Selective detection of azelnidipine in pharmaceuticals via carbon dot mediated spectrofluorimetric method: A green approach.

A spectrofluorimetric method using fluorescent carbon dots (CDs) was developed for the selective detection of azelnidipine (AZEL) pharmaceutical in the presence of other drugs. In this study, N-doped CDs (N-CDs) were synthesized through a single-step hydrothermal process, using citric acid and urea as precursor materials. The prepared N-CDs showed a highly intense blue fluorescence emission at 447 nm, with a photoluminescence quantum yield of ~21.15% and a fluorescence lifetime of 0.47 ns. The N-CDs showed selective fluorescence quenching in the presence of all three antihypertensive drugs, which was used as a successful detection platform for the analysis of AZEL. The photophysical properties, UV-vis light absorbance, fluorescence emission, and lifetime measurements support the interaction between N-CDs and AZEL, leading to fluorescence quenching of N-CDs as a result of ground-state complex formation followed by a static fluorescence quenching phenomenon. The detection platform showed linearity in the range 10-200 µg/ml (R2 = 0.9837). The developed method was effectively utilized for the quantitative analysis of AZEL in commercially available pharmaceutical tablets, yielding results that closely align with those obtained from the standard method (UV spectroscopy). With a score of 0.76 on the 'Analytical GREEnness (AGREE)' scale, the developed analytical method, incorporating 12 distinct green analytical chemistry components, stands out as an important technique for estimating AZEL.

Development and Validation of Stability-indicating RP-HPLC Method for Estimation of Pranlukast Hydrate in its Laboratory Mixture.

Pranlukast hydrate is an anti-asthmatic drug and used in the treatment of acute asthma. Stability-indicating RP-HPLC method for pranlukast hydrate has been developed and validated. The reverse phase high performance liquid chromatographic method was developed using Shimadzu Column: Kromosil 100 C18 (150 mm × 4.6 mm × 5 µm) and mobile phase Acetonitrile: 0.1% Glacial acetic acid (85: 15% v/v). Eluent was monitored with UV-detector at 262 nm with a flow rate of 0.5 mL/min, temperature maintained at 30°C. Stress testing was carried out in acidic, alkaline, oxidative, photolytic and dry heat degradation conditions. The method was validated as per the International Conference for Harmonization guidelines and includes specificity, accuracy, precision, linearity and limit of quantitation and detection parameters. A relative standard deviation <2% indicates the developed method was precise. The accuracy of the method was represented by recovery studies ranging between 99.41 and 99.72%. In acid, alkaline, oxidative stress conditions, pranlukast hydrate degrades significantly and in photolytic, dry heat, hydrolytic conditions remain stable. This proposed method is suitable for the analysis of pranlukast hydrate in its laboratory mixture.

A solar-responsive zinc oxide photoanode for solar-photon-harvester photoelectrochemical (PEC) cells.

A highly efficient, nanostructured, solar-responsive zinc-oxide (SRZO) photoanode has been achieved by utilization of a versatile solution precursor plasma spray (SPPS) deposition technique. For the first time, it is demonstrated that a front-illumination type SRZO photo-anode fabricated with a ZnO/stainless steel (SS-304) configuration can generate an enhanced photo-electrochemical (PEC) current of 390 µA cm-2, under solar radiation from a solar simulator with an AM1.5 global filter (∼1 sun). The SRZO electrode displayed a solar-to-hydrogen (STH) conversion efficiency of 2.32% when investigated for H2 evolution in a PEC cell. These electrodes exhibited a maximum peak efficiency of 86% using 320 nm photons during incident photon-to-current conversion efficiency measurement. Interestingly, the film lattice of SRZO showed a significant red-shift of 0.37 eV in the ZnO band gap thereby providing solar photon absorptivity to SRZO. Further, an enhanced charge transport property by virtue of increased donor density (∼4.11 × 1017 cm-3) has been observed, which is higher by an order of magnitude than that of its bulk counterpart. Efficient optical absorption of solar photons and higher donor-density of SRZO have been thus attributed to its superior PEC performance.

Effect of Education on Awareness, Knowledge, and Willingness to Be Vaccinated in Females of Western India.

Cervical Cancer is the second most leading cause of death among Indian women. Infection by human papillomavirus (HPV) is one of the major causes of cervical cancer. Two prophylactic HPV vaccines approved and recommended for adolescents and young women in India. However, due to lack of appropriate knowledge, education, resources, and proper communication, these tools have little impact on disease burden. It is important to understand attitude, knowledge, and beliefs of females about HPV, cervical cancer, and HPV vaccine. Hence, the present study aimed to check awareness, educate females about cervical cancer and HPV vaccine, and evaluate the major hurdles in acceptability of HPV vaccine. Total 693 females of age 16 to 40 years of diverse background were enrolled in the study. Questionnaires were prepared to assess knowledge about cervical cancer and HPV vaccine before and after education and impact of knowledge on willingness to administer the vaccine. Education was given with the help of concern physicians. Final follow-up was done after 1 month to assess the attitude towards vaccination. The overall awareness before education was found to be 20.63%; maximum in females of medical (51.37%), and paramedical background (33.33%). Improvement after education was observed in terms of improved information about etiology, symptoms, precautions, and vaccination for cervical cancer. Acceptability of HPV vaccine was found to be poor (40.11% refused to undergo vaccination and 32.17% were in dilemma/unable to decide). Besides religious beliefs, high cost of the vaccine and unavailability of proper and convincing information about the vaccine would be the chief reasons for poor acceptability of HPV vaccine.

Repurposing of Iloperidone: Antihypertensive and ocular hypotensive activity in animals.

PURPOSE: Iloperidone, second generation antipsychotic drug, reported in clinical trial to produce orthostatic hypotension as side effect. It was claimed to be antagonistic at alpha adrenergic receptor in central nervous system. We evaluated effect of Iloperidone on peripheral alpha 1 adrenoreceptor by in silico and in vitro methods while in vivo hypotensive, antihypertensive and ocular hypotensive activity was evaluated in animals. METHODS: Pharmacological activity prediction of Iloperidone was done using PASSOnline and SwissTargetPrediction softwares and molecular docking with Alpha 1A adrenoreceptor using AutoDock Vina. Hypotensive activity in normotensive and antihypertensive activity against DOCA-salt induced hypertension in rats were evaluated at doses 0.03 mg/Kg and 0.1 mg/Kg, i.p of Iloperidone. Blood pressure was measured by invasive blood pressure measurement technique using PowerLab 4/30 and intraocular pressure was measured using digital tonometer. RESULTS: Iloperidone (0.1 mg/Kg) showed significant decrease in blood pressure (38.96 ± 1.1%) in normotensive rats, while in DOCA salt induced hypertensive rats, systolic blood pressure was found to be decreased by 29.04 ± 1.45% and 31.43 ± 1.21% in 0.03 mg/Kg and 0.1 mg/Kg treated rats respectively. Iloperidone prevented rise in systolic BP with adrenaline. Intraocular pressure was found to be decreased by 36.66 ± 3.15% in rabbits after 1 h of instillation of 0.1% Iloperidone. CONCLUSION: Iloperidone exerted hypotensive and/or anti-hypertensive activity in rats and ocular hypotensive activity in rabbits.

Cyclosporine laden tailored microemulsion-gel depot for effective treatment of psoriasis: In vitro and in vivo studies.

Psoriasis is a widespread chronic disease affecting 1-3 % of total population. In major cases (>80 %), it is treated by topical application of corticosteroids. However, the topical route is very challenging due to physico-chemical nature of diseased stratum corneum and so no single treatment works for every patient. The oral route showed severe side effects due to systemic immunosuppression, which can be avoided by topical route. The aim of the research work was to investigate cyclosporine loaded microemulsion based gel for effective cyclosporine permeation and retention in the skin tissue for psoriasis treatment. The pseudo ternary phase diagram at three Smix ratios (2:1, 1:1, and 1:2; Tween 80: isopropyl alcohol) were constructed using isopropyl myristate as oil phase. The Smix at 2:1 ratio showed large microemulsion area. The transmission electron microscope images showed spherical non-aggregated oil globules with the size < 50 nm. The selected microemulsion (Cy-2-ME12O55SM) was incorporated in Carbopol 940 gel for topical application. The ex vivo diffusion study showed improved permeation (>24 h) with microemulsion-gel in comparison to cyclosporine suspension. The microemulsion-gel was non-irritating on the rabbit skin. In drug retention studies, microemulsion-gel showed high drug retention (trapping, 38.92 %) in the skin tissue, which was due to destabilization of microemulsion after penetration in the skin layer causing precipitation of cyclosporine. The depot effect due to cyclosporine precipitates could be helpful for sustained effect of cyclosporine for the effective treatment of psoriasis.

Anticancer activity of saponin isolated from Albizia lebbeck using various in vitro models.

ETHNOPHARMACOLOGICAL RELEVANCE: Albizia lebbeck (L.) Benth. (Family: Mimosaceae) is commonly known as Sirisha in Sanskrit. The leaves and pods of A. lebbeck were claimed to be used against cancer in traditional medicine. Previous studies using bark, leaves, seeds and pods of A. lebbeck showed cytotoxic activity against hepatic, colon, larynx, cervical and breast cancer cell lines. AIM OF THE STUDY: To evaluate the anticancer activity of saponin rich fraction of Albizia lebbeck by using various in vitro models. MATERIALS AND METHODS: Albiziasaponins (A-E) are oleanene triterpene presents in Albizia lebbeck were used for in silico studies. In silico testing of albiziasaponins for structure based pharmacological activity prediction using PASS Online software and docking with Autodock tool and Autodock Vina revels it's anticancer and apoptogenic potential. Antiproliferative activity of saponin rich fraction of A. lebbeck was performed using MCF-7 human breast cancer cells by MTT assay methods. Anti-angiogenic property of saponin rich fraction of A. lebbeck was evaluated in in vitro shell less chick embryo cultures with different concentrations (0.1 µg/ml, 0.5 µg/ml, and 1 µg/ml) by using ImageJ software. In vitro cultured lymphocytes chromosomal aberration assay was performed to determine the physical integrity of chromosomes in cells and effect of saponin rich fraction of A. lebbeck on cell cycle. Apoptogenic potential was evaluated using Caspases-3 and Caspase-8 ELISA assay in MCF-7 cells. RESULTS: Result of MTT assay showed IC50 of saponin rich fraction of A. lebbeck at 1 µg/ml in MCF-7 cells. Treatment with saponin rich fraction of A. lebbeck significantly (p < 0.05) reduced angiogenic parameters. Significant chromosomal aberrations (hypodiploid, hyperdiploid, ring, premature separation, Dicentric fragments, Acentric fragment, chromatid break, and chromosomal gap) were observed in saponin rich fraction of A. lebbeck treated groups. Treatment with saponin rich fraction of A. lebbeck increased levels of Caspases-3 (optical density of 0.24 at 450 nm) and Caspase-8 (optical density of 0.31 at 450 nm) as compared to staurosporine (optical density of 2.47 and 2.65 for caspases-3 and -8 respectively at 450 nm). CONCLUSION: In our study, saponin rich fraction of A. lebbeck showed antiproliferative, antiangiogenic and apoptogenic potential using various in-vitro models. It also found to increase chromosomal aberration and thereby may affect cell cycle.

Screening of flavonoids rich fractions of three Indian medicinal plants used for the management of liver diseases

ABSTRACTThe decoctions of the Butea monosperma (Lam.) Taub., Fabaceae, Bauhinia variegata L., Fabaceae, and Ocimum gratissimum L., Lamiaceae, are traditionally used for the treatment of various types of hepatic disorder. Phytochemical studies have shown that total flavonoids from these plants were the major constituents of the picked out part of each plant. The present study was planned to investigate the hepatoprotective effect of flavonoid rich fractions of the B. monosperma, B. variegata and O. gratissimum against paracetamol induced liver damage. Flavonoid rich fractions were isolated by solvent fractionation from each plant. Each fraction was subjected to various qualitative chemical tests to findout the metabolites. Flavonoid fractions of each plant were subjected for pharmacological screening. The rats were monitored for change in liver morphology, biochemical parameters like serum glutamate pyruvate transaminase, serum glutamate oxaloacetate transaminase, alkaline phosphatase and total bilirubin for the groups receiving the flavonoid-rich fractions. All flavonoid rich fractions showed significant hepatoprotective activity. The histological studies supported the biochemical parameters. From the results of biochemical analysis and histopathological studies, it can be accomplished that in the ethyl acetate fraction of O. gratissimum showed highest hepatoprotective activity as compared to other fractions. The present study was the first evidence of flavonoid-rich fractions of each plant have a remarkable hepatoprotective effect. All fractions contain a potent hepatoprotective agent suggested to be a flavone, which may find clinical application in amelioration of paracetamol-induced liver damage.

Zirconia-Nanoparticle-Reinforced Morphology-Engineered Graphene-Based Foams.

The morphology of graphene-based foams can be engineered by reinforcing them with nanocrystalline zirconia, thus improving their oil-adsorption capacity; This can be observed experimentally and explained theoretically. Low zirconia fractions yield flaky microstructures where zirconia nanoparticles arrest propagating cracks. Higher zirconia concentrations possess a mesh-like interconnected structure where the degree of coiling is dependant on the local zirconia content.

Nano-enabled tribological thin film coatings: global patent scenario.

The aim of this paper is to present current status and future prospects of nano-enabled tribological thin film coatings based on worldwide patent landscape analysis. The study also presents an overview of technological trends by carrying out state-of-the-art literature analysis, including survey of corporate websites. Nanostructured tribological coatings encompass a wide spectrum of nanoscale microstructures, including nanocrystalline, nanolayered, nano-multilayered, nanocomposite, nanogradient structures or their unique combinations, which are composed of single or multi-component phases. The distinct microstructural features of the coatings impart outstanding tribological properties combined with multifunctional attributes to the coated components. Their unique combination of remarkable properties make them ideal candidates for a wide range of applications in diverse fields such as cutting and metalworking tools, biomedical devices, automotive engine components, wear parts, hard disc drives etc. The patent landscape analysis has revealed that nano-enabled tribological thin film coatings have significant potential for commercial applications in view of the lion's share of corporate industry in patenting activity. The largest patent portfolio is held by Japan followed by USA, Germany, Sweden and China. The prominent players involved in this field are Mitsubishi Materials Corp., Sandvik Aktiebolag, Hitachi Ltd., Sumitomo Electric Industries Ltd., OC Oerlikon Corp., and so on. The outstanding potential of nanostructured thin film tribological coatings is yet to be fully unravelled and, therefore, immense opportunities are available in future for microstructurally engineered novel coatings to enhance their performance and functionality by many folds.

Effect of Boerhaavia diffusa in experimental prostatic hyperplasia in rats.

OBJECTIVE: Present investigation was undertaken to study the effectiveness of hydroalcoholic extract of roots of Boerhaavia diffusa in experimental benign prostatic hyperplasia (BPH) in rats using various animal models. MATERIALS AND METHODS: BPH in rats was induced by subcutaneous injection of testosterone (5 mg/kg) daily for 28 days. Rats were divided in to five groups (six rats each). A negative control group received arachis oil (1 ml/kg s.c.) and four groups were injected testosterone. These four groups were further divided into reference group (finasteride 1 mg/kg), model group (testosterone), study group A (B. diffusa 100 mg/kg), and study group B (B. diffusa 250 mg/kg). On the 29(th) day, rats were sacrificed and body weight, prostate weight, bladder weight, and serum testosterone level were measured and histological studies were carried out. Further in vitro analysis of B. diffusa extract on contractility of isolated rat vas deferens and prostate gland, produced by exogenously administered agonists were carried out. All results were expressed as mean ± SEM. 0 Data were analyzed by one-way analysis of variance followed by Tukey's test. RESULTS: B. diffusa (100 mg/kg) treatment for 28 days resulted in significant inhibition of prostate growth (P < 0.05). Drug extract did not have significant change on serum testosterone level. Histopathological analysis of prostate gland supported above results. Results of in vitro experiment suggest that extracts had attenuated the contractile responses of isolated vas deferens and prostate gland to exogenously applied agonists. CONCLUSION: The results suggested that treatment with B. diffusa may improve symptoms of disease and inhibit the increased prostate size. In vitro study implies that herbal extracts has the machinery to produce beneficial effect on prostatic smooth muscle, which would relieve the urinary symptoms of disease. B. diffusa could be a potential source of new treatment of prostatic hyperplasia.

Protective effect of aqueous extract of Oroxylum indicum Linn. (root bark) against DNBS-induced colitis in rats.

OBJECTIVE: Aqueous root extract of Oroxylum indicum was evaluated in rats against dinitrobenzene sulfonic acid (DNBS) induced colitis. MATERIALS AND METHODS: Rats were pre-treated orally for seven days and continued for four days after the induction of colitis with OI(aq) (100, 200, and 400 mg/kg) or vehicle. Colitis was induced by intracolonic instillation of 25 mg of DNBS per rat dissolved in 50% alcohol and 4 days later, the colonic mucosal damage was analyzed along with food intake, body weight, colon weight, spleen weight, histological damage, myeloperoxidase (MPO) activity, malondialdehyde (MDA) levels, reduced glutathione (GSH), and nitric oxide levels in colonic tissue homogenate. RESULTS: Significant reduction in gross damage area, weight loss and increase in colonic and spleen weight were evident in test substance-pretreated animals' dose dependently as compared to vehicle treated control. These effects were confirmed biochemically by a reduction in colonic myeloperoxidase activity, malondialdehyde levels, nitric oxide levels, and increase in reduced glutathione (GSH) levels. Furthermore, microscopic examination revealed diminution of inflammatory cell infiltration and submucosal edema in colon segments of rats treated with OI(aq). CONCLUSION: The results demonstrate the protective effect of OI(aq) in the animal model of acute colitis possibly through an antioxidant, anti-lipoperoxidative or due to reduction in nitric oxide generation.

Assessment of the antidiabetic potential of Cassia grandis using an in vivo model.

The aqueous and ethanolic extracts of C. grandis (Family: Leguminosae) were evaluated for antidiabetic activity by a glucose tolerance test, in normal rats and alloxan-induced diabetic rats. The aqueous and ethanolic extracts showed that they significantly lowered the blood glucose levels to normal in the glucose tolerance test. In alloxan-induced diabetic rats the maximum reduction in blood glucose was observed after three hours, at a dose level of 150 mg/kg of body weight. The percentage of protection given by the aqueous and ethanolic extracts was 32.72 and 46.42%, respectively. In the long-term treatment of alloxan-induced diabetic rats, the degree of protection was determined by measuring the blood glucose, cholesterol, and triglycerides on the tenth day. Both the extracts showed a significant antidiabetic activity comparable to that of glibenclamide. These results showed that the Cassia grandis possessed significant antidiabetic activity.