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1.
ACS Omega ; 9(15): 16893-16903, 2024 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-38645323

RESUMO

Wine has been utilized as a source for medicinal preparations, combined with various herbs, to treat particular ailments and disorders. By utilizing herb extracts, regular but limited consumption of these herbal wines helps to decrease the need for prescription medications to treat a variety of ailments. The diversity and the composition of the yeast micropopulation significantly contribute to the sensory characteristics of wine. A particular metabolic activity characterizes the growth of each wine yeast species, which determines the concentrations of flavor compounds in the final wine. Numerous herbs, such as tulsi, ginger, aloe vera, tea, amla, lemongrass, and peppermint, are used in the preparation of herbal wines, where either the herb or herbal blends are primarily used as the substrate. The variants provided improved accuracy, increased acceptability, and broader uses for the novel product. Herbal wines pave the way to provide nutraceuticals to consumers and protection against pathogenic microorganisms and inflammation through their richness in antioxidants. The existing herbal wines and their health advantages are discussed in this Review, along with some new directions for the herbal wine business.

2.
Heliyon ; 10(7): e28359, 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38560145

RESUMO

Due to increasing concerns about environmental impact and toxicity, developing green and sustainable methods for nanoparticle synthesis is attracting significant interest. This work reports the successful green synthesis of silver (Ag), silver-titanium dioxide (Ag@TiO2), and silver-selenium dioxide (Ag@SeO2) nanoparticles (NPs) using Beta vulgaris L. extract. Characterization by XRD, SEM, TEM, and EDX confirmed the successful formation of uniformly distributed spherical NPs with controlled size (25 ± 4.9 nm) and desired elemental composition. All synthesized NPs and the B. vulgaris extract exhibited potent free radical scavenging activity, indicating significant antioxidant potential. However, Ag@SeO2 displayed lower hemocompatibility compared to other NPs, while Ag@SeO2 and the extract demonstrated reduced inflammation in a carrageenan-induced paw edema animal model. Interestingly, Ag@TiO2 and Ag@SeO2 exhibited strong antifungal activity against Rhizoctonia solani and Sclerotia sclerotium, as evidenced by TEM and FTIR analyses. Generally, the findings suggest that B. vulgaris-derived NPs possess diverse biological activities with potential applications in various fields such as medicine and agriculture. Ag@TiO2 and Ag@SeO2, in particular, warrant further investigation for their potential as novel bioactive agents.

3.
Sci Rep ; 14(1): 6361, 2024 03 16.
Artigo em Inglês | MEDLINE | ID: mdl-38493177

RESUMO

Loratadine (LoR) is a highly lipophilic and practically insoluble in water, hence having a low oral bioavailability. As it is formulated as topical gel, it competitively binds with the receptors, thus reducing the side-effects. The objective of this study was to prepare LoR loaded nanosponge (LoR-NS) in gel for topical delivery. Nine different formulations of emulsion were prepared by solvent evaporation method with polyvinyl alcohol (PVA), ethyl cellulose (EC), and dichloromethane (DCM). Based on 32 Full Factorial Design (FFD), optimization was carried out by varying the concentration of LOR:EC ratio and stirring rate. The preparations were subjected for the evaluation of particle size (PS), in vitro release, zeta potential (ZP) and entrapment efficiency (EE). The results revealed that the NS dispersion was nanosized with sustained release profiles and significant PS. The optimised formulation was formulated and incorporated into carbopol 934P hydrogel. The formulation was then examined to surface morphological characterizations using scanning electron microscopy (SEM) which depicted spherical NS. Stability studies, undertaken for 2 months at 40 ± 2 °C/75 ± 5% RH, concluded to the stability of the formulation. The formulation did not cause skin irritation. Therefore, the prepared NS hydrogel proved to be a promising applicant for LoR as a novel drug delivery system (NDDS) for safe, sustained and controlled topical application.


Assuntos
Hidrogéis , Loratadina , Tamanho da Partícula
4.
Curr Mol Pharmacol ; 17: e18761429269383, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38389415

RESUMO

BACKGROUND: Lung cancer (LC) incidence is rising globally and is reflected as a leading cause of cancer-associated deaths. Lung cancer leads to multistage carcinogenesis with gradually increasing genetic and epigenetic changes. AIMS: Sanguinarine (sang) mediated the anticancer effect in LCC lines by involving the stimulation of reactive oxygen species (ROS), impeding Bcl2, and enhancing Bax and other apoptosis-associated protein Caspase-3, -9, and -PARP, subsequently inhibiting the LC invasion and migration. OBJECTIVE: This study was conducted to investigate the apoptotic rate and mechanism of Sang in human LC cells (LCC) H522 and H1299. METHODS: MTT assay to determine the IC50, cell morphology, and colony formation assay were carried out to show the sanguinarine effect on the LC cell line. Moreover, scratch assay and transwell assay were performed to check the migration. Western blotting and qPCR were done to show its effects on targeted proteins and genes. ELISA was performed to show the VEGF effect after Sanguinarine treatment. Immunofluorescence was done to check the interlocution of the targeted protein. RESULTS: Sang significantly inhibited the growth of LCC lines in both time- and dose-dependent fashions. Flow cytometry examination and Annexin-V labeling determined that Sang increased the apoptotic cell percentage. H522 and H1299 LCC lines treated with Sang showed distinctive characteristics of apoptosis, including morphological changes and DNA fragmentation. CONCLUSION: Sang exhibited anticancer potential in LCC lines and could induce apoptosis and impede the invasion and migration of LCC, emerging as a promising anticancer natural agent in lung cancer management.


Assuntos
Antineoplásicos , Isoquinolinas , Neoplasias Pulmonares , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Apoptose , Benzofenantridinas/farmacologia , Benzofenantridinas/uso terapêutico , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Estresse Oxidativo
5.
J Cosmet Dermatol ; 23(3): 1015-1028, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38268219

RESUMO

BACKGROUND: Tocopherols are well-known antioxidant and moisturizing agent. Tocopherol succinate (TS) are widely used in many skin products especially used in anti-aging and skin whitening product formulation. AIM: We previously reported the successful synthesis and preliminary characterizations of stable TS ethosomal gels (TSEG) (DOI: 10.1111/jocd.14907). Herein, we develop and further characterize TSEG to enhance the stability of the developed formulation with increased permeation through skin. METHODS: Cold method technique was used to prepare TS ethosomes. The developed ethosomal vesicle size was 250 nm, which allowed TS to penetrate through the stratum corneum layer and act on melanocytes. For stability study was assessed by thermogravimetric analysis (TGA) by placing TSEG and unloaded/control ethosomal gel (CEG) at various temperature conditions, that is, 8°C, 25°C, 40°C, and 40°C ± 75% RH for 3 months. Organoleptic evaluation was done in terms of color, odor, and phase separation. Transmission electron microscopy (TEM), Fourier Transform infrared spectroscopy (FTIR), x-ray diffraction spectroscopy (XRD), zeta potential (ZP) and particle size (PS) was used for TSEG physical characterizations. In vitro dissolution and ex-vivo permeation studies (using Franz diffusion cell) were performed for both TSEG and CEG formulations. Human women (N = 34) were used to evaluate in vivo biophysical parameters including erythema, melanin, moisture content, sebum level, and skin elasticity. RESULTS: Developed formulation was highly thermostable during the 3 months. Erythema, melanin, and sebum level decreased while marked improvement (p < 0.05) in moisture content and elasticity have been observed for the developed TSEG. CONCLUSION: The developed TSEG formulation was found to be efficient, safe (no adverse effects observed), stable (at least for 3 months), and easy to use for topical application with improved skin complexation and skin integrity.


Assuntos
Absorção Cutânea , alfa-Tocoferol , Humanos , Feminino , alfa-Tocoferol/metabolismo , Administração Cutânea , Melaninas/metabolismo , Lipossomos/metabolismo , Pele/metabolismo , Eritema , Géis/metabolismo
6.
Bioprocess Biosyst Eng ; 47(1): 75-90, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38081951

RESUMO

A significant waste (e.g., high oil content and pollutants such as heavy metals, dyes, and microbial contaminants) in water is generated during crude oil extraction and industrial processes, which poses environmental challenges. This study explores the potential of Ag@Fe3O4 nanocomposite (NC) biosynthesized using the aqueous leaf extract of Laurus nobilis for the treatment of oily wastewater. The NC was characterized using ultraviolet-visible (UV-Vis) spectrophotometry, Scanning Electron Microscopy (SEM), Fourier Transformed Infrared (FTIR) and X-Ray Diffraction (XRD) spectroscopies. The crystalline structure of the NC was determined to be face-centered cubic with an average size of 42 nm. Ag@Fe3O4 NC exhibited significant degradation (96.8%, 90.1%, and 93.8%) of Rose Bengal (RB), Methylene Blue (MB), and Toluidine Blue (TB), respectively, through a reduction reaction lasting 120 min at a dye concentration of 10 mg/L. The observed reaction kinetics followed a pseudo-first-order model, with rate constants (k-values) of 0.0284 min-1, 0.0189 min-1, and 0.0212 min-1 for RB, MB, and TB, respectively. The fast degradation rate can be attributed to the low band gap (1.9 eV) of Ag@Fe3O4 NC. The NC elicited an impressive effectiveness (99-100%, 98.0%, and 91.8% within 30 min) in removing, under sunlight irradiation, several heavy metals, total petroleum hydrocarbons (TPH), and total suspended solids (TSS) from the oily water samples. Furthermore, Ag@Fe3O4 NC displayed potent antibacterial properties and a good biocompatibility. These findings contribute to the development of efficient and cost-effective methods for wastewater treatment and environmental remediation.


Assuntos
Metais Pesados , Nanocompostos , Águas Residuárias , Fotólise , Antibacterianos/farmacologia , Antibacterianos/química , Água , Corantes/química , Nanocompostos/química , Catálise
7.
Mol Biotechnol ; 2023 Dec 28.
Artigo em Inglês | MEDLINE | ID: mdl-38155285

RESUMO

MicroRNAs (miRNAs) are typically non-coding RNAs of 18-26 nucleotides (nts) that are produced endogenously and regulated post-transcriptionally through degradation or translational repression. Since miRNAs are evolutionarily conserved, their preservation is essential for important regulatory functions in plant development, growth, and responses to environmental stress. Sorghum bicolor (sbi) is a valuable food and fodder crop which is grown worldwide. A range of sbi miRNAs were identified so far as being connected to plant development and stress responses. Herein, we employed a variety of bioinformatics tools for miRNA profiling in sbi and a PCR-based platform for the validation of these miRNAs. In total, 74 new conserved sbi miRNAs from 52 miRNA families have been predicted. Using the psRNA Target method, 10613 different protein targets of these predicted miRNAs have been attained. These targets include 54 GO-terms which have substantial targets in the biological, molecular, and cellular processes. We particularly found that the sbi-miR1861c and sbi-miR5050 are involved to regulate sulphur compound biosynthetic process, while the significant spliceosomal complex is regulated by sbi-miR815b and sbi-miR7768b. Also, we report that the pre-ribosome, electron transport chain, cell communication, cellular respiration, protein localization, and photosynthesis are controlled by sbi-miR2907b, sbi-miR530, sbi-miR7749, sbi-miR1858a, sbi-mi7729a, and sbi-miR417, respectively. The identification and validation of these novel sbi miRNAs shall contribute a lot in improving the crop yield and ensure sustainable agriculture.

8.
Saudi Pharm J ; 31(12): 101839, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37965489

RESUMO

Itraconazole (ITZ) is a renowned antifungal medication, however its therapeutic efficacy is limited by low solubility and oral bioavailability. The current research work attempted to augment the oral bioavailability of ITZ by incorporating into self-emulsifying micelles (SEMCs). To fabricate the SEMCs, various preparation techniques including physical mixture, melt-emulsification, solvent evaporation and kneading, were opted by using different weight ratio of drug and solubilizers i.e. Gelucire-50/13 or Gelucire-44/14 and characterized both in vitro and in vivo. The prepared SEMCs were found to be in the size range from 63.4 ± 5.2 to 284.2 ± 19.5 nm with surface charges ranging from -16 ± 1.2 to -27 ± 2.0 mV. The drug solubility was improved to a reasonable extent with all investigated formulations, however, SEMCs in group 6 prepared by kneading method (KMG6) using Gelucire-44/14: drug (10:1 presented 87.6 folds' increase (964.93 ± 2 µg/mL) compared to solubility of crystalline ITZ (11 ± 2 µg/mL) through kneading method. In addition, KMG6 SEMCs shows the fast drug release compared to other SEMCs. Further, KMG6 SEMCs also exhibited 5.12-fold higher relative intestinal serosal fluid absorption compared to crystalline ITZ. The pharmacokinetic parameters such Cmax, AUC and Tmax of KMG6 SEMCs significantly improved compared to crystalline ITZ. In conclusion, the manipulation of ITZ solubility, dissolution rate and absorption using SEMCs is a promising strategy for bioavailability enhancement.

9.
Sci Rep ; 13(1): 13545, 2023 08 19.
Artigo em Inglês | MEDLINE | ID: mdl-37598271

RESUMO

The effect of three independent variables (i.e., tyrosine, sucrose, and incubation time) on melanin production by Aureobasidium pullulans AKW was unraveled by two distinctive approaches: response surface methodology (i.e. Box Behnken design (BBD)) and artificial neural network (ANN) in this study for the first time ever using a simple medium. Regarding BBD, sucrose and incubation intervals did impose a significant influence on the output (melanin levels), however, tyrosine did not. The validation process exhibited a high consistency of BBD and ANN paradigms with the experimental melanin production. Concerning ANN, the predicted values of melanin were highly comparable to the experimental values, with minor errors competing with BBD. Highly comparable experimental values of melanin were achieved upon using BBD (9.295 ± 0.556 g/L) and ANN (10.192 ± 0.782 g/L). ANN accurately predicted melanin production and showed more improvement in melanin production by about 9.7% higher than BBD. The purified melanin structure was verified by scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), X-ray diffraction pattern (XRD), and thermogravimetric analysis (TGA). The results verified the hierarchical architecture of the particles as small compasses by SEM analysis, inter-layer spacing in the XRD analysis, maximal atomic % for carbon, and oxygen atoms in the EDX analysis, and the great thermal stability in the TGA analysis of the purified melanin. Interestingly, the current novel endophytic strain was tyrosine-independent, and the uniquely applied ANN paradigm was more efficient in modeling the melanin production with appreciate amount on a simple medium in a relatively short time (168 h), suggesting additional optimization studies for further maximization of melanin production.


Assuntos
Melaninas , Tirosina , Redes Neurais de Computação , Sacarose
10.
Colloids Surf B Biointerfaces ; 230: 113526, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37647750

RESUMO

Loratadine (LRD) belongs to second-generation tricyclic H1 antihistamine class, known for its non-sedating properties in allergic reactions. H1 antihistamines avoid and block the responses to allergens or histamine in nose and conjunctivae, thereby abolishing itching, congestion and sneezing. LRD is a Biopharmaceutical Class System (BCS) class II drug with dissolution or solubility limited absorption which limited the oral bioavailability and therapeutic efficacy of LRD. To improve the oral bioavailability of LRD for allergic disease (urticaria) treatment, LRD solid dispersions (LRD-SDs) were integrating into oro-dispersible films (ODFs). LRD-SDs were prepared through hot-melt extrusion method (HME) using d-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS-1000), and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (SP). Subsequently, LRD-SDs were incorporated in ODFs by solvent casting method. The physicochemical and mechanical properties of LRD solid dispersions-loaded oro-dispersible films (LRD-SDs-ODFs), were evaluated. The in-vitro dissolution, ex-vivo permeation, oral bioavailability, and pharmacodynamics studies were conducted to evaluate LRD-SDs-ODFs efficiency. LRD-SDs-ODFs showed superior solubility and in-vitro dissolution results compared to that of pure LRD (p < 0.05). The solubility of the LRD-SD coded as LTS-4 was 190 times higher than the pure drug in aqueous media. The average hydrodynamic particle size (PS), polydispersity index (PDI), and zeta potential (ZP) of SD particles were 76 ± 2.1 nm, 0.20 ± 0.08 and - 19.16 ± 1.4 mV, respectively. Moreover, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) results confirmed the amorphousness of LRD in LRD-SDs-ODFs. The permeability flux of LRD was 44.6 ± 3.1 µg/cm2/h from DPF-5 formulation. Likewise, in vivo oral bioavailability of DPF-5 in Sprague-Dawley rats was significantly increased (p < 0.05) compared to free LRD. Further, wheal area was reduced 20 % higher than LRD in 8 h (p < 0.05). Overall, LRD-SDs-ODFs considerably enhanced LRD solubility, dissolution rate, bioavailability, and antihistaminic efficacy. Our findings show that SDs-ODFs is an effective carrier system for delivering poorly soluble LRD.


Assuntos
Produtos Biológicos , Loratadina , Ratos , Animais , Ratos Sprague-Dawley , Disponibilidade Biológica , Varredura Diferencial de Calorimetria
11.
Molecules ; 28(10)2023 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-37241888

RESUMO

Quercetin (QtN) displays low systemic bioavailability caused by poor water solubility and instability. Consequently, it exerts limited anticancer action in vivo. One solution to increase the anticancer efficacy of QtN is the use of appropriate functionalized nanocarriers that preferentially target and deliver the drug to the tumor location. Herein, a direct advanced method was designed to develop water-soluble hyaluronic acid (HA)-QtN-conjugated silver nanoparticles (AgNPs). HA-QtN reduced silver nitrate (AgNO3) while acting as a stabilizing agent to produce AgNPs. Further, HA-QtN#AgNPs served as an anchor for folate/folic acid (FA) conjugated with polyethylene glycol (PEG). The resulting PEG-FA-HA-QtN#AgNPs (further abbreviated as PF/HA-QtN#AgNPs) were characterized both in vitro and ex vivo. Physical characterizations included UV-visible (UV-Vis) spectroscopy, Fourier transform infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), particle size (PS) and zeta potential (ZP) measurements, and biopharmaceutical evaluations. The biopharmaceutical evaluations included analyses of the cytotoxic effects on the HeLa and Caco-2 cancer cell lines using the MTT assay; cellular drug intake into cancer cells using flow cytometry and confocal microscopy; and blood compatibility using an automatic hematology analyzer, a diode array spectrophotometer, and an enzyme-linked immunosorbent assay (ELISA). The prepared hybrid delivery nanosystem was hemocompatible and more oncocytotoxic than the free, pure QtN. Therefore, PF/HA-QtN#AgNPs represent a smart nano-based drug delivery system (NDDS) and could be a promising oncotherapeutic option if the data are validated in vivo.


Assuntos
Produtos Biológicos , Nanopartículas Metálicas , Neoplasias , Humanos , Ácido Hialurônico/química , Quercetina/farmacologia , Nanopartículas Metálicas/química , Células CACO-2 , Prata , Polietilenoglicóis/química , Água , Espectroscopia de Infravermelho com Transformada de Fourier
12.
Sci Rep ; 13(1): 5637, 2023 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-37024671

RESUMO

Considered heavy metals, such as As(III), Bi(II), Cd(II), Cr(VI), Mn(II), Mo(II), Ni(II), Pb(II), Sb(III), Se(-II), Zn(II), and contaminating chemical compounds (monocyclic aromatic hydrocarbons such as phenolic or polycyclic derivatives) in wastewater (petrochemical industries: oil and gas production plants) are currently a major concern in environmental toxicology due to their toxic effects on aquatic and terrestrial life. In order to maintain biodiversity, hydrosphere ecosystems, and people, it is crucial to remove these heavy metals and polluting chemical compounds from the watery environment. In this study, different Nanoparticles (α-Fe2O3, CuO, and ZnO) were synthesized by green synthesis method using Portulaca oleracea leaf extract and characterized by UV-Vis spectrophotometers, FTIR spectroscopy, X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM), Energy Dispersive Spectroscopy (EDS) techniques in order to investigate morphology, composition, and crystalline structure of NPs, these were then used as adsorbent for the removal of As(III), Bi(II), Cd(II), Cr(VI), Mn(II), Mo(II), Ni(II), Pb(II), Sb(III), Se(-II), and Zn(II) from wastewater, and removal efficiencies of were obtained 100% under optimal conditions.

13.
Molecules ; 28(4)2023 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-36838699

RESUMO

In this study, pEGFP-LUC was used as a model plasmid and three distinct cationic lipids (dioleyloxy-propyl-trimethylammonium chloride [DOTMA], dioleoyl trimethylammonium propane [DOTAP], and cetylpyridinium chloride [CPC]) were tested along with PEG 5000, as a nonionic surfactant, to prepare glyceryl monostearate (GMS)-based cationic solid lipid nanoparticles (cSLNs). Both the type and quantity of surfactant had an impact on the physicochemical characteristics of the cSLNs. Thermal analysis of the greater part of the endothermic peaks of the cSLNs revealed they were noticeably different from the individual pure compounds based on their zeta potential (ZP ranging from +17 to +56 mV) and particle size (PS ranging from 185 to 244 nm). The addition of cationic surfactants was required to produce nanoparticles (NPs) with a positive surface charge. This suggested that the surfactants and extensive entanglement of the lipid matrix GMS provided support for the behavioral diversity of the cSLNs and their capacity to interface with the plasmid DNA. Additionally, hemolytic assays were used to show that the cSLNs were biocompatible with the human colon cancer HCT-116 and human bronchial epithelial 16-HBE cell lines. The DOTMA 6-based cSLN was selected as the lead cSLN for further ex vivo and in vivo investigations. Taken together, these new findings might provide some guidance in selecting surfactants to prepare extremely efficient and non-toxic cSLN-based therapeutic delivery systems (e.g., gene therapy).


Assuntos
Nanopartículas , Compostos de Amônio Quaternário , Humanos , Compostos de Amônio Quaternário/química , Tensoativos/química , Nanopartículas/química , Cátions
14.
Molecules ; 28(3)2023 Feb 03.
Artigo em Inglês | MEDLINE | ID: mdl-36771180

RESUMO

Wilson's disease causes copper accumulation in the liver and extrahepatic organs. The available therapies aim to lower copper levels by various means. However, a potent drug that can repair the damaged liver and brain tissue is needed. Silymarin has hepatoprotective, antioxidant, and cytoprotective properties. However, poor oral bioavailability reduces its efficacy. In this study, a "thin film hydration method" was used for synthesizing silymarin-encapsulated liposome nanoparticles (SLNPs) and evaluated them against copper toxicity, associated liver dysfunction and neurobehavioral abnormalities in Wistar rats. After copper toxicity induction, serological and behavioral assays were conducted to evaluate treatment approaches. Histological examination of the diseased rats revealed severe hepatocyte necrosis and neuronal vacuolation. These cellular degenerations were mild in rats treated with SLNPs and a combination of zinc and SLNPs (ZSLNPs). SLNPs also decreased liver enzymes and enhanced rats' spatial memory significantly (p = 0.006) in the diseased rats. During forced swim tests, SLNPs treated rats exhibited a 60-s reduction in the immobility period, indicating reduced depression. ZSLNPs were significantly more effective than traditional zinc therapy in decreasing the immobility period (p = 0.0008) and reducing liver enzymes, but not in improving spatial memory. Overall, SLNPs enhanced oral silymarin administration and managed copper toxicity symptoms.


Assuntos
Degeneração Hepatolenticular , Silimarina , Ratos , Animais , Ratos Wistar , Silimarina/uso terapêutico , Cobre/farmacologia , Lipossomos/farmacologia , Fígado , Degeneração Hepatolenticular/tratamento farmacológico , Zinco/farmacologia , Zinco/uso terapêutico
16.
Pharmaceutics ; 14(12)2022 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-36559181

RESUMO

Rizatriptan (RZT) is an efficient anti-migraine drug which belongs to the class of selective 5 HT (1B/1D) serotonin receptor agonists. Nevertheless, RZT elicits several adverse effects and RZT nasal sprays have a limited half-life, requiring repeated doses that could cause patient noncompliance or harm to the nasopharynx and cilia. The current research aimed to develop orally disintegrating films (ODFs) of RZT employing maltodextrin (MTX) and pullulan (PUL) as film-forming polymers, as well as propylene glycol (PG) as a plasticizer. The ODFs were prepared by solvent casting method (SCM). The technique was optimized using Box-Behnken design (BBD), contemplating the ratios of PUL: MTX and different levels of PG (%) as factor variables. The influence of these factors was systematically analyzed on the selected dependent variables, including film thickness, disintegration time (D-time), folding endurance (FE), tensile strength (TS), percent elongation (%E), moisture content (%), and water uptake (%). In addition, the surface morphology, solid state analysis, drug content uniformity (%), drug release (%), and pH of the RZT-ODFs were also studied. The results demonstrated a satisfactory stable RZT-ODFs formulation that exhibited surface homogeneity and amorphous RZT in films with no discernible interactions between the model drug and polymeric materials. The optimized film showed a rapid D-time of 16 s and remarkable mechanical features. The in vitro dissolution kinetics showed that 100% RZT was released from optimized film compared to 61% RZT released from conventional RZT formulation in the initial 5 min. An animal pharmacokinetic (PK) investigation revealed that RZT-ODFs had a shorter time to achieve peak plasma concentration (Tmax), a higher maximum plasma concentration (Cmax), and area under the curve (AUC0-t) than traditional oral mini capsules. These findings proposed a progressive approach for developing anti-migraine drugs that could be useful in reducing the complications of dysphagia in geriatric and pediatric sufferers.

17.
Int J Mol Sci ; 23(24)2022 Dec 14.
Artigo em Inglês | MEDLINE | ID: mdl-36555575

RESUMO

Antibacterial restorative materials against caries-causing bacteria are highly preferred among high-risk patients, such as the elderly, and patients with metabolic diseases such as diabetes. This study aimed to enhance the antibacterial potential of resin composite with Magnesium-doped Zinc oxide (Mg-doped ZnO) nanoparticles (NPs) and to look for their effectiveness in the alloxan-induced diabetic model. Hexagonal Mg-doped ZnO NPs (22.3 nm diameter) were synthesized by co-precipitation method and characterized through ultraviolet-visible (UV-Vis), Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), scanning electron microscopy (SEM), and energy dispersive spectroscopy (EDS) analysis. The Mg-doped ZnO NPs (1, 2.5 and 5% w/w) were then evaluated for antibacterial activity using a closed system in vitro biofilm model. Significant enhancement in the antibacterial properties was observed in composites with 1% Mg-doped ZnO compared to composites with bare ZnO reinforced NPs (Streptococcus mutans, p = 0.0005; Enterococcus faecalis, p = 0.0074, Saliva microcosm, p < 0.0001; Diabetic Saliva microcosm, p < 0.0001). At 1−2.5% Mg-doped ZnO NPs concentration, compressive strength and biocompatibility of composites were not affected. The pH buffering effect was also achieved at these concentrations, hence not allowing optimal conditions for the anaerobic bacteria to grow. Furthermore, composites with Mg-doped ZnO prevented secondary caries formation in the secondary caries model of alloxan-induced diabetes. Therefore, Mg-doped ZnO NPs are highly recommended as an antibacterial agent for resin composites to avoid biofilm and subsequent secondary caries formation in high-risk patients.


Assuntos
Diabetes Mellitus , Nanopartículas Metálicas , Nanopartículas , Óxido de Zinco , Humanos , Idoso , Óxido de Zinco/farmacologia , Óxido de Zinco/química , Zinco , Aloxano , Magnésio/farmacologia , Óxido de Magnésio/farmacologia , Óxido de Magnésio/uso terapêutico , Suscetibilidade à Cárie Dentária , Nanopartículas/química , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Antibacterianos/química , Nanopartículas Metálicas/química , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X , Testes de Sensibilidade Microbiana
18.
Molecules ; 27(23)2022 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-36500511

RESUMO

Background: Nickel stannate nanocomposites could be useful for removing organic and toxic water pollutants, such as methyl orange (MO). Aim: The synthesis of a nickel oxide-tin oxide nanocomposite (NiO-SnO2 NC) via a facile and economically viable approach using a leaf extract from Ficus elastica for the photocatalytic degradation of MO. Methods: The phase composition, crystallinity, and purity were examined by X-ray diffraction (XRD). The particles' morphology was studied using scanning electron microscopy (SEM). The elemental analysis and colored mapping were carried out via energy dispersive X-ray (EDX). The functional groups were identified by Fourier transform infrared spectroscopy (FTIR). UV-visible diffuse reflectance spectroscopy (UV-vis DRS) was used to study the optical properties such as the absorption edges and energy band gap, an important feature of semiconductors to determine photocatalytic applications. The photocatalytic activity of the NiO-SnO2 NC was evaluated by monitoring the degradation of MO in aqueous solution under irradiation with full light spectrum. The effects of calcination temperature, pH, initial MO concentration, and catalyst dose were all assessed to understand and optimize the physicochemical and photocatalytic properties of NiO-SnO2 NC. Results: NiO-SnO2 NC was successfully synthesized via a biological route using F. elastica leaf extract. XRD showed rhombohedral NiO and tetragonal SnO2 nanostructures and the amorphous nature of NiO-SnO2 NC. Its degree of crystallinity, crystallite size, and stability increased with increased calcination temperature. SEM depicted significant morphological changes with elevating calcination temperatures, which are attributed to the phase conversion from amorphous to crystalline. The elemental analysis and colored mapping show the formation of highly pure NiO-SnO2 NC. FTIR revealed a decrease in OH, and the ratio of oxygen vacancies at the surface of the NC can be explained by a loss of its hydrophilicity at increased temperatures. All the NC samples displayed significant absorption in the visible region, and a blue shift is seen and the energy band gap decreases when increasing the calcination temperatures due to the dehydration and formation of compacted large particles. NiO-SnO2 NC degrades MO, and the photocatalytic performance decreased with increasing calcination temperature due to an increase in the crystallite size of the NC. The optimal conditions for the efficient NC-mediated photocatalysis of MO are 100 °C, 20 mg catalyst, 50 ppm MO, and pH 6. Conclusions: The auspicious performance of the NiO-SnO2 NCs may open a new avenue for the development of semiconducting p-n heterojunction catalysts as promising structures for removing undesirable organic pollutants from the environment.


Assuntos
Compostos Azo , Nanocompostos , Compostos Azo/química , Nanocompostos/química , Catálise , Extratos Vegetais
19.
Molecules ; 27(24)2022 Dec 17.
Artigo em Inglês | MEDLINE | ID: mdl-36558144

RESUMO

This study aimed to establish the phytochemical profile of Glochidion velutinum and its cytotoxic activity against prostate cancer (PC-3) and breast cancer (MCF-7) cell lines. The phytochemical composition of G. velutinum leaf extract and its fractions was established with the help of total phenolic and flavonoid contents and LC-MS/MS-based metabolomics analysis. The crude methanolic extract and its fractions were studied for pharmacological activity against PC-3 and MCF-7 cell lines using the MTT assay. The total phenolic content of the crude extract and its fractions ranged from 44 to 859 µg GAE/mg of sample whereas total flavonoid contents ranged from 20 to 315 µg QE/mg of sample. A total of forty-eight compounds were tentatively dereplicated in the extract and its fractions. These phytochemicals included benzoic acid derivatives, flavans, flavones, O-methylated flavonoids, flavonoid O- and C-glycosides, pyranocoumarins, hydrolysable tannins, carbohydrate conjugates, fatty acids, coumarin glycosides, monoterpenoids, diterpenoids, and terpene glycosides. The crude extract (IC50 = 89 µg/mL), the chloroform fraction (IC50 = 27 µg/mL), and the water fraction (IC50 = 36 µg/mL) were found to be active against the PC-3 cell line. However, the crude extract (IC50 = 431 µg/mL), the chloroform fraction (IC50 = 222 µg/mL), and the ethyl acetate fraction (IC50 = 226 µg/mL) have shown prominent activity against breast cancer cells. Moreover, G. velutinum extract and its fractions presented negligible toxicity to normal macrophages at the maximum tested dose (600 µg/mL). Among the compounds identified through LC-MS/MS-based metabolomics analysis, epigallocatechin gallate, ellagic acid, isovitexin, and rutin were reported to have anticancer activity against both prostate and breast cancer cell lines and might be responsible for the cytotoxic activities of G. velutinum extract and its bioactive fractions.


Assuntos
Neoplasias da Mama , Malpighiales , Humanos , Feminino , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Cromatografia Líquida , Antioxidantes/química , Clorofórmio , Espectrometria de Massas em Tandem , Células MCF-7 , Neoplasias da Mama/metabolismo , Flavonoides/farmacologia , Flavonoides/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Glicosídeos
20.
Materials (Basel) ; 15(22)2022 Nov 18.
Artigo em Inglês | MEDLINE | ID: mdl-36431686

RESUMO

Herein, zinc oxide nanoparticles (ZnO NPs) were greenly synthesized from Tridax procumbens aqueous leaf extract (TPE) and characterized physically (e.g., Fourier-transform infrared (FTIR) spectroscopy and scanning electron microscopy (SEM)) and biologically (test of their anti-diabetic activity). Anti-diabetic activities of TPE and TPE-derived ZnO NPs have been carried out in a streptozotocin (STZ)­induced diabetic rat model. Diabetes mellitus (DM) was induced with a single intraperitoneal dosage of the glucose analogue STZ (55 mg/Kg) known to be particularly toxic to pancreatic insulin-producing beta-cells. TPE and TPE-derived ZnO NPs were administered orally, once every day for 21 days in diabetic rats, at 100 and 200 mg/Kg, respectively. The standard antidiabetic medication, glibenclamide, was used as a control at a dose of 10 mg/Kg. Various parameters were investigated, including bodyweight (bw) variations, glycemia, lipidaemia, glycated hemoglobin (HbA1c), and histopathological alterations in the rat's liver and pancreas. The TPE-mediated NPs were small, spherical, stable, and uniform. Compared to TPE and, to a lesser extent, glibenclamide, TPE-derived ZnO NPs lowered blood glucose levels considerably (p < 0.05) and in a dose-dependent manner while preventing body weight loss. Further, positive benefits for both the lipid profile and glycated hemoglobin were also noticed with TPE-derived ZnO NPs. The histopathological assessment revealed that synthesized TPE-derived ZnO NPs are safe, non-toxic, and biocompatible. At 200 mg/Kg/day, TPE-derived ZnO NPs had a more substantial hypoglycemic response than at 100 mg/Kg/day. Thus, in this first reported experimental setting, ZnO NPs biosynthesized from the leaf extract of Tridax procumbens exert more potent anti-diabetic activity than TPE and glibenclamide. We conclude that such a greenly prepared nanomaterial may be a promising alternative or complementary (adjuvant) therapy, at least to the current Indian's traditional medicine system. Translational findings are prompted in human populations to determine the efficacy of these NPs.

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