Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 42
Filtrar
Más filtros

Banco de datos
Tipo del documento
Intervalo de año de publicación
1.
Molecules ; 28(18)2023 Sep 07.
Artículo en Inglés | MEDLINE | ID: mdl-37764280

RESUMEN

Green approaches for nanoparticle synthesis have emerged as biocompatible, economical, and environment-friendly alternatives to counteract the menace of microbial drug resistance. Recently, the utilization of honey as a green source to synthesize Fe2O3-NPs has been introduced, but its antibacterial activity against one of the opportunistic MDR pathogens, Klebsiella pneumoniae, has not been explored. Therefore, this study employed Apis mellifera honey as a reducing and capping agent for the synthesis of iron oxide nanoparticles (Fe2O3-NPs). Subsequent to the characterization of nanoparticles, their antibacterial, antioxidant, and anti-inflammatory properties were appraised. In UV-Vis spectroscopic analysis, the absorption band ascribed to the SPR peak was observed at 350 nm. XRD analysis confirmed the crystalline nature of Fe2O3-NPs, and the crystal size was deduced to be 36.2 nm. Elemental analysis by EDX validated the presence of iron coupled with oxygen in the nanoparticle composition. In ICP-MS, the highest concentration was of iron (87.15 ppm), followed by sodium (1.49 ppm) and other trace elements (<1 ppm). VSM analysis revealed weak magnetic properties of Fe2O3-NPs. Morphological properties of Fe2O3-NPs revealed by SEM demonstrated that their average size range was 100-150 nm with a non-uniform spherical shape. The antibacterial activity of Fe2O3-NPs was ascertained against 30 clinical isolates of Klebsiella pneumoniae, with the largest inhibition zone recorded being 10 mm. The MIC value for Fe2O3-NPs was 30 µg/mL. However, when mingled with three selected antibiotics, Fe2O3-NPs did not affect any antibacterial activity. Momentous antioxidant (IC50 = 22 µg/mL) and anti-inflammatory (IC50 = 70 µg/mL) activities of Fe2O3-NPs were discerned in comparison with the standard at various concentrations. Consequently, honey-mediated Fe2O3-NP synthesis may serve as a substitute for orthodox antimicrobial drugs and may be explored for prospective biomedical applications.


Asunto(s)
Miel , Abejas , Animales , Antioxidantes/farmacología , Estudios Prospectivos , Antibacterianos/farmacología , Hierro , Klebsiella pneumoniae , Nanopartículas Magnéticas de Óxido de Hierro
2.
Int J Mol Sci ; 23(3)2022 Jan 28.
Artículo en Inglés | MEDLINE | ID: mdl-35163422

RESUMEN

Aging is a complex process indicated by low energy levels, declined physiological activity, stress induced loss of homeostasis leading to the risk of diseases and mortality. Recent developments in medical sciences and an increased availability of nutritional requirements has significantly increased the average human lifespan worldwide. Several environmental and physiological factors contribute to the aging process. However, about 40% human life expectancy is inherited among generations, many lifespan associated genes, genetic mechanisms and pathways have been demonstrated during last decades. In the present review, we have evaluated many human genes and their non-human orthologs established for their role in the regulation of lifespan. The study has included more than fifty genes reported in the literature for their contributions to the longevity of life. Intact genomic DNA is essential for the life activities at the level of cell, tissue, and organ. Nucleic acids are vulnerable to oxidative stress, chemotherapies, and exposure to radiations. Efficient DNA repair mechanisms are essential for the maintenance of genomic integrity, damaged DNA is not replicated and transferred to next generations rather the presence of deleterious DNA initiates signaling cascades leading to the cell cycle arrest or apoptosis. DNA modifications, DNA methylation, histone methylation, histone acetylation and DNA damage can eventually lead towards apoptosis. The importance of calorie restriction therapy in the extension of lifespan has also been discussed. The role of pathways involved in the regulation of lifespan such as DAF-16/FOXO (forkhead box protein O1), TOR and JNK pathways has also been particularized. The study provides an updated account of genetic factors associated with the extended lifespan and their interactive contributory role with cellular pathways.


Asunto(s)
Envejecimiento/genética , Daño del ADN , Redes Reguladoras de Genes , Animales , Apoptosis , Humanos , Longevidad , Estrés Fisiológico
3.
Molecules ; 27(4)2022 Feb 21.
Artículo en Inglés | MEDLINE | ID: mdl-35209242

RESUMEN

The objective of the current research is to develop ZnO-Manjistha extract (ZnO-MJE) nanoparticles (NPs) and to investigate their transdermal delivery as well as antimicrobial and antioxidant activity. The optimized formulation was further evaluated based on different parameters. The ZnO-MJE-NPs were prepared by mixing 10 mM ZnSO4·7H2O and 0.8% w/v NaOH in distilled water. To the above, a solution of 10 mL MJE (10 mg) in 50 mL of zinc sulfate was added. Box-Behnken design (Design-Expert software 12.0.1.0) was used for the optimization of ZnO-MJE-NP formulations. The ZnO-MJE-NPs were evaluated for their physicochemical characterization, in vitro release activity, ex vivo permeation across rat skin, antimicrobial activity using sterilized agar media, and antioxidant activity by the DPPH free radical method. The optimized ZnO-MJE-NP formulation (F13) showed a particle size of 257.1 ± 0.76 nm, PDI value of 0.289 ± 0.003, and entrapment efficiency of 79 ± 0.33%. Drug release kinetic models showed that the formulation followed the Korsmeyer-Peppas model with a drug release of 34.50 ± 2.56 at pH 7.4 in 24 h. In ex vivo studies ZnO-MJE-NPs-opt permeation was 63.26%. The antibacterial activity was found to be enhanced in ZnO-MJE-NPs-opt and antioxidant activity was found to be highest (93.14 ± 4.05%) at 100 µg/mL concentrations. The ZnO-MJE-NPs-opt formulation showed prolonged release of the MJE and intensified permeation. Moreover, the formulation was found to show significantly (p < 0.05) better antimicrobial and antioxidant activity as compared to conventional suspension formulations.


Asunto(s)
Antiinfecciosos/farmacología , Antioxidantes/farmacología , Nanopartículas del Metal/química , Extractos Vegetales/química , Rubia/química , Piel/efectos de los fármacos , Óxido de Zinc/química , Animales , Antiinfecciosos/química , Antioxidantes/química , Fenómenos Químicos , Química Farmacéutica , Composición de Medicamentos , Liberación de Fármacos , Estabilidad de Medicamentos , Pruebas de Sensibilidad Microbiana , Modelos Químicos , Ratas , Piel/metabolismo , Análisis Espectral
4.
Molecules ; 27(9)2022 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-35566224

RESUMEN

Isopropyl Isothiocyanate (IPI) is a poorly water-soluble drug used in different biological activities. So, the present work was designed to prepare and evaluate IPI loaded vesicles and evaluated for vesicle size, polydispersity index (PDI) and zeta potential, encapsulation efficiency, drug release, and drug permeation. The selected formulation was coated with chitosan and further assessed for the anti-platelet and anti-thrombotic activity. The prepared IPI vesicles (F3) exhibited a vesicle size of 298 nm ± 5.1, the zeta potential of −18.7 mV, encapsulation efficiency of 86.2 ± 5.3% and PDI of 0.33. The chitosan-coated IPI vesicles (F3C) exhibited an increased size of 379 ± 4.5 nm, a positive zeta potential of 23.5 ± 2.8 mV and encapsulation efficiency of 77.3 ± 4.1%. IPI chitosan vesicle (F3C) showed enhanced mucoadhesive property (2.7 folds) and intestinal permeation (~1.8-fold) higher than IPI vesicles (F3). There was a significant (p < 0.05) enhancement in size, muco-adhesion, and permeation flux achieved after coating with chitosan. The IPI chitosan vesicle (F3C) demonstrated an enhanced bleeding time of 525.33 ± 12.43 s, anti-thrombin activity of 59.72 ± 4.21, and inhibition of platelet aggregation 68.64 ± 3.99%, and anti-platelet activity of 99.47%. The results of the study suggest that IPI chitosan vesicles showed promising in vitro results, as well as improved anti-platelet and anti-thrombotic activity compared to pure IPI and IPI vesicles.


Asunto(s)
Quitosano , Nanopartículas , Portadores de Fármacos , Sistemas de Liberación de Medicamentos , Liberación de Fármacos , Isotiocianatos , Sistema de Administración de Fármacos con Nanopartículas , Tamaño de la Partícula
5.
Molecules ; 27(14)2022 Jul 13.
Artículo en Inglés | MEDLINE | ID: mdl-35889343

RESUMEN

The nano-drug delivery system has gained greater acceptability for poorly soluble drugs. Alogliptin (ALG) is a FDA-approved oral anti-hyperglycemic drug that inhibits dipeptidyl peptidase-4. The present study is designed to prepare polymeric ALG nanoparticles (NPs) for the management of diabetes. ALG-NPs were prepared using the nanoprecipitation method and further optimized by Box−Behnken experimental design (BBD). The formulation was optimized by varying the independent variables Eudragit RSPO (A), Tween 20 (B), and sonication time (C), and the effects on the hydrodynamic diameter (Y1) and entrapment efficiency (Y2) were evaluated. The optimized ALG-NPs were further evaluated for in vitro release, intestinal permeation, and pharmacokinetic and anti-diabetic activity. The prepared ALG-NPs show a hydrodynamic diameter of between 272.34 nm and 482.87 nm, and an entrapment efficiency of between 64.43 and 95.21%. The in vitro release data of ALG-NPs reveals a prolonged release pattern (84.52 ± 4.1%) in 24 h. The permeation study results show a 2.35-fold higher permeation flux than pure ALG. ALG-NPs exhibit a significantly (p < 0.05) higher pharmacokinetic profile than pure ALG. They also significantly (p < 0.05) reduce the blood sugar levels as compared to pure ALG. The findings of the study support the application of ALG-entrapped Eudragit RSPO nanoparticles as an alternative carrier for the improvement of therapeutic activity.


Asunto(s)
Portadores de Fármacos , Nanopartículas , Tamaño de la Partícula , Piperidinas , Polímeros , Uracilo/análogos & derivados
6.
AAPS PharmSciTech ; 23(2): 71, 2022 Feb 10.
Artículo en Inglés | MEDLINE | ID: mdl-35146576

RESUMEN

The current investigation was performed with an aim to improve the aqueous solubility, dissolution rate, and thus the biological activity of apigenin (APG) using the solubilizers hydroxypropyl beta-cyclodextrin (HPßCD) and chitosan (CTSN). A binary and ternary inclusion complexes of APG with HPßCD and CTSN were prepared by physical mixing, fusion, and solvent evaporation methods. The liquid state characterization of the APG, the solubilizers, and the physical and chemical interactions between them was done through phase solubility approach. The solid-state characterization was performed by proton nuclear magnetic resonance (1H-NMR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD). The in vitro dissolution test and antioxidant activity and in vivo anti-inflammatory activity of the ternary inclusion complex in albino rats were performed to assess the performance of the APG. Phase solubility study results revealed a remarkable increase in apparent stability constant (Kc) and complexation efficiency (CE) of HPßCD in presence of CTSN in ternary complex with above 8 folds more increment in solubility of APG than its binary complex. The in vitro dissolution rate, antioxidant activity, and the anti-inflammatory effect of the APG ternary inclusion complex were found to be significantly higher than that of pure APG. Solid state characterization confirmed the formation of a ternary inclusion complex. 1H-NMR study gave more insight at molecular level into how different groups of APG were responsible for complex formation with the HPßCD and how CTSN was significantly influencing on the APG-HPßCD complex formed. Nevertheless, pharmacokinetic and histopathological studies of our APG-HPßCD-CTSN ternary complex would yield much rewarding results.


Asunto(s)
Quitosano , Ciclodextrinas , beta-Ciclodextrinas , 2-Hidroxipropil-beta-Ciclodextrina , Apigenina , Rastreo Diferencial de Calorimetría , Solubilidad , Difracción de Rayos X , Animales , Ratas
7.
Molecules ; 26(11)2021 May 29.
Artículo en Inglés | MEDLINE | ID: mdl-34072306

RESUMEN

The present research work is designed to prepare and evaluate piperine liposomes and piperine-chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (-7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.


Asunto(s)
Alcaloides/química , Benzodioxoles/química , Quitosano/química , Liposomas/química , Piperidinas/química , Alcamidas Poliinsaturadas/química , Antineoplásicos/química , Antioxidantes/química , Adhesión Celular , Supervivencia Celular , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos , Liberación de Fármacos , Humanos , Técnicas In Vitro , Concentración 50 Inhibidora , Células MCF-7 , Microscopía Electrónica de Transmisión , Tamaño de la Partícula , Permeabilidad , Espectroscopía Infrarroja por Transformada de Fourier
8.
J Liposome Res ; 30(4): 377-387, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31412744

RESUMEN

The present study was designed with an aim to develop and optimize naproxen proniosomes (NAPRNs) using Box-Behnken Design (BBD). The formulation was optimized using three independent variables [maltodextrin (X1), surfactant concentration (X2) and drug concentration (X3)] at three different levels (low, medium and high). The prepared fifteen formulations were evaluated for drug entrapment efficiency, vesicle size and transdermal flux to select the optimized naproxen niosomes (NAPRNopt). The developed NAPRNs formulations showed the nano-size vesicle (218-417 nm) and high encapsulation efficiency (60.48-92.48%) with high flux value (23.17-27.37 µg/cm2/h). The formulation NAPRNopt has shown the vesicle size of 376.12 ± 4.12 nm with entrapment efficiency 86.43 ± 3.63% and transdermal flux of 27.56 ± 1.43 µg/cm2/h. The SEM study revealed the formulation NAPRNopt showed irregular surface morphology of niosomes. The formulation NAPRNopt gel showed biphasic release behaviour as an initial fast release and later slower release with the Higuchi release mechanism. The anti-inflammatory study results showed a better effect than the standard NAP gel in the rat model.


Asunto(s)
Sistemas de Liberación de Medicamentos/métodos , Liposomas/metabolismo , Naproxeno/metabolismo , Absorción Cutánea , Piel/metabolismo , Administración Cutánea , Algoritmos , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/farmacocinética , Carragenina , Liberación de Fármacos , Edema/inducido químicamente , Edema/prevención & control , Cinética , Liposomas/farmacocinética , Liposomas/ultraestructura , Microscopía Electrónica de Rastreo , Naproxeno/farmacocinética , Tamaño de la Partícula , Ratas
9.
Drug Dev Ind Pharm ; 46(9): 1524-1534, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32808552

RESUMEN

This research planned to ameliorate an aqueous solubility and dissolution of Curcumin (CUR) by the formulation of inclusion complex with ß-cyclodextrin (ß-CD) and polyvinylpyrrolidone (PVP). The phase solubility study was performed to assess the solubility of CUR. The prepared CUR complex assessed for dissolution study, physicochemical evaluation, in-vitro antioxidant activity, molecular modeling, and anti-inflammatory assessment. The pivotal findings of phase-solubility studies demonstrate apparent stability constant (Kc) and complexation efficiency (CE) values for CUR-ß-CD and CUR-ß-CD-PVP complex was 175.4 M -1, 1.15% and 833.3.2 M -1 and 5.21%, respectively. The characterization results revealed amorphization of crystalline state (CUR) into amorphous state. The maximum drug release found with the ternary CUR complex (F7), i.e. 45.41 ± 3.78% in 6 h study. The chemical shift in the NMR supports that the aromatic ring of CUR is completely complexed inside the ß-CD cavity. The antioxidant activity of pure CUR was found to be 58.02 ± 2.21% and CUR ternary complex (F7) showed significantly higher activity to 96.02 ± 2.46%. The in-vivo effect of CUR complex (F7) was also found significantly higher than that of pure CUR. The molecular modeling study depicted that PVP increased the stability of the ternary complex by forming the link between CUR and ß-CD. Thus, the ternary inclusion complex of CUR-ß-CD-PVP could contribute as an innovative outcome in the enhancement of solubility and in-vivo activity.


Asunto(s)
Antiinflamatorios/farmacología , Curcumina , Povidona/química , beta-Ciclodextrinas , Antiinflamatorios/química , Simulación del Acoplamiento Molecular , Solubilidad
10.
Drug Dev Ind Pharm ; 45(11): 1799-1806, 2019 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-31448962

RESUMEN

A rapid, accurate, and sensitive reverse phase high-performance liquid chromatographic (RP-HPLC) method was developed and validated for the estimation of Thymoquinone (TMQ) in API as well as in noisome. The chromatograms were developed with the mobile phase - water: 2-propanol: methanol (50:45:5 v/v/v) as a solvent system at 254 nm. The method was validated as per ICH guidelines for different parameters and the recovery of TMQ was calculated in developed niosomes. Further, TMQ loaded niosomes (TMQNIOS) were prepared and evaluated for different parameters. The optimized TMQNIOS (F3) was further evaluated for surface morphology, in vitro drug release, permeation study, and confocal laser scanning microscopic (CLSM) study. The method showed linearity range between 6.25 and 100 µg/ml with low detection limit and quantitation limit with a value of 2.08 and 6.25 µg/ml. The developed formulations showed the vesicle size and encapsulation efficiency in the range of 157.32 ± 3.15 to 211.44 ± 5.23 nm and 59.32 ± 4.87 to 83.21 ± 3.55%, respectively. The drug release result showed the significant higher release from TMQNIOS in compared to TMQDIS, and the release kinetics data showed Higuchi's equation with highest regression coefficient values. The permeation study and the confocal laser microscopy study further confirmed the enhancement in permeation of TMQ in the intestinal mucosa.


Asunto(s)
Benzoquinonas/análisis , Benzoquinonas/farmacocinética , Química Farmacéutica/métodos , Animales , Benzoquinonas/administración & dosificación , Cromatografía Líquida de Alta Presión/métodos , Cromatografía de Fase Inversa/métodos , Composición de Medicamentos , Liberación de Fármacos , Cabras , Mucosa Intestinal/diagnóstico por imagen , Mucosa Intestinal/metabolismo , Liposomas , Microscopía Confocal , Tamaño de la Partícula , Permeabilidad
11.
ACS Omega ; 9(14): 15882-15892, 2024 Apr 09.
Artículo en Inglés | MEDLINE | ID: mdl-38617686

RESUMEN

In the present study, ZnO nanoparticles were synthesized by using aqueous extracts of Aerva persica roots. Characterization of as-prepared ZnO nanoparticles was carried out using different techniques, including powder X-ray diffraction (XRD), UV-vis diffuse reflectance spectroscopy (DRS), Fourier transform infrared (FTIR) spectroscopy, field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM) and BET surface area analysis. Morphological analysis confirmed the small, aggregated flake-shaped morphology of as-synthesized ZnO nanostructures. The as-prepared ZnO nanoparticles were analyzed for their potential application as anti-inflammatory (using in vivo inhibition of carrageenan induced paw edema) and antioxidant (using in vitro radical scavenging activity) agents. The ZnO nanoparticles were found to have a potent antioxidant and anti-inflammatory activity comparable to that of standard ascorbic acid (antioxidant) and indomethacin (anti-inflammatory drug). Therefore, due to their ecofriendly synthesis, nontoxicity, and biocompatible nature, zinc oxide nanoparticles synthesized successfully from roots extract of the plant Aerva persica with potent efficiencies can be utilized for different biomedical applications.

12.
PeerJ ; 12: e16795, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38313003

RESUMEN

This study explores the neuroprotective potential of hibiscetin concerning memory deficits induced by lipopolysaccharide (LPS) injection in rats. The aim of this study is to evaluate the effect of hibiscetin against LPS-injected memory deficits in rats. The behavioral paradigms were conducted to access LPS-induced memory deficits. Various biochemical parameters such as acetyl-cholinesterase activity, choline-acetyltransferase, antioxidant (superoxide dismutase, glutathione transferase, catalase), oxidative stress (malonaldehyde), and nitric oxide levels were examined. Furthermore, neuroinflammatory parameters such as tumor necrosis factor-α, interleukin-1ß (IL-1ß), IL-6, and nuclear factor-kappa B expression and brain-derived neurotrophic factor as well as apoptosis marker i.e., caspase-3 were evaluated. The results demonstrated that the hibiscetin-treated group exhibited significant recovery in LPS-induced memory deficits in rats by using behavioral paradigms, biochemical parameters, antioxidant levels, oxidative stress, neuroinflammatory markers, and apoptosis markers. Recent research suggested that hibiscetin may serve as a promising neuroprotective agent in experimental animals and could offer an alternative in LPS-injected memory deficits in rodent models.


Asunto(s)
Productos Biológicos , Trastornos de la Memoria , FN-kappa B , Animales , Ratas , Antioxidantes/metabolismo , Factor Neurotrófico Derivado del Encéfalo/metabolismo , Caspasa 3/metabolismo , Lipopolisacáridos/toxicidad , Trastornos de la Memoria/inducido químicamente , Trastornos de la Memoria/tratamiento farmacológico , FN-kappa B/metabolismo , Productos Biológicos/farmacología
13.
ACS Omega ; 8(46): 44183-44194, 2023 Nov 21.
Artículo en Inglés | MEDLINE | ID: mdl-38027324

RESUMEN

Piperine (PPN) is a natural alkaloid derived from black pepper (Piper nigrum L.) and has garnered substantial attention for its potential in breast cancer therapy due to its diverse pharmacological properties. However, its highly lipophilic characteristics and poor dissolution in biological fluids limit its clinical application. Therefore, to overcome this limitation, we formulate and evaluate PPN-encapsulated polycaprolactone (PCL) nanoparticles (PPN-PCL-NPs). The nanoparticles were prepared by a single-step nanoprecipitation method and further optimized by a formulation design approach. The influence of selected independent variables PCL (X1), poloxamer 188 (P-188; X2), and stirring speed (SS; X3) were investigated on the particle size (PS), polydispersity index (PDI), and % encapsulation efficiency (EE). The selected optimized nanoparticles were further assessed for stability, in vitro release, and in vitro antibreast cancer activity in the MCF-7 cancer cell line. The PS, PDI, zeta potential, and % EE of the optimized PPN-PCL-NPs were observed to be 107.61 ± 5.28 nm, 0.136 ± 0.011, -20.42 ± 1.82 mV, and 79.53 ± 5.22%, respectively. The developed PPN-PCL-NPs were stable under different temperature conditions with insignificant changes in their pharmaceutical attributes. The optimized PPN-PCL-NPs showed a burst release for the first 6 h and later showed sustained release for 48 h. The PPN-PCL-NPs exhibit exceptional cytotoxic effects in MCF-7 breast tumor cells in comparison with the native PPN. Thus, the formulation of PPN-loaded PCL-NPs can be a promising approach for better therapeutic efficacy against breast cancer.

14.
Pharmaceutics ; 15(2)2023 Feb 08.
Artículo en Inglés | MEDLINE | ID: mdl-36839903

RESUMEN

Miconazole nitrate (MN) is a poorly water-soluble and antifungal drug used for fungal infections. The present research work was designed to develop topical MN-loaded bilosomes (BSs) for the improvement of therapeutic efficacy. MZBSs were prepared by using the thin-film hydration method and further optimized by using the Box-Behnken statistical design (BBD). The optimized miconazole bilosome (MZBSo) showed nano-sized vesicles, a low polydispersity index, a high entrapment efficiency, and zeta potential. Further, MZBSo was incorporated into the gel using carbopol 934P and chitosan polymers. The selected miconazole bilosome gel (MZBSoG2) demonstrated an acceptable pH (6.4 ± 0.1), viscosity (1856 ± 21 cP), and spreadability (6.6 ± 0.2 cm2). Compared to MZBSo (86.76 ± 3.7%), MZBSoG2 showed a significantly (p < 0.05) slower drug release (58.54 ± 4.1%). MZBSoG2 was found to be a non-irritant because it achieved a score of zero (standard score) in the HET-CAM test. It also exhibited significant antifungal activity compared to pure MZ against Candida albicans and Aspergillus niger. The stability study results showed no significant changes after stability testing under accelerated conditions. MZ-loaded gels could serve as effective alternative carriers for improving therapeutic efficacy.

15.
Cent Nerv Syst Agents Med Chem ; 23(2): 126-136, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37608652

RESUMEN

BACKGROUND: The primary phytoconstituents reported to have neuroprotective effects are flavonoids and phenolic compounds. Aerva persica roots are reported to be rich in flavonoids and phenolic compounds. Therefore, this study aimed to explore the nootropic potential of Aerva persica roots. OBJECTIVE: The objective of this study was to evaluate the nootropic potential of Aerva persica roots against D-galactose-induced memory impairment. METHODS: In this study, the roots of Aerva persica were extracted with 70% ethanol. The obtained extract was evaluated for total phenolic content using the Folin-Ciocalteu method and total flavonoid content using the aluminium chloride colorimetric assay. Afterward, the acute oral toxicity of the extract was determined following the Organisation for Economic Co-operation and Development (OECD) guideline 423. Additionally, two doses of Aerva persica (100 and 200 mg/kg body weight (BW)) were evaluated for their nootropic potential against D-galactose-induced memory impairment. The nootropic potential of the crude extract was assessed through a behavioural study and brain neurochemical analysis. Behavioural studies involved the evaluation of spatial reference- working memory using the radial arm maze test and the Y-maze test. Neurochemical analysis was performed to determine the brain's acetylcholine, acetylcholinesterase, glutathione (GSH), and malondialdehyde (MDA) levels. RESULTS: The total phenolic content and total flavonoid content were found to be 179.14 ± 2.08 µg GAE/mg and 273.72 ± 3.94 µg QE/mg, respectively. The Aerva persica extract was found to be safe up to 2000 mg/kg BW. Following the safety assessment, the experimental mice received various treatments for 14 days. The behavioural analysis using the radial maze test showed that the extract at both doses significantly improved spatial reference-working memory and reduced the number of total errors compared to disease control groups. Similarly, in the Y-maze test, both doses significantly increased the alteration percentage and the percentage of novel arm entry (both indicative of intact spatial memory) compared to disease control. In neurochemical analysis, Aerva persica at 200 mg/kg significantly normalised the acetylcholine level (p<0.0001) and GSH level (p<0.01) compared to disease control. However, the same effect was not observed with Aerva persica at 100 mg/kg. Additionally, Aerva persica at 200mg/kg BW significantly decreased the acetylcholinesterase level (p<0.0001) and decreased the brain's MDA level (p<0.01) compared to the disease control, whereas the effect of Aerva persica at 100 mg/kg BW in reducing acetylcholinesterase was non-significant. CONCLUSION: Based on the results, it can be concluded that the nootropic potential of Aerva persica was comparable to that of the standard drug, Donepezil, and the effect might be attributed to the higher content of flavonoids and phenolic compounds.


Asunto(s)
Amaranthaceae , Nootrópicos , Ratones , Animales , Nootrópicos/farmacología , Galactosa/toxicidad , Acetilcolinesterasa , Acetilcolina/efectos adversos , Trastornos de la Memoria/inducido químicamente , Trastornos de la Memoria/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Glutatión/efectos adversos , Etanol , Flavonoides/farmacología , Flavonoides/uso terapéutico , Aprendizaje por Laberinto
16.
Expert Rev Anti Infect Ther ; 20(2): 231-241, 2022 02.
Artículo en Inglés | MEDLINE | ID: mdl-34112047

RESUMEN

INTRODUCTION: Global emergence of coronavirus disease-19 (COVID-19) has clearly shown variable severity, mortality, and frequency between and within populations worldwide. These striking differences have made many biological variables attractive for future investigations. One of these variables, vitamin D, has been implicated in COVID-19 with rapidly growing scientific evidence. AREAS COVERED: The review intended to systematically explore the sources, and immunomodulatory role of vitamin D in COVID-19. Search engines and data sources including Google Scholar, PubMed, NCBI, Scopus, and Web of Science were used for data collection. The search terms used were Vitamin D, COVID-19, immune system, and antiviral mechanism. Overall, 232 sources of information were collected and 188 were included in this review. EXPERT OPINION: Interaction of vitamin D and vitamin D receptor (VDR) triggers the cellular events to modulate the immune system by regulation of many genes. Vitamin D operates as a double-edged sword against COVID-19. First, in macrophages, it promotes the production of antimicrobial and antiviral proteins like ß-defensin 2 and cathelicidin, and these proteins inhibit the replication of viral particles and promote the clearance of virus from the cells by autophagy. Second, it suppresses cytokine storm and inflammatory processes in COVID-19.


Asunto(s)
Factores de Restricción Antivirales/inmunología , Autofagia , COVID-19 , Citocinas/inmunología , Vitamina D , COVID-19/complicaciones , COVID-19/inmunología , Humanos , Macrófagos/inmunología , Receptores de Calcitriol , SARS-CoV-2 , Vitamina D/inmunología , Vitaminas
17.
Membranes (Basel) ; 12(7)2022 Jul 11.
Artículo en Inglés | MEDLINE | ID: mdl-35877904

RESUMEN

The majority of food packaging materials are petroleum-based polymers, which are neither easily recyclable nor ecologically friendly. Packaging films should preferably be transparent, light in weight, and easy to process, as well as mechanically flexible, and they should meet the criteria for food encapsulation. In this study, poly (vinyl alcohol) (PVA)-based films were developed by incorporating glass flakes into the films. The selection of PVA was based on its well-known biodegradability, whereas the selection of glass flakes was based on their natural impermeability to oxygen and moisture. The films were processed using the blade coating method and were characterized in terms of transparency, oxygen transmission rate, mechanical strength, and flexibility. We observed that the incorporation of glass flakes into the PVA matrix did not significantly change the transparency of the PVA films, and they exhibited a total transmittance of around 87% (at 550 nm). When the glass flakes were added to the PVA, a significant reduction in moisture permeation was observed. This reduction was also supported and proven by Bhardwaj's permeability model. In addition, even after the addition of glass flakes to the PVA, the films remained flexible and showed no degradation in terms of the water vapor transmission rate (WVTR), even after bending cycles of 23,000. The PVA film with glass flakes had decent tensile characteristics, i.e., around >50 MPa. Increasing the concentration of glass flakes also increased the hardness of the films. Finally, a piece of bread was packaged in a well-characterized composite film. We observed that the bread packaged in the PVA film with glass flakes did not show any degradation at all, even after 10 days, whereas the bread piece packaged in a commercial polyethylene bag degraded completely. Based on these results, the developed packaging films are the perfect solution to replace commercial non-biodegradable films.

18.
CNS Neurol Disord Drug Targets ; 21(6): 479-491, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-34477535

RESUMEN

BACKGROUND AND OBJECTIVE: Hearing loss is a common audio-vestibular-related neurosensory disability of inner ears, in which patients exhibit clinical symptoms of dizziness, gait unsteadiness, and oscillopsia, at an initial stage. While, if such disorders are untreated for a prolonged duration then the progression of disease into a chronic state significantly decreases GABA level as well as an alteration in the neurotransmission of CNS systems. Hence, to control the progression of disease into a chronic approaches for timely and targeted delivery of the drugs at the site of action in the ear is now attracting the interest of neurologists for effective and safe treatment of such disorders. Among delivery systems, owing to small dimension, better penetration, rate-controlled release, higher bioavailability; nanocarriers are preferred to overcome delivery barriers, improvement in residence time, and enhanced the performance of loaded drugs. Subsequently, these carriers also stabilize encapsulated drugs while also provide an opportunity to modify the surface of carriers to favor guided direction for site-specific targeting. Contrary to this; conventional routes of drug delivery such as oral, intravenous, and intramuscular are poorer in performance because of inadequate blood supply to the inner ear and limited penetration of blood-inner ear barrier. CONCLUSION: This review summarized novel aspects of non-invasive and biocompatible nanoparticles- based approaches for targeted delivery of drugs into the cochlea of the ear to reduce the rate, and extent of the emergence of any hearing loss mediated neurological disorders.


Asunto(s)
Oído Interno , Pérdida Auditiva , Nanopartículas , Sistemas de Liberación de Medicamentos/métodos , Pérdida Auditiva/tratamiento farmacológico , Humanos , Preparaciones Farmacéuticas
19.
Anticancer Agents Med Chem ; 22(4): 668-686, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-34238197

RESUMEN

Lung cancer is the second most common cancer and the primary cause of cancer-related death in both men and women worldwide. Due to diagnosis at an advanced stage, it is associated with high mortality in the majority of patients. At present, various treatment approaches are available, such as chemotherapy, surgery, and radiotherapy, but all these approaches usually cause serious side effects like degeneration of normal cells, bone marrow depression, alopecia, extensive vomiting, etc. To overcome the aforementioned problems, researchers have focused on the alternative therapeutic approach in which various natural compounds are reported, which possessed anti-lung cancer activity. Phytocompounds exhibit their anti lung cancer activity via targeting various cell-signaling pathways, apoptosis and cell cycle arrest, and by regulating antioxidant status and detoxification. Apart from the excellent anti-cancer activity, clinical administration of phytocompounds is confined because of their high lipophilicity and low bioavailability. Therefore, researchers show their concern in the development of a stable, safe and effective approach of treatment with minimal side effects by the development of nanoparticle-based delivery of these phytocompounds to the target site. Targeted delivery of phytocompound through nanoparticles overcomes the aforementioned problems. In this article, the molecular mechanism of phytocompounds, their emerging combination therapy, and their nanoparticles-based delivery systems in the treatment of lung cancer have been discussed.


Asunto(s)
Neoplasias Pulmonares , Nanopartículas , Terapia Combinada , Sistemas de Liberación de Medicamentos , Femenino , Humanos , Neoplasias Pulmonares/tratamiento farmacológico
20.
Int J Biol Macromol ; 194: 338-346, 2022 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-34800521

RESUMEN

Presented research aimed to develop a spray drying process without the use of organic solvents for the preparation of novel Karaya gum polymer microparticles (MPs) of Ganoderma lucidum polysaccharide (GLP). The prepared microparticles were characterized and evaluated. Prepared novel karaya gum micro-particles loaded Ganoderma lucidum polysaccharide (GLP MPs) were observed an effect on cadmium (CAD) induced testicular toxicity. A total of 40 rats (male) was divided into 4 groups viz. 1. Control group, 2. GLP MPs (250 mg/kg, 60 days of b.w per day), 3. CAD (60 days of 30 mg/l/day), 4. GLP MPs + CAD. CAD was responsible for altering the sex hormones, oxidative stress and inflammatory cytokines. Furthermore, elevated levels of indicator of oxidative stress, malondialdehyde, and a reduced action of SOD, GSH, and CAT (antioxidant enzymes), were observed in the tissues of the testicles of CAD- treated group. Such harmful occurrences were followed by an up-regulation in proinflammatory cytokines (TNF-α, IL-1ß) levels, protein expression of Nrf2, and HO-1 expression was decreased. GLP MPs pre-treatment significantly abrogated these toxic effects which were confirmed histologically. This study concluded that pre-treatment with GLP MPs exerts a protective effect against CAD-induced male reproductive testicular toxicity.


Asunto(s)
Cadmio/toxicidad , Citocinas/metabolismo , Polisacáridos Fúngicos/química , Hormonas Esteroides Gonadales/metabolismo , Mediadores de Inflamación/metabolismo , Goma de Karaya/química , Estrés Oxidativo , Animales , Fenómenos Químicos , Portadores de Fármacos , Polisacáridos Fúngicos/administración & dosificación , Peroxidación de Lípido , Masculino , Ratas , Análisis Espectral
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA