliation method. The synthesis of Co-GQDs@V2O5-NS was accomplished wherein Co-GQDs adsorbed on the surface of V2O5-NS that offered the quenching of fluorescence of Co-GQDs. Afterward, the addition of tiopronin into the quenched probe disclosed the proportional recovery of fluorescence of Co-GQDs. Here, the addition of tiopronin provides the decomposition of V2O5-NS and conversion into the V4+ that aids in releasing the quenched fluorescence of Co-GQDs. The limit of detection and linearity range for tiopronin was found to be 1.43 ng/mL and 10-700 ng/mL, respectively. Moreover, it demonstrated high selectivity, good stability at experimental conditions, and practicality in analyzing tiopronin in spiked sample analysis. Hence, the designed Co-GQDs@V2O5-NS nanosized sensor enables high sensitivity, selectivity, simplicity, label-free, and eco-friendly tiopronin recognition. In the future, the utility of Co-GQDs@V2O5-NS can open a new door for sensing tiopronin in provided samples.

2.
Nat Prod Bioprospect ; 13(1): 39, 2023 Oct 16.
Artigo em Inglês | MEDLINE | ID: mdl-37843642

RESUMO

The primary approaches to treat cancerous diseases include drug treatment, surgical procedures, biotherapy, and radiation therapy. Chemotherapy has been the primary treatment for cancer for a long time, but its main drawback is that it kills cancerous cells along with healthy ones, leading to deadly adverse health effects. However, genitourinary cancer has become a concern in recent years as it is more common in middle-aged people. So, researchers are trying to find possible therapeutic options from natural small molecules due to the many drawbacks associated with chemotherapy and other radiation-based therapies. Plenty of research was conducted regarding genitourinary cancer to determine the promising role of natural small molecules. So, this review focused on natural small molecules along with their potential therapeutic targets in the case of genitourinary cancers such as prostate cancer, renal cancer, bladder cancer, testicular cancer, and so on. Also, this review states some ongoing or completed clinical evidence in this regard.

3.
Gels ; 9(8)2023 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-37623124

RESUMO

Nanocomposite polymeric gels infused with fluorescent nanoparticles have surfaced as a propitious category of substances for biomedical purposes owing to their exceptional characteristics. The aforementioned materials possess a blend of desirable characteristics, including biocompatibility, biodegradability, drug encapsulation, controlled release capabilities, and optical properties that are conducive to imaging and tracking. This paper presents a comprehensive analysis of the synthesis and characterization of fluorescent-nanoparticle-impregnated nanocomposite polymeric gels, as well as their biomedical applications, such as drug delivery, imaging, and tissue engineering. In this discourse, we deliberate upon the merits and obstacles linked to these substances, encompassing biocompatibility, drug encapsulation, optical characteristics, and scalability. The present study aims to provide an overall evaluation of the potential of fluorescent-nanoparticle-impregnated nanocomposite polymeric gels for biomedical applications. Additionally, emerging trends and future directions for research in this area are highlighted.

4.
Polymers (Basel) ; 15(3)2023 Jan 17.
Artigo em Inglês | MEDLINE | ID: mdl-36771784

RESUMO

Piroxicam is a Biopharmaceutical Classification System (BCS) Class II drug having poor aqueous solubility and a short half-life. The rationale behind the present research was to develop a Piroxicam nanosuspension to enhance the solubility and thereby the in vitro bioavailability of the drug. Piroxicam nanosuspension (PRX NS) was prepared by an anti-solvent precipitation technique and optimized using a full-factorial design. Herein, the nanosuspension was prepared using polymer polyvinylpyrrolidone (PVP) K30® and Poloxamer 188® as a stabilizer to improve the solubility and in vitro bioavailability of the drug. Nine formulations were prepared based on 32 full-factorial experimental designs to study the effect of the formulation variables such as concentration of poloxamer 188 (%) (X1) and stirring speed (rpm) (X2) as a process variable on the response of particle size (nm) and solubility (µg/mL). The prepared NS was characterized by phase solubility, Fourier-transform infrared (FT-IR), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), transmission electron microscopy (TEM), particle size, zeta potential, entrapment efficiency, and percent drug release. DSC and XRPD analysis of freeze-dried NS formulation showed conversion of PRX into a less crystalline form. NS formulations showed a reduction in the size from 443 nm to 228 nm with -22.5 to -30.5 mV zeta potential and % drug entrapment of 89.76 ± 0.76. TEM analysis confirmed the size reduction at the nano level. The solubility was increased from 44 µg/mL to 87 µg/mL by altering the independent variables. The solubility of PRX NS in water was augmented by 14- to 15-fold (87.28 µg/mL) than pure PRX (6.6 µg/mL). The optimized formulation (NS9) at drug-to-stabilizer concentration exhibited a greater drug release of approximately 96.07% after 120 min as compared to the other NS formulations and pure PRX (36.78%). Thus, all these results revealed that the prepared NS formulations have improved the solubility and in vitro dissolution compared to the pure drug. Furthermore, an increase in the drug release was observed from the NS than that of the pure PRX. All these outcomes signified that the prepared PRX NS showed an increase in solubility and in vitro dissolution behavior; which subsequently would aid in attainment of enhanced bioavailability.

5.
Molecules ; 28(2)2023 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-36677558

RESUMO

The present work describes the design and development of seventeen pyrimidine-clubbed benzimidazole derivatives as potential dihydrofolate reductase (DHFR) inhibitors. These compounds were filtered by using ADMET, drug-likeness characteristics calculations, and molecular docking experiments. Compounds 27, 29, 30, 33, 37, 38, and 41 were chosen for the synthesis based on the results of the in silico screening. Each of the synthesized compounds was tested for its in vitro antibacterial and antifungal activities using a variety of strains. All the compounds showed antibacterial properties against Gram-positive bacteria (Staphylococcus aureus and Staphylococcus pyogenes) as well as Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). Most of the compounds either had a higher potency than chloramphenicol or an equivalent potency to ciprofloxacin. Compounds 29 and 33 were effective against all the bacterial and fungal strains. Finally, the 1,2,3,4-tetrahydropyrimidine-2-thiol derivatives with a 6-chloro-2-(chloromethyl)-1H-benzo[d]imidazole moiety are potent enough to be considered a promising lead for the discovery of an effective antibacterial agent.


Assuntos
Antagonistas do Ácido Fólico , Antagonistas do Ácido Fólico/farmacologia , Simulação de Acoplamento Molecular , Antibacterianos/farmacologia , Benzimidazóis/farmacologia , Resistência Microbiana a Medicamentos , Pirimidinas/farmacologia , Relação Estrutura-Atividade , Testes de Sensibilidade Microbiana , Estrutura Molecular
6.
Bull Natl Res Cent ; 46(1): 159, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35669155

RESUMO

Background: During coronavirus pandemic, an unpredictable pile of biomedical waste (BMW) gathers at the top. India produces 710 tonnes of biomedical waste daily. The contribution of COVID-19 related biomedical waste was 126 tonnes per day in first wave of the pandemic. BMW's rapid growth is putting a strain on current waste management facilities, especially in developing countries. A sudden boost in biomedical waste needs rapid and proper segregation and disposal methods to avoid future consequences. Main body of the abstract: From literatures and statistical data available on Central Pollution Control Board (CPCB) it shows that India lags behind in large-scale sorting, collection, careful storage, transfer and disposal of bio waste. India has its own guidelines set by the CPCB to ensure the safe disposal of biomedical waste during diagnosis, treatment and quarantine of COVID-19 patients. Although there are strict guidelines for bio-waste management, many hospitals in the process of implementing them often dispose of waste in inappropriate, chaotic and indiscriminate ways due to negligence or laziness. Often, due to poor separation practices, hospital waste is mixed with general waste, resulting in harmful overall waste flow. Waste disposal handlers are not safe due to their exposure to various health risks and inadequate training in waste management. The present review sheds light on guidelines, measures, and challenges related to biomedical waste management. Short conclusion: Improper waste separation leads to improper waste disposal. Waste generation and management issues are causing daily problems as they have a profound impact on the dramatically changing global environment, including air, water and soil pollution. In addition, BMW's daily production and its processing are inversely proportional. This situation suggests that India will soon be drowning in its own garbage. The focus of this review is on the generation and disposal of biomedical waste. Based on a review of the literature, this evaluation provides a comparative picture of the current status of waste generation, national waste management strategies, and some measures to contribute to waste management and avoid future disasters.

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