24 research outputs found
Bioanalytical method development and validation of atrasentan in human plasma using verapamil as internal standard by liquid chromatography coupled with tandem mass spectrometry
No full textA satisfactory LC-MS/MS separation and good peak symmetry for Atrasentan were obtained with Agilent, Zorbax, XDB C18 (2.1 x 50 mm ID, 5 μm), and a mobile phase containing a mixture of 5 mM Ammonium Formate buffer with 0.1% formic acid were mixed with HPLC grade Acetonitrile in the proportion of 70:30, v/v was delivered at a flow rate of 0.150 mL/min by positive ion mode (API 4000) with an injection volume of 10 µL and a run time of 3 min. Detection is performed by atmospheric pressure electrospray ionization (ESI) mass spectrometry in positive ion mode. The precursor to product ion transitions is m/z 5.11.600 to 354.04 for Atrasentan, and m/z 455.40 to 165.00 for Verapamil (Internal standard) were used for quantization. The retention time of Atrasentan and Verapamil (Internal standard) was found to be 1.68 & 0.96 min
Flavonoids and Alzheimer’s disease: reviewing the evidence for neuroprotective potential
No full textNeurodegeneration, which manifests as several chronic and incurable diseases, is an age-related condition that affects the central nervous system (CNS) and poses a significant threat to the public's health for the elderly. Recent decades have experienced an alarming increase in the incidence of neurodegenerative disorders (NDDs), a severe public health issue due to the ongoing development of people living in modern civilizations. Alzheimer's disease (AD) is a leading trigger of age-related dementia. Currently, there are no efficient therapeutics to delay, stop, or reverse the disease's course development. Several studies found that dietary bioactive phytochemicals, primarily flavonoids, influence the pathophysiological processes underlying AD. Flavonoids work well as a supplement to manufactured therapies for NDDs. Flavonoids are effective in complementing synthetic approaches to treat NDDs. They are biologically active phytochemicals with promising pharmacological activities, for instance, antiviral, anti-allergic, antiplatelet, anti-inflammatory, antitumor, anti-apoptotic, and antioxidant effects. The production of nitric oxide (NO), tumor necrosis factor (TNF-α), and oxidative stress (OS) are downregulated by flavonoids, which slow the course of AD. Hence, this research turned from preclinical evidence to feasible clinical applications to develop newer therapeutics, focusing on the therapeutic potential of flavonoids against AD
Development and Validation of a Stability-Indicating RP-HPLC Method for the Simultaneous Determination of Palonosetron and Fosnetupitant
No full textA simple, accurate, and robust RP-HPLC method was developed and validated for the simultaneous estimation of Palonosetron (PST) and Fosnetupitant (FST) in Akynzeo I.V. formulation. Chromatographic separation was achieved using a Waters C18 column (250 × 4.6 mm, 5 μm) with a mobile phase of K2HPO4 buffer: Acetonitrile (70:30 v/v) at a flow rate of 1.0 mL/min, and a detection wavelength of 228 nm. PST and FST exhibited retention times of 1.76 min and 2.31 min, respectively. Linearity was observed within 0.125–0.375 μg/mL for PST and 117.5–352.5 μg/mL for FST. The developed method was validated as per ICH Q2(R1) guidelines and was found precise, accurate, specific, and stability-indicating
ANALYTICAL METHOD DEVELOPMENT AND VALIDATION OF AMLODIPINE IN HUMAN PLASMA USING LIQUID CHROMATOGRAPHY-MASS SPECTROMETRY/MASS SPECTROMETRY
No full textObjective: The objective of the present investigation was to develop a novel, simple, and economic method for the estimation of amlodipine in positive ion mode in human plasma using amlodipine maleate d4 as an internal standard.Methods: The chromatographic separation was performed on Zorbax SB, C18, 50 mm*4.6 mm, and 3.5 mm. The mobile phase was prepared with a mixture of 5 mm ammonium acetate in 0.1% formic acid: High performance liquid chromatographic (HPLC) grade methanol:HPLC grade acetonitrile (40:30:30) that run isocratically at the flow rate of 0.700 ml/min and run time at 2.50 min.Results: The analytical method is valid for the estimation of amlodipine, in human plasma over a range of 0.100 ng/ml–9.990 ng/ml with the detection of amlodipine m/z - 409.10 (parent) and 238.00 (product), and internal standard Amlodipine Maleate d4 m/z - 413.20 (parent), and 238.00 (product) in positive ion mode. The results of carryover test, matrix effect, linearity, precision and accuracy, stabilities, dilution integrity, and run size evaluation test presented in this report are within the acceptance range.Conclusion: A sensitive method for the separation and determination of amlodipine in plasma has been developed based on solid-phase extraction with disposable extraction cartridges in combination with LC and mass spectrophotometers (MS/MS)
Fighting Antibiotic Resistance: New Pyrimidine-Clubbed Benzimidazole Derivatives as Potential DHFR Inhibitors
No full textThe present work describes the design and development of seventeen pyrimidine-clubbed benzimidazole derivatives as potential dihydrofolate reductase (DHFR) inhibitors. These compounds were filtered by using ADMET, drug-likeness characteristics calculations, and molecular docking experiments. Compounds 27, 29, 30, 33, 37, 38, and 41 were chosen for the synthesis based on the results of the in silico screening. Each of the synthesized compounds was tested for its in vitro antibacterial and antifungal activities using a variety of strains. All the compounds showed antibacterial properties against Gram-positive bacteria (Staphylococcus aureus and Staphylococcus pyogenes) as well as Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). Most of the compounds either had a higher potency than chloramphenicol or an equivalent potency to ciprofloxacin. Compounds 29 and 33 were effective against all the bacterial and fungal strains. Finally, the 1,2,3,4-tetrahydropyrimidine-2-thiol derivatives with a 6-chloro-2-(chloromethyl)-1H-benzo[d]imidazole moiety are potent enough to be considered a promising lead for the discovery of an effective antibacterial agent
Fast and Sensitive Bioanalytical Method for the Determination of Deucravacitinib in Human Plasma Using HPLC-MS/MS: Application and Greenness Evaluation
No full textPlaque psoriasis is a common, long-lasting illness that affects the immune system and causes significant negative impacts on a patient’s physical health, well-being, and ability to work effectively. Deucravacitinib (DEU) is the first oral medication used in the treatment of plaque psoriasis, a chronic skin condition that causes red, scaly patches on the skin. DEU is a type of medication called an oral Janus kinase (JAK) inhibitor, which works by blocking specific enzymes that play a role in the inflammation and immune response associated with psoriasis. Therefore, a quick, easy, novel, reliable, sensitive, and straightforward liquid chromatography-tandem mass spectrometry (LC-MS/MS) approach was used to analyze DEU in plasma samples. The LC-MS/MS method for the determination of DEU in human plasma was based on using trimethoprim as an internal standard (IS). The separation of DEU and IS was carried out via liquid–liquid extraction (LLE). The extract was then subjected to the chromatographic system separation using the ACE-C18 column (4.6 × 100 mm, 5 µm). The mobile phase employed consisted of methanol and a solution of 2 mM ammonium formate (80:20 v/v, respectively). The flow rate used was set at 0.9 mL min−1. The creative strategy was performed by running an ABSCIEX API 4000 mass spectrometer with an electron spray ionization source in multiple reaction monitoring (MRM) mode. The ion transitions m/z 426.3 → 358.2 were used for DEU quantitation, while the ion transitions m/z 291.1 → 261.1 were used for trimethoprim quantitation. The accuracy, precision, linearity, recovery, and selectivity of DEU were deemed acceptable when validated for a concentration range between 0.500 and 601.050 ng/mL, utilizing a weighting factor of 1/x2
Design, optimization, and characterization of Zolmitriptan loaded liposomal gels for intranasal delivery for acute migraine therapy
No full textZolmitriptan is the primary drug for the treatment of Migraine. However, the bioavailability of the drug is low and requires repetitive administration leading to side effects. Zolmitriptan's bioavailability can be improved by incorporating it into liposomes as a topical intranasal gel. The formulation was developed using a Central composite design employing a response surface approach. The new formulations were tested for particle size, shape, drug entrapment efficiency, and in vitro drug release. Permeation experiments and histopathology in rats were also conducted to determine the formulation's safety. The vesicle size was found to be in the range of 103.82 ± 7.16 to 694.38 ± 1.02 nm, zeta potential --19.28 to −32.8 mV, Entrapment Efficiency from 55.49 ± 1.37 to 99.12 ± 0.36 %, and cumulative drug release from 59.71 ± 6.94 to 99.38 ± 0.13 % respectively. In-vitro drug release of G1 and G3 gel formulations showed a non-Fickian released pattern during the studies. A comparison of the permeation coefficient of G1 (0.539 μg/cm2) and G3 (5.3 μg/cm2) showed a slight variation in the drug release rate after 24 h. For the liposomal gel and its solution, we found a significant difference in drug penetration of p0.05 after 12 h compared to the control gel. There were substantial differences in bioavailability and pharmacokinetics between the optimal Liposomal Gel Formulation and other formulations, including the drug solution, liposomal suspension, and optimized formulation F12. The liposomal gel is non-irritating and safe for topical administration by histopathological investigations. Therefore, the study demonstrated that Zolmitriptan Liposomal gel has better efficacy, good tolerability, and enhanced bioavailability, making it an optimal treatment for acute Migraine
TRANSDERMAL PATCHES FOR THE TREATMENT OF ANGINA PECTORIS: AN EFFECTIVE DRUG DELIVERY SYSTEM-A REVIEW
No full textTopical delivery methods have been used since the dawn of time, employed to cure a wide range of ailments and for aesthetic purposes. Transdermal drug delivery has evolved throughout time, with the development of passive and active technologies that have resulted in enhanced distribution, accuracy in drug dosage, and better fulfilment of the requirements of the individual. The search for more powerful pharmaceuticals that can be delivered to the skin through appropriate transdermal technologies will continue to be a focus in the development of drugs for transdermal patches and other forms of delivery. Topical and transdermal distribution has been around for a while, but this review will focus on transdermal patches and how they\u27ve evolved. The articles have been searched on different search engines such as Scopus database, Science direct, PubMed, Google scholar, and Bentham science using multiple keywords. An adhesive transdermal patch is applied to the skin and contains medicine that is absorbed into the bloodstream through the skin. It aids in the recovery of an afflicted part of the body. When compared to oral, topical, i. v., and i. m. administration systems, transdermal drug delivery allows a controlled release of the medicine into patients, often by either a porous membrane or by body heat melting small layers of medication embedded in the adhesive. The fundamental drawback of transdermal delivery methods is that the skin is a highly efficient barrier, therefore, only tiny molecules can enter the skin and be administered in this manner
PHARMACEUTICAL AND BIOPHARMACEUTICAL ASPECTS OF QUANTUM DOTS-AN OVERVIEW
No full textIn the twenty-first century, nanotechnology has become cutting-edge technology. It is interdisciplinary and multidisciplinary, covering numerous fields such as medicine, engineering, biology, physics, material sciences, and chemistry. The present work aims to cover the optical properties, method of preparations, surface modifications, bio-conjugation, characterization, stability, and cytotoxicity of quantum dots (QDs).
Articles were reviewed in English literature reporting the pharmaceutical and bio-pharmaceutical aspects of QDs which were indexed in Scopus, web of science, google scholar and PubMed without applying the year of publication criterion.
One significant value of utilizing nanotechnology is that one can alter and control the properties in a genuinely unsurprising way to address explicit applications\u27 issues. In science and biomedicine, the usage of functional nanomaterials has been broadly investigated and has become one of the quick-moving and stimulating research directions. Different types of nanomaterial (silicon nanowires, QDs, carbon nanotubes, nanoparticles of gold/silver) were extensively utilized for biological purposes. Nanomedicine shows numerous advantages in the natural characteristics of targeted drug delivery and therapeutics. For instance, protection of drugs against degradation, improvement in the drug\u27s stability, prolonged circulation time, deceased side effects, and enhanced distribution in tissues. The present review article deals with the quantum dots, their optical properties, method of preparations, surface modifications, bio-conjugation, characterization, stability, and cytotoxicity of quantum dots. The review also discusses various biomedical applications of QDs.
The QDs-based bio-nanotechnology will always be in the growing list of unique applications, with progress being made in specialized nanoparticle development, the detection of elegant conjugation methods, and the discovery of new targeting ligands
Psychological effects of COVID-19 on patients with cancer, their caregivers: A systematic review
No full textThere is limited study reporting the severity of anxiety and depression in cancer cohort and their caregivers. We aimed in this systematic review to determine the prevalence of stress, anxiety, depression among comprehensive cancer patient and their caregivers during COVID-19 pandemic. A systematic review search was performed on PubMed, PsycINFO, CINAHL, and Scopus till June 2021. PRISMA guidelines were used in this systematic review. Reviews were performed to collect all original research articles to describe prevalence of stress, anxiety, depression among the cancer patients and their caregivers. All analysis was done by using RStudio version 1.0.136. 4 studies from our search criteria were eligible for inclusion for anxiety symptoms. Meta-analyses revealed that no any significant difference in incidence of anxiety in cancer and their caregivers. The pooled odds ratio 1.00 [95% CI; 0.87- 1.15]. Pooled prevalence in patients and their caregivers 49% [25%; 74%] and 50% [26%; 73%] respectively. Anxiety was relatively higher in cancer patients and their care givers. Isolation, married caregivers showed most significant factor to increase anxiety in cancer patients and their care givers. This metaanalyses suggest that prevalence of anxiety in cancer patients and their caregivers were significantly increasing during COVID-19
