Contents:
Neurodegenerative diseases constitute a pressing global health challenge, characterized by the gradual loss of neuronal function and structure, leading to cognitive impairment and motor deficits. Biomarkers play a crucial role in understanding the complex pathophysiological pathways of neurodegenerative disorders. By analyzing a variety of recent studies and advancements in the field, we aim to unravel the potential of biomarkers in not only facilitating early diagnosis but also shedding light on disease progression and, consequently, offering critical insights into therapeutic strategies including network pharmacology. These biomarkers cover a wide range of neuroimaging, cerebrospinal fluid, blood-based and genetic markers that help us better understanding of disease etiology and progression. Furthermore, this article explores the dynamic field of biomarker research, including the integration of advanced technologies such as neuroimaging, genomics and proteomics along with the challenges and limitations in the field, including standardization and validation issues, as well as ethical concerns surrounding the use of biomarkers. This review serves as a comprehensive resource for researchers, clinicians and doctors interested in the fight against neurodegenerative diseases. By synthesizing current knowledge on biomarkers, their potential as diagnostic, prognostic and therapeutic tools, ultimately contributing to the development of innovative strategies aimed at mitigating the devastating impact of neurodegeneration can be elucidated.
Background
This comprehensive review highlights the importance of bio-conjugated metallic complexes in drug design, particularly in the field of metallo-pharmaceutical science. The review emphasizes the need for biological relevance and the coordination of biomolecules or modified bio-compounds with metallic systems to maximize drug action and minimize toxicity.
Materials and Methods
The objective of this review is to discuss various diseases, which exemplify the potential of bio-conjugated metallic complexes as a promising approach for drug design.
Results
Utilizing physiologically active ligands in metal complexes has demonstrated improved antioxidant, antiviral, antitubercular and antitumor effects.
Conclusion
Bio conjugated systems have become a viable method for creating molecules with several uses that are good for human health. The development of metal-based imaging agents and drug delivery systems has increased due to the conjugation of metals with biologically active compounds.
Oxadiazoles and their derivatives represent a significant class of organic compounds, wielding profound implications in both the realms of medicinal science and heterocyclic rings housing oxygen and nitrogen atoms, has garnered attention owing to their multifaceted. Pharmacological potential. The diverse array of biological activities exhibited by oxadiazole derivatives spans antimicrobial, anti-inflammatory, anti-cancer and anti-viral effects. Beyond medicinal applications, these compounds showcase utility in agriculture, with their herbicidal, insecticidal and fungicidal properties enabling their role as effective plant protection agents. Researchers have been focusing on the synthesis and exploration of these compounds for their potential in drug development. This review article is an in-depth exploration of diverse synthetic methodologies for oxadiazole and its derivatives while highlighting their associated pharmacological activities. It offers valuable insights into this class of compounds' versatile chemistry and potential therapeutic applications.
This study examined the present situation of Antimicrobial Resistance (AMR) and prevailing Antimicrobial Stewardship Programs (ASP), and its impact during COVID-19 globally and specifically in Abu Dhabi, UAE aiming to identify and define the problem(s) resulting in increasing trends of antibiotic resistance during COVID, potential impact factors, anticipated outcomes and provide a conclusion to aid our approach towards sustainable antimicrobial stewardship program and combat against antimicrobial resistance. The ongoing global AMR crisis is an escalating worldwide challenge and may have been intensified by the COVID-19 pandemic due to uncertainty surrounding COVID-19 treatment, which has resulted in a surge in antibiotic usage, interruptions in infection prevention and control measures within overburdened healthcare systems, and the diversion of both human and financial resources have been redirected from monitoring and addressing AMR threats. Consequently, there is a heightened urgency to emphasize actions aimed at containing AMR and enhancing the ability to swiftly detect, understand, and respond to emerging AMR threats. The Emirate of Abu Dhabi is not immune to this escalating challenge. With resources diverted from antimicrobial stewardship to meet urgent healthcare needs, and evidence of significant pre-emptive antibiotic use in COVID-19 patients potentially impacted levels of resistance and resulted in readmissions. Consequently, the threat of AMR remains substantial, leading to a reevaluation of an existing stewardship program in in-patient settings prompted by the pandemic. The review revealed a shortage of adequate data to determine the extent to which COVID-19 has impacted the current stewardship program in the Emirate of Abu Dhabi.
Background
Nonsteroidal anti-inflammatory drugs, or NSAIDs, including mefenamic acid, are commonly used for the relief of moderate to serious pain. However, their poor water solubility affects their bioavailability and potential therapeutic benefit. Improving the solubility of these poorly soluble medications is essential for optimizing their therapeutic efficacy. The use of hydrotropic agents, or hydrotropy, has become a popular method for improving solubility.
Materials and Methods
Argon Remedies Pvt. Ltd., an Indian company, provided the mefenamic acid. The hydrotropic drugs that were chosen were sodium acetate, sodium salicylate and resorcinol. Using Infrared Spectroscopy (IR) and Differential Scanning Calorimetry (DSC), the medication was analyzed. The solubility investigations involved the preparation of hydrotropic solutions with various levels of concentration (10%, 20%, 30% and 40%) and the use of UV/Vis spectrophotometry to ascertain the equilibrium dissolution of mefenamic acid in these solutions. It was determined if hydrotropic substances affected spectrophotometric estimation.
Results
Mefenamic acid's thermal stability and functional groups were validated by DSC and IR studies. According to equilibrium solubility measurements, sodium acetate, resorcinol and sodium salicylate, all at 40% concentration, gave the highest solubility enhancement ratio of 22.9. The spectrophotometric estimation of mefenamic acid was not affected by the hydrotropic agents. Mefenamic acid formulations including the chosen hydrotropic agents demonstrated a notable increase in solubility when compared to the medication by itself.
Conclusion
Mefenamic acid's solubility is greatly increased by hydrotropy and the most efficient hydrotropic agent is sodium salicylate. This approach provides a viable and effective substitute for enhancing the therapeutic effectiveness and bioavailability of poorly soluble medications, such as mefenamic acid, which may result in higher compliance among patients and clinical results.
Background
Azilsartan, a poorly soluble angiotensin receptor blocker belonging to BCS class II, faces challenges related to low solubility and bioavailability. To address these issues, this study compares two formulation approachessolid dispersion and nanosuspension-aimed at enhancing the solubility and bioavailability of Azilsartan.
Materials and Methods
Nine batches of Azilsartan-solid dispersion were prepared using spray drying with HPMC E5 LV, while nine batches of nanosuspension were formulated via solvent evaporation with PVPK-30. The formulations were evaluated for particle size, polydispersity index, zeta potential, X-ray diffraction pattern, morphology, solubility, and in vitro drug release. The optimal batches, solid dispersion-6 and nanosuspension-6, were selected based on drug content and entrapment efficiency for further comparative evaluation.
Results
Solid dispersion-6 and nanosuspension-6 exhibited drug content of 93.23% and 95.71%, respectively. The particle sizes measured for solid dispersion-6 and nanosuspension-6 were 511.4 nm and 347.6 nm, respectively. Morphological differences between the formulations were evident in photomicrographs. Drug dissolution rates were 95.25% for solid dispersion-6, 96.14% for nanosuspension-6, and 98.14% in an in vitro dissolution study.
Conclusion
The nanosuspension showed greater improvement in solubility and bioavailability, highlighting its potential as a nanocarrier for Azilsartan in clinical applications.
Background
The complex physicochemical properties of the lipids have considerable impact on the solubility and stability of the Lipid Based Nanocarriers (LBN). The major challenge in the successful development of LBN lies on the selection of suitable lipid and its ability to achieve high drug payloads. The wet lab screening of lipids is time consuming and economically not viable. Therefore, the present research aims to apply Hansen solubility parameters to predict the solubility/miscibility of 5-Fluorouracil (5FU) and curcumin in various lipids.
Materials and Methods
The apparent solubility of 5FU and curcumin in various lipids were determined by shake flask method. Theoretical predictions of Hansen Solubility Parameter (HSP) for lipids and actives were done by group contribution method proposed by van Krevelen. The various molecular descriptors of 5FU, curcumin and the range of lipids are obtained from Qikprop predictions, version 4.4, Schrodinger.
Results
Lipids exhibit low dispersion force component (δD) than 5FU and curcumin indicating that they are poor solvents; rather the polar and hydrogen bonding components might have contributed to the solubility of the actives in lipids. Hence, the actives are more soluble in those lipids with free -OH groups as in case of Maisine CC, Labrafac PG and Compritol 888 ATO which is in good correlation with the experimental values.
Conclusion
The HSP sphere radius provides an insight to screen the excipients prior to wet lab experiments. Thus, the HSP approach can be utilized as a promising tool in the preliminary screening of lipid excipients in the development of lipid nanoparticles.
Background
Conventional eye formulations are generally flushed away from the lacrimal area due to the rapid elimination of drugs from this region, with only a small amount being absorbed. The short-term precorneal contact time, coupled with corneal impermeability, leads to decreased bioavailability, necessitating repeated instillation of drops. Therefore, there is an urgent need for a system that can address these issues, maintain sustained drug action and enhance effectiveness. Numerous attempts have already been made to develop a system that can sustain drug release, with in situ gels being one promising approach.
Objectives
This study aimed to formulate and evaluate a temperature-sensitive in situ ocular gel drug delivery system for Acetazolamide (ACZ) to treat glaucoma, providing prolonged drug release.
Materials and Methods
A temperature-sensitive ophthalmic in situ gel of ACZ was prepared using a cold method and temperature-dependent polymers. The prepared gel was assessed for its appearance, clarity, pH, gelling ability, gelling temperature, sterility, viscosity, ex vivo permeation study, in vitro ocular irritancy test and in vivo pharmacodynamics study.
Results
The ex vivopermeation study and in vivo pharmacodynamics study revealed that Formulation 3 exhibited the highest drug release. The formulation was found to be sterile. The in vitro ocular irritancy test (Hen’s Egg Test-Chorioallantoic Membrane) confirmed that the formulation was non-irritating and the in vivo pharmacodynamics study on Wistar rats demonstrated that the formulation remained effective for an extended period. In situ gels extended the contact time and improved bioavailability, making them a promising approach for advanced drug delivery.
Aim/Background
The aim of this study was to enhance the bioavailability of Enzalutamide by developing cross-linked cyclodextrin nanosponges loaded with the drug (EZL-CDNS). The objective of the work is to thoroughly investigate the impact of different molar ratios of DPC and cyclodextrin on the fundamental properties of EZL-CDNS, such as particle size, entrapment efficiency, and zeta potential.
Materials and Methods
The Box-Behnken design methodology was employed to systematically investigate the factors affecting the properties of EZL-CDNS. Particle size, entrapment efficiency, and zeta potential were selected as response variables. The experimental design involved varying the molar ratios of DPC and cyclodextrin. The encapsulation of enzalutamide within the nanostructured carriers was confirmed using DSC and FTIR and morphology with SEM.
Results
The EZL-CDNS exhibited a size distribution ranging from 295 to 471 nm, entrapment efficiency values spanning from 51.7% to 90.7%, and zeta potential values ranging from -15.3 to -28.1 mV. DSC and FTIR analyses confirmed the successful encapsulation of enzalutamide, leading to its transition into an amorphous state. SEM revealed the porous structure of EZL-CDNS. Importantly, in vitro drug release profiles demonstrated a significant improvement compared to pure EZL. Pharmacokinetic Modelling supported a zero-order release pattern, suggesting an enhanced bioavailability profile. EZL-CDNS exhibited a quicker onset of action, higher peak plasma Concentration (Cmax), increased overall drug exposure, and the potential for a sustained release pattern.
Conclusion
This study successfully developed and characterised EZL-CDNS with different DPC/cyclodextrin molar ratios. Nanostructured carriers had good size distribution, entrapment efficiency, and zeta potential. The increased in vitro drug release profile and pharmacokinetic modelling results suggest higher bioavailability and sustained release of enzalutamide. Further research is needed to confirm these findings and evaluate EZL-CDNS’s clinical uses.
Background
Phloridzin, a plant compound is of interest in the field of research due to its antioxidant, anti-inflammatory, anticancer and antidiabetic activity. The current study’s objectives were to create, characterize and evaluate the toxicity of synthesized phloridzin chitosan nanoparticles in Sprague Dawley rats.
Materials and Methods
The chitosan nanoparticle was synthesized by ionic gelation method. The synthesized nanoparticles were characterized using different techniques like Dynamic Light Scattering, Fourier Transform Infrared Spectroscopy, X-ray Diffraction, Fourier Emission Scanning Electron Microscopy and %Drug Entrapment Efficiency. The toxicity and cellular uptake of phloridzin chitosan nanoparticles were further evaluated by in vitro and in vivo methods. MTT and cellular uptake assay were carried out in SH-SY5Y cells. Following in in vivo Lorke method and the Organization for Economic Co-operation and Development 407, the sub-chronic toxicity of phloridzin chitosan nanoparticles was investigated.
Results
Chitosan encapsulated phloridzin nanoparticles showed an average particle size of 246.6 d.nm in Dynamic Light Scattering analysis with a polydispersity index of 0.526 and zeta potential of 30.9mv. Fourier Transform Infrared Spectroscopy and X-ray Diffraction analysis confirmed the presence and stability of phloridzin-encapsulated chitosan nanoparticles. In Fourier Emission Scanning Electron Microscopy analysis, the dehydrated sample size was found to be 186 nm. Drug entrapment efficiency was found to be 50.38%. Cell viability range was above 60% after 48 hr incubation. Cellular uptake of nanoparticles was confirmed. The data obtained from the Lorke method indicated that LD50 exceeded 5000 mg/kg. No significant alterations were observed in hematological, biochemical and histopathological studies.
Conclusion
The findings suggest that the Phloridzin nanoparticles encased in chitosan did not significantly produce toxicity in both in vitro and in vivo.
Background
Ocular drug delivery is hindered by a number of reasons, including nasolacrimal drainage, tear turnover and eye blinking. One of the important factors is rapid removal of drug from the eye. The fast elimination rate of drug leads to the loss of drug from the conventional dosage form like eye drop. So, to avoid this problem a novel formulation was designed in which drug will entrap in micro sponges and the micro sponges will be laden into gel.
Aim
The basic purpose of the study is to formulate atenolol loaded micro sponge gel for the treatment of glaucoma. The microsponges were laden into a gel base to enhance the dwelling time of formulations in eye.
Materials and Methods
Oil in oil emulsion diffusion method is used for formulating the microsponges by using polymers like Eudragit RS-100 and Eudragit RL-100. The microsponges were subjected to different analytical tools like particle size analysis, surface topography, drug entrapment efficiency, drug loading, pH determination, viscosity, in vitro release study and evaluated. The formulation was then laden in to the gel. The gel was then characterized for pH, viscosity and drug release study. Here, we have described a novel formulation of microsponges loaded gel of Atenolol for glaucoma with the complete characterization and in vitro release study.
Results
The particle size of microsponges was found to be in the range of 7.5±0.65 to 9.2±0.5μm. The entrapment efficiencies varied from 70.12% to 80.22%. The percentage yield of the microsponges were found in the range of 75.12 to 85%. The cumulative percentage drug release varies from 60.12% to 79.32%. The microsponge loaded gel has pH in the range of 6.94±0.78 to 7.39±0.65. The viscosity of the different formulation was 220 to 287 Pa.s.
Conclusion
Microsponges loaded gel of Atenolol for glaucoma with the complete characterization and in vitro release was studied. From the in vitro studies it can be revealed that the microsponge loaded gel may be exploited for future applications for management of glaucoma
Objectives
The aim of the present study is to formulate and evaluate acyclovir loaded aspasomal topical gel by using Aloe vera gel base to enhance skin permeation and reduce the associated oral side effects of acyclovir.
Materials and Methods
Acyclovir loaded aspasomes were formulated by using Ascorbyl Palmitate, Cholesterol and Chloroform: Methanol in 9:1 ratio by Thin Film Hydration Method. Phosphate Buffer Solution (PBS) pH 7.4 was used to hydrate the film obtained. The formulated aspasomes were further characterized for Drug Content, Vesicle Size, Poly Dispersibility Index (PDI) and % Entrapment Efficiency (EE). Optimized formulation of Acyclovir loaded Aspasomes was incorporated in Aloe gel base containing Carbopol 940 (1.5%). The formulated gels were characterized for pH, viscosity, spreadability, in vitro drug diffusion and ex vivo diffusion studies.
Results
32 Factorial Design (Design Expert Software) was used for the optimization study. The optimized Aspasomal Formulation (F8) showed % Entrapment Efficiency of 87.98±0.47%, Vesicle Size of 128.6±1.8 nm and Drug Content of 84.05±0.17%. The formulated aspasomal gel resulted to have a neutral pH value, with 1557±0.213 cps viscosity and 6.9±0.163 g.cm/sec spreadability. The in vitro diffusion studies (12 hr) and ex vivo diffusion studies (12 hr) revealed that aspasomal gel released the drug in the range of 0.715±0.11% to 87.48±0.42% and 63.56±0.36% respectively and that of marketed acyclovir gel released the drug in the range of 0.661±0.51% to 34.077±0.43% and 30.64±0.62% respectively, indicating the enhanced skin diffusion of aspasomal gel revealing that the formulated aspasomal gel is a better carrier than the marketed gel for transdermal application.
Conclusion
Optimized Formulation (F8) showed better results in terms of vesicle size, % EE and drug release. Formulated aspasomal gel showed optimum results in terms of pH, viscosity, spreadability and percentage drug release. In vitro studies and ex vivo studies conclude that acyclovir loaded aspasomal gel revealed controlled drug release than the marketed gel (12 hr). The stability studies indicated no significant change in physical characteristics.
Aim
To evaluate the pharmacokinetics and toxicity properties of Valganciclovir Hydrochloride, a potent antiviral agent, using in silico models.
Background
Valganciclovir Hydrochloride is an FDA-approved antiviral agent and understanding its pharmacokinetic and toxicological properties is critical for optimizing its use.
Objectives
To assess the pharmacokinetic properties, toxicity profile and bioactive characteristics of Valganciclovir Hydrochloride using computational in silico models.
Materials and Methods
Lipinski’s Rule of Five was applied to evaluate the compound’s solubility and intestinal absorption properties. The drug’s plasma protein binding and Blood-Brain Barrier (BBB) penetration were also assessed to understand its distribution profile. Clearance rates were calculated to evaluate how efficiently the compound is eliminated from the body. Additionally, the LD50 value of Valganciclovir Hydrochloride was estimated using a rat toxicity model to understand its toxicity threshold. Pharmacological activities were further assessed using the PASS online server to evaluate its bioactive properties and potential toxic effects on non-tumor cell lines.
Results
Valganciclovir Hydrochloride exhibited high solubility and a moderate rate of intestinal absorption. The drug showed low plasma protein binding and poor BBB penetration, suggesting that its distribution is primarily localized within the body. The compound demonstrated a low clearance rate of 5 mL/min/kg. Toxicity analysis revealed an estimated LD50 value of 3,080,000 mg/kg via the oral route, indicating a relatively high toxicity threshold. The PASS analysis highlighted various bioactive properties without any toxic effects on non-tumor cell lines, with a Probability of occurrence (Pa) value lower than 0.5, further supporting the non-toxic profile of the compound.
Introduction
Tuberculosis (TB) remains one of the leading causes of infectious deaths worldwide, ranking second only to COVID-19. The rise of Multidrug-Resistant (MDR) and Extensively Drug-Resistant (XDR) TB strains highlights the critical need for novel and effective treatment approaches.
Methodology
This research explores a targeted pulmonary drug delivery system using Dry Powder Inhalers (DPI) to administer the antibiotic Linezolid (Lzd) directly to the lungs. Biodegradable Microparticles (MPs) of Linezolid were synthesized using chitosan polymer via spray drying, with Critical Process Parameters (CPPs) such as inlet temperature, aspiration rate, and feed rate optimized to achieve desired Particle Size (PS) and Entrapment Efficiency (%EE). Comprehensive evaluations were conducted, including in vivo studies, stability testing, H37 RV strain sensitivity, particle size distribution, crystallinity, flow properties, and drug-polymer compatibility.
Results and Discussion
The optimized batch of Linezolid (Lzd) MPs exhibited an impressive 89.57% entrapment efficiency with a particle size 3.9 μm. Physically, the MPs were a free-flowing powder with a bulk density of 0.171 g/cm3, tapped density of 0.2287 g/ cm3, Carr’s index of 25%, and Hausner’s ratio of 0.95. These spherical particles demonstrated sustained drug release for up to 12 hr, with a process yield of 75.91% and a moisture content of 1.58%. Importantly, the MPs showed significant inhibitory effects against the H37 RV strain of Mycobacterium tuberculosis across various concentrations. In vivo studies revealed a 55.2% increase in bioavailability with the Lzd DPI formulation, which was 1.25 times higher than the oral tablet.
Conclusion
This novel inhalation system holds the potential to reduce dosing frequency, minimize side effects, and improve patient adherence, offering a promising alternative for effective TB management.
Aim/Background
Tuberculosis (TB) is a severe airborne infectious disease caused by Mycobacterium tuberculosis, a contagious bacillus and the second leading cause of mortality. A pivotal obstacle in Tuberculosis (TB) therapy lays in the swift emergence of resilient TB mycobacterial variants during treatment regimens, thereby precipitating the dissemination of Multi-Drug Resistant (MDR-TB) and extensively drug-resistant M. tuberculosis (XDR-TB) strains. The objective of present study to evaluate toxicity of synthesized novel DprE1 inhibitors.
Materials and Methods
Research is currently directed towards discovering novel targets possessing advantageous microbiological characteristics for treating tuberculosis. Key compounds such as imidazo-pyridine, pyrazine, pyrimidine and quinazoline are pivotal elements of therapeutic significance in this endeavour. Despite this, there remains a scarcity of drugs developed for this infectious disease. Decaprenyl-phosphoryl-β-D-ribose-2-Epimerase (DprE1) is a crucial enzyme involved in arabinose biosynthesis, a component of the mycobacterium cell wall. We had synthesized series of compounds with basic nucleus imidazo-pyridine, quinazoline-4- carboxaminde and benzothiazole substituted; these compounds were subjected for in vitro antitubercular assay (Risazurine microtiter assay) and DprE1 enzyme specific studies. Three compounds (each from series) were selected here for toxicity studies. Activity of these selected compounds was 5i-0.8 μmol/L, 5g-1.01 μmol/L and 3a-1.27 μmol/L. Initial screening for acute and subacute toxicity involved albino mice weighing between 25-31 g, following OECD 423 guidelines.
Results
The research determined that a dose of 300 mg/kg was safe, with no abnormalities observed in the animals on the 7th, 14th and 28th days of the study.
Conclusion
Necropsies revealed normal average weights and vital organs (heart, lungs, liver and kidney) in all groups compared to the control group. Histopathological examinations did not indicate any abnormalities such as swelling, elongation, shrinking, deformation, or cell death in the vital organs studied.
Background
The objective of this research was to develop a nano emulsion of ipriflavone (IP nano emulsion), a soy isoflavone to enhance its solubility, bioavailability and bone regeneration potential.
Materials and Methods
The oil phase and surfactants for the IP nano emulsion were selected by plotting ternary phase diagrams. Optimisation of surfactant and oil concentrations was achieved using the Box-Behnken Design in Design Expert software. A monodisperse nano emulsion was produced using sonication and the globule size was below 100 nm. The zeta potential readings for the below -15 mV. The optimised formulation was tested for its morphology and examined using TEM imaging.
Results
In vitro drug release studies exhibited a release of 80% of ipriflavone in 90 min. The selected formulation demonstrated stability over a three-month period in accelerated conditions of temperature and humidity. The bone regeneration capacity of IP nano emulsion was tested on a dexamethasone-induced osteoporotic zebrafish model. The Caudal vertebrae bone of treated zebrafish showed significant bone regeneration compared to untreated and was confirmed by length measurements.
Conclusion
The nano emulsion displayed effective bone regeneration capability in zebrafish models, indicating the usefulness of nano emulsion in the treatment of osteoporosis.
Background
Thyroid disorder is one of the most prevalent critical issues for public health in clinical practice. Lipid profiles and cardiovascular attenuation are significantly affected by thyroid dysfunction. Thyroid dysfunction related to altitudes (height from sea level) has attracted endocrinologists worldwide.
Objectives
The current study aimed to investigate the prevalence of thyroid dysfunction and its association with lipid profile among the Saudi population residing at different altitudes and to explore the effect of altitudes on thyroid status.
Materials and Methods
In this retro cross-sectional study, a large dataset of thyroid hormones and lipid profiles from walk-in patients of both genders doing hormonal and biochemical tests at public labs and government hospital labs from sea level (Jeddah), low altitude (Najran) and high altitude (Asir) were analyzed over the last five years. The data was analyzed using IBM-SPSS version 27. (SPSS Inc., Chicago, IL).
Results
Subclinical hypothyroidism was the common laboratory finding in all three regions. The overall mean value of TC, LDL-C and TG was significantly high (p<0.05) in the hypothyroidism group in all three regions. A significant positive correlation was observed between lipid profile, lipid ratio and TSH. However, there was a negative correlation between lipid profile, lipid ratio and FT4. On the other hand, HDL-C shows a weak but significant negative correlation with FT4. The risk of developing subclinical hypothyroidism was relatively low in the Asir region (high altitude). However, the risk of developing primary hypothyroidism and subclinical hyperthyroidism was significantly high in the Asir region (high altitudes). In the Najran region, the relative risk of developing subclinical hypothyroidism and primary hypothyroidism was high in comparison to sea level.
Conclusion
The prevalence of subclinical hypothyroidism with High TC and high LDL-C follows the order: Najran>Jeddah (sea level)>Asir (high altitudes). However, the prevalence of subclinical hypothyroidism with high TG follows the order: Jeddah (sea level)>Najran>Asir (high altitudes). The risk for developing primary hypothyroidism and subclinical hyperthyroidism was high at high altitudes.
Background
Manilkara zapota, a plant with a rich history in traditional medicine, holds potential as a therapeutic agent. However, its neuroprotective properties remain largely unexplored, highlighting the need for further scientific research to understand its potential in this regard.
Objectives
This study aimed to explore the neuroprotective effects of Manilkara zapota ethanolic extract against haloperidol-induced Parkinsonism in Swiss albino mice.
Materials and Methods
The M. zapota leaf powder was extracted using 70% ethanol, followed by a qualitative and quantitative investigation. In this study, the effects of extract at 200 and 400 mg/kg (p.o.) against haloperidol in mice were assessed using various in vivo behavioural parameters including catalepsy, grid hang, horizontal bar, and parallel bar tests.
Results
The qualitative analysis of ethanolic extract identified phenols, alkaloids, carbohydrates, flavonoids, tannins, proteins, and saponins. Furthermore, the quantitative assessment indicated total flavonoid and phenol contents of 64.52 mg RTE/g and 17.6 mg GAE/g, respectively. The extract showed significant and dose-dependent enhancements in behavioural activity, motor function, muscle strength, and motor coordination. Moreover, its administration dose-dependently elevated antioxidant enzyme levels, such as glutathione, superoxide dismutase, and catalase in haloperidol-treated mice, suggesting its ability to alleviate oxidative stress. Additionally, the histopathological analysis indicated that ethanolic extract treatment restored normal architecture.
Conclusion
These findings suggest that M. zapota extract has significant neuroprotective properties against haloperidol-induced Parkinsonism, possibly via its antioxidant properties. Further research is needed to understand its mechanisms and therapeutic potential for Parkinson's disease.
Background
The prime objective of the investigation is to measure the capability of expanding the enumeration of platelet in rodent model utilizing hydro-alcoholic extract of Psidium guajava L. fruit in addition with in silico modelling on Dengue Virus Protease Inhibitors.
Materials and Methods
Using a double maceration procedure with 30% water and 70% ethanol, the harvested fruit was extracted. Heparin-induced thrombocytopenic rats were used to assess the extract's thrombocytopenic action. Prednisolone was used as the standard medication and the animals were divided into five categories. The platelet count was performed using a hemocytometer. Additionally, bleeding duration was assessed and at last in silico studies has been carried out through several softwares to identify the targeting molecule.
Results
Prednisolone, Psidium guajava L. low dosage and Psidium guajava L. high dose on the 14th day demonstrated the numbers of platelet 1732614, 874021 and 946224 respectively compared with toxicant control in the heparin-induced thrombocytopenic rat model.
Conclusion
It is clear from the results above that Psidium guajava L. significantly increased the count of platelet when equated to the toxicant control. Thus, it can be said that Psidium guajava L. plant extract significantly induces thrombocytopenia and it is found that NS2-NB3 protease is the promising target for dengue virus and in future we will try to identify the quercetin or quercetin derivatives of Psidium guajava L. responsible for producing effectiveness against the said target.
Aim
Broccoli fiber has enormous safety net as well as high pre-biotic value. Amoxicillin is although an effective drug against infections is equally harmful to gut microbiota and therefore the above side-effect impedes the use of amoxicillin. The present study deals with evaluating the dual benefits of the partially depolymerized fiber to deliver amoxicillin when the same is used as base fiber in lieu of Micro Crystalline Cellulose (MCC), as well as in protecting the gut microbiota by serving as transient refuge cum pre-biotic material.
Materials and Methods
Broccoli was partially depolymerized by alkali treatment and subjected to pre formulation studies such as powder microscopy, ash content analysis, particle density and angle of repose. Then using the partially depolymerized fiber formulated tablet dosage form of amoxicillin (500 mg). Using XRD and FTIR the interaction of partially depolymerized fiber with amoxicillin was studied. Release pattern of amoxicillin from the fiber and selective preference and binding of various probiotic species was studied simultaneously using different simulated gut systems.
Results
Study findings show that broccoli fiber instantaneously released amoxicillin and the space vacated by amoxicillin is being occupied rapidly by various probiotic species and thereby could survive the amoxicillin effect. The parachute effect of the fiber to probiotic is also reconfirmed by simulated gut digestion process and findings show the post gut digested fiber also exhibited significant prebiotic value. The fiber also met various physiochemical parameters that of MCC and also formulation dependent characteristics such as flow, compressibility and disintegration. Zero modification to the fiber vis-à-vis amoxicillin also established by X-ray Diffraction (XRD) and Fourier-Transform Infrared Spectroscopy (FTIR).
Conclusion
Probiotic microbes when encounter amoxicillin shows greater preference towards the partially depolymerized fiber and seek parachute effect from the fiber. Broccoli fiber is useful to deliver amoxicillin and also protect gut microbiome.
Background
Flavonoids are the natural product belongs to an important class of plant secondary metabolites. They are polyphenolic compounds and known for decades as a potent natural antioxidant. Curcumin (flavonoid polyphenol) and quercetin (flavonol) both are popular natural antioxidants and contributes a major role as an individual in the treatment of oxidative stress. This research study is more focused in their combination effect against oxidative stress.
Materials and Methods
In this present research, we focused on hydro-alcoholic maceration of Curcuma longa rhizomes and Morinda citrifolia fruits to extract the curcumin and quercetin respectively. Also, their role in oxidative stress was studied using in-vitro techniques.
Results
The percentage (%) yield of hydro-alcoholic extract attained from Curcuma longa rhizomes and Morinda citrifolia fruits were found to be 23.06% and 21.08% respectively.
Conclusion
Additionally, through DPPH (2,2-diphenyl-l-picrylhydrazyl) and Lipid peroxidation (LPO) assay, it was observed that curcumin and quercetin in combination gives the highest antioxidant activity when compared with their individual response at same concentration.
Background
Microgreens, the early developmental stage of edible plants, have gained prominence for their dense nutrient composition. Yet the variations in quercetin content among different microgreen species remain insufficiently explored.
Aim
The aim of this research was to use HPTLC to compare the quercetin content of commercial flax, chia, and sunflower seeds as well as the comparable microgreens.
Materials and Methods
Toluene, ethyl acetate, and formic acid were used as the mobile phase at a ratio of 5:4:0.2 (%v/v/v) for the chromatographic analysis, which was conducted using aluminum-backed silica gel 60F254 plates. To ensure that the results were precise, accurate, and reproducible, rigorous technique validation processes were carried out.
Results
Total Flavonoid content in the three seeds and microgreens studied, and the highest value was 38.92±0.4 and 76.36±0.4gm QE/100g. Well separated and compact spots (R) of quercetin (0.41±0.03) were detected. The regression equation obtained was y=0.0002x + 0.0001, with a correlation coefficient (R2) of 0.9833. The linearity range (μg/spots) was 20-100. The LOD/ LOQ (ng/spot) were 37.66/114.15. Salvia hispanica L Seeds and microgreens (0.84±0.01 and 0.88±0.005% W/W) contained maximum amount of quercetin compared to Linus usitatissimum L. and Helianthus annus L. in ethanolic extract.
Conclusion
The study revealed that the Salvia hispanica L. microgreen possess the highest quercetin content among the studied seeds and microgreens, while microgreens of all three plants are promising sources of quercetin, showcasing a remarkable increase compared to their seeds. Highlighting their potential as dietary sources rich in quercetin.
Introduction
Ziziphushamur Engl. (Vernacular name: Xamurgob) is a thorny shrub native to Ethiopia, Kenya and Somalia. The plant is extensively used in the traditional system of the Somali region in the treatment of jaundice and mental illness. Lack of prior experimental studies and wide usage in traditional medicine demands the toxicological evaluation of Ziziphus hamur Engl. The aim of this study was to evaluate the safety of Ziziphus hamur root bark by sub-acute toxicity study in male albino wistar rats. Investigation of cytokine levels were done to check for cytokine modulatory role of Ziziphus hamur, thereby providing insights on the toxicity profile and for the therapeutic property of Ziziphus hamur.
Materials and Methods
The aqueous extract of Z. hamur root bark was used for this study. The sub-acute toxicity study was carried out as per OECD guidelines. 24 albino Wistar rats (only males) were grouped and subjected to sub-acute toxicity study with orally administered extract doses of 100, 200 and 400 mg/kg body weight for 28 days. The biochemical parameters for hepatic and renal injury and hematological parameters were assessed. The evaluation of cytokines IL-6, TNF-α, INF-γ, IL-2 and IL-10 were done by ELISA to document the toxic responses in vivo. The histological studies of the liver and renal tissues were performed to check tissue damage caused.
Results
We noticed no mortality, no behavioural changes and physical changes in sub-acute toxicity experimental rats proving the preliminary evidence about the safety of the Z. hamur root bark extract. No noticable changes in water and food intake among the experimental rats proved the non-toxic nature of Z. hamur root bark extract. Body weight gain in the test group and control group of experimental rats were similar without significant difference. The biochemical analysis for liver toxicity, renal toxicity and lipid profile parameters also proved the evidence for non-toxic nature and healthier effect of Z. hamur by significant decrease in marker enzyme activities, TGL, LDL, VLDL and significantly higher level of HDL. The hematological parameters assessment showed significant beneficial effects in the treatment of the extract at the dose of 400 mg/kg body weight. The levels of IL-6 (7.68% decrease), TNF-α (7.58% decrease), IL-2 (3.46% increase) and IFN-γ (7.79% decrease) were altered without statistical significance and IL-10 was significantly increased (50.32%; p <0.001) compared to the control suggesting that Ziziphus hamur is non-toxic and safe for the use of various pathological treatments.
Conclusion
Results of this study concluded that Z. hamur has no toxicity, revealed by biochemical, haematological and histopathological parameters, up to a dose of 400 mg/kg body weight in experimental animals. Changes in the cytokine levels in sub-acute toxicity studies supported the cytokine modulatory effect of Ziziphus hamur that could benefit towards its therapeutic potential.
Introduction
Mucoadhesive microspheres for drug delivery are retained in the stomach for an extended period for localized drug release and effect.
Objectives
This research aims to explore the mucoadhesive properties of Azadirachta indica fruit mucilage when incorporated into mucoadhesive microspheres, utilizing Acyclovir as a model drug.
Materials and Methods
Employing a Box Behnken design, 13 formulations of microspheres were developed, varying Azadirachta indica Mucilage (AIFM) levels, carbomer 934P and stirring speed. Design Expert software was used to assess the impact of these factors on entrapment efficacy and mucoadhesion time. Congeniality studies involved the examination of microspheres for Acyclovir content and discharge.
Results
Results indicated that Acyclovir entrapment increased with higher AIFM levels and mucoadhesion time was prolonged in formulations with elevated AIFM levels. The optimal stirring speed was determined to be 750 rpm.
Conclusion
The study concludes that Acyclovir demonstrates effective stomach-specific drug delivery through carbomer 934P, further enhanced by Azadirachta indica fruit mucilage, particularly at a stirring speed of 750 rpm in the formulation of mucoadhesive microspheres.
Background
Favipiravir, a purine nucleic acid analogue (T-705), was used to treat SARS-CoV-2 patients. Existing methods often target specific nitrosamines in various matrices but not necessarily Favipiravir. These findings highlight the lack of a comprehensive method for detecting all seven potential nitrosamine impurities in Favipiravir API.
Materials and Methods
The current approach discusses the trace-level quantification of nitrosamine impurities (NDEA, NDIPA, NEIPA, NMBA, NMPA, NDMA and NDBA) in Favipiravir API. The set of nitrosamine impurities were separated on gradient elution mode (1.0%v/v formic acid and 100.0% methanol) throughout a 20 min run period using Symmetry C18 (150X4.6 mm, 5 μm) with a flow rate of 0.8 mL/min. The Column oven was saturated to attain a temperature of 40°±1.0°C, where the auto sampler was maintained at 50. A rinse volume of 1200 μL was employed before and after aspiration, with a dip time of 5 seconds. All the nitrosamine impurities were quantified and ionized in positive polarity mode of Electron Spray Ionization (ESI) using Multiple Reaction Monitoring (MRM).
Results
The retention times of the impurities NDEA, NDIPA, NEIPA, NMBA, NMPA, NDMA, NDBA and Favipiravir were found to be 8.51,10.54, 9.60, 6.45, 11.06, 5.41,12.67 and 6.96 min respectively. % Individual impurity in un spiked test solution has not been detected with any of the impurities. 1.29-1.98 was the %RSD for precision with 6-time repetitions Linearity was tested for specific impurities at six levels (5-100 ng/mL), with correlation coefficients (r2) ranging from 0.995-0.999. The percentage recovery of each impurity at LOQ level was observed to be 83.7-107.2, whereas 91.1-101.8 at three levels of accuracy (50%, 100%, 200%) injected in triplicate.
Conclusion
This novel LC-MS/ MS method effectively separates and quantifies seven nitrosamine impurities in Favipiravir API, offering a reliable tool for quality control. This study validates an LC-MS/MS method for detecting nitrosamine impurities in Favipiravir API according to International Conference on Harmonization (ICH) guidelines.
Background
Patient counselling is recognized as an integral component of healthcare services, providing essential guidance to patients. However, it has been observed that in India, practical attendance of designated patient education sessions is not emphasised. Therefore, the principal aim of this research endeavour was to evaluate the Knowledge, Attitude, and Practice of Healthcare Professionals (HCPs) and the Community towards patient education.
Materials and Methods
This research aimed to assess the KAP of patient counselling among Healthcare Professionals (HCPs) and Patient Caregivers (PCs) in THF. A cross-sectional survey was conducted, utilizing a self-administered questionnaire. The study highlights variations in knowledge of patient counselling practices and represents the first comprehensive assessment of HCPs’ knowledge and the community’s perception of patient counselling.
Results
The respondents consisted of 347 females (69.4%) and 153 males (30.6%), representing different professional cadres, including doctors (39.0%), nursing staff (59.4%), and Clinical Pharmacists (CP) (1.6%). Approximately 41.2% of the participants demonstrated a “Positive” attitude towards patient counselling. However, the community generally held a positive attitude towards patient counselling, highlighting areas for improvement and potential interventions to enhance patient care services.
Conclusion
There was no significant variation in the knowledge of different categories of HCPs and facility levels about patient counselling. Encouragingly, the overall attitude of respondents towards patient education and counselling was positive. Based on the above, strategies are needed to build capacity of HCPs and awareness of community to enhance the interaction between physicians, clinical pharmacists and patients.
Aim
This Study aimed to develop a stable, efficient, and reproducible RP-HPLC method that indicates stability, for the simultaneous determination of Remogliflozin Etabonate and Metformin HCl.
Materials and Methods
The Separation Process By using Methanol: 0.05 M KH2PO4 (75:25%v/v) as the mobile phase and a linear gradient protocol with a detection wavelength of 240 nm, the chromatographic separation was accomplished on (Anachrom) Cosmosil C18 (250×4.6 mm, 5 μm) Column. 35°C was the column temperature, and the flow rate was 1 mL per min. For Remogliflozin Etabonate and Metformin HCl, the retention times were determined to be 8.51 and 2.63 min, respectively. Studies on forced deterioration were conducted in thermal, photolytic, oxidative, acidic, basic, oxidizing environments. According to ICH guidelines, the method’s robustness, accuracy, precision, linearity, LOD, and specificity were all verified.
Results
The regression analysis indicated a strong correlation with a linear curve in the concentration ranges 1-5 μg mL-1 for Remogliflozin Etabonate and 5-25 μg mL-1 for Metformin HCl, demonstrating the linearity of the developed method. Moreover, the approach used in the study was distinctive in that it successfully avoided degradants even after subjecting the dugs to forced degradation. The percentage recovery of REMO and MET from the pharmaceutical dosage form was in the range of 99.33%-99.73% and 99.64%-99.93% respectively. The method was characterized by high accuracy, precision, and robustness, with LOD and LOQ values of 2.218 μg mL-1 and 6.724 μg mL-1 for Remogliflozin Etabonate and 0.582 μg/mL and 1.764 μg/mL for Metformin HCl, respectively.
Conclusion
The developed method can be used in routine analysis of bulk and dosage forms due to its adaptability, accuracy, and high precision.
Background
A quantifiable method has been developed to determine the key starting material, its intermediates and known impurities in the presence of Imipramine Hydrochloride in the final API of a synthetic laboratory sample. This newly developed Reverse-Phase High-Performance Liquid Chromatography (RP-HPLC) method is, facile, specific and reliably practical.
Materials and Methods
The separation column employed was Inertsil ODS-3 C18 with a mobile phase comprised of (A) 0.1% OPA (pH adjusted to 3.2) and (B) acetonitrile. Mobile phase A is a 100% buffer solution. Acetonitrile was used as mobile phase “B” and mobile phase B was used as 100% organic Solvent. The analytes were detected at 220 nm using a UV detector where the flow rate of the mobile phase was kept at 1.0 mL min-1 and the gradient program was set as T/% B: 0/30, 5/30, 10/80, 12/80, 15/30, 20/30 with a fixed flow rate of 1.0 mL min-1.
Results
According to the regulatory standards advised by the ICH, the performance of this method is best agreed upon by all the important parameters. The approach used in the present work can be used for process development and determining the purity of associated compounds of Imipramine Hydrochloride, key starting material (2,2-dinitro-1,2-diphenylene ethane), intermediate-1 (2-2-diamino-1,2-diphenyl ethane diphosphate) and intermediate-2 (iminodibenzyl) all in a single method.
Conclusion
This newly developed and validated method will save time and create ease by preventing the development of different methods for analyzing intermediates and impurity profiling.
Aim
This study introduces a novel simultaneous analytical quantification of Lopinavir (LPV) and Ritonavir (RTV) in drug products by using LC-MS/MS.
Materials and Methods
The present study were carried out on Acquity™ LC system from Waters paired with a triple quadrupole mass spectrometer and employing positive ion mode for optimal mass spectra. The developed method exhibited molecular and product ions for both analytes for improved resolution and signal intensity, choosing an 80:20 v/v mobile phase consists of ACN and 0.1% HCOOH in water. Strong performance was shown by the Acquity BEH C18 column, which ensured distinct peak morphologies and effective elution with retention periods of 1.89 min for LPV and 1.85 min for RTV.
Results
The approach showed remarkable linearity (r2=0.998 for LPV and r2=0.999 for RTV) over the range of 10-150 ng/mL for both medications, confirmed through recovery studies with percentage recoveries of 102.46-110.66% for LPV and 104.50-111.12% for RTV. Selectivity assessments revealed no interference, attesting to the method’s suitability for concurrent quantification. Appropriate %RSD values for peak area and retention time were found by precision evaluations to be between 1.92% and 1.33%. Robustness tests revealed stability with %RSD values for both compounds when the Limit of Quantification (LOQ) and Linit of Detection (LOD) were set at 0.010 g/mL and 0.0003 g/mL, respectively varying between 1.98% and 1.67% for peak area and 1.47% and 0.87% for retention duration. When this approach was used to examine tablet samples that were on the market, the percentage recovery values for LPV is 100.8% and 101.99% for RTV and, underscoring its efficacy for routine quality control testing and establishing it as a precise, sensitive, and robust tool for pharmaceutical analysis.
Conclusion
The suggested method’s results were determined to be acceptable and validated in compliance with regulatory requirements. This approach accurately calculated two pharmaceutical analytes simultaneously.
Introduction
Prazosin is a quinazoline derivative and a selective antagonist of the α1 adrenergic receptor. The atomic structure is C19H21N5O4 and its molecular weight is 383.41 Prazosin is a helpful medication for managing and treating various illnesses. Through the thiazide-sensitive Na-Cl co-transporter, at the early distal tubule the diuretic polythiazide prevents active chloride re-absorption, increasing the excretion of water, salt and chloride. Its molecular formula is C11H13ClF3N3O4S3.
Materials and Methods
The chromatographic settings were optimized using Design Expert Software. Column used is DIKMA spursil Column C18 (2.1x50 mm; 3.0 micrometre), ratio of the mobile phase KH2PO4: Methanol (45:55), pH 3 phosphate buffer.
Results
The flow rate 0.3 mL/min. Run time: 5 min, wavelength: 265 nm, injection volume: 4 μL. For polythiazide and prazosin, the % RSD of precision was found to be 0.8 and 0.2, respectively. Polythiazide and Prazosin had accuracy of 100.15 and 100.30, linearity COR is 0.999 for both drugs, the corresponding LOD and LOQ were determined to be 2.91 and 10.04, accordingly. The percentages of Studies on acid, base, peroxide, thermal and photodegradation revealed that 0.27, 3.93, 10.66, 7.36 and 7.07.
Conclusion
The UPLC-QbD validated method is used to determine the amounts of Polythiazide and Prazosin. This approach assessed the system's suitability, specificity, sensitivity, accuracy, linearity, precision and robustness according to ICH standards.
Background
Inflammation, a complex biological process mediated by arachidonic acid metabolites, plays a crucial role in various diseases like arthritis, psoriasis and neurodegenerative disorders. The Cyclooxygenase (COX) pathway, particularly COX-2, is a well-established anti-inflammatory target.
Materials and Methods
This study aimed to discover and evaluate novel pyrazole derivatives as potential COX-2 inhibitors via virtual screening. The 3D crystal structure of Cyclooxygenase-II (PDB: 1CX2) was prepared and optimized for in-silico investigations. Molecular docking analysis using AutoDock Vina assessed ligand-protein interactions, guided by CASTp3.0-predicted binding sites. Ligands were energy minimized and docked against the protein and drug-likeness/synthetic accessibility was predicted using SwissADME and pkCSM. Biological activity and medicinal chemistry were assessed using network diagrams, Bioavailability Radar and BOILED-Egg model for absorption and brain penetration prediction. This integrated approach facilitates the identification of potential COX-2 inhibitors with favorable pharmacokinetic profiles for further development.
Results
Through molecular docking, three compounds (D202, D305 and F505) exhibited the highest binding affinity for COX-2, surpassing the native ligand’s residual binding. Subsequent ADMET prediction revealed promising pharmacokinetic properties, including significant oral bioavailability scores (0.55) and synthetic feasibility scores ranging from 3.05 to 3.74.
Conclusion
These findings suggest the potential of these pyrazole derivatives as promising lead candidates for further development as novel anti-inflammatory agents.
Aim
To carry out Synthesis and Evaluation of novel 2, 5-substituted Pyrazolonefor Neuroprotective Potential in SH-SY5Y Human Neuroblastoma Cells.
Materials and Methods
Alzheimer’s Disease (AD) has become a serious public health concern as a result of people living longer than ever before. It is critically necessary to discover a way to halt and postpone the illness. The present study aims to determine if new synthetic analogue pyrazole derivatives may protect against toxicity caused by Aβ25-35 and its underlying mechanisms in neuroblastoma cells like SH-SY5Y. PyRx 0.9 software was used for molecular docking studies. The cells of SH-SY5Y were preincubated for 30 min with varying doses of the generated compounds (C1-C10) to induce neurotoxicity. They were then grown in Aβ25-35 (25 mol/L) for 48 hr. Cell viability was determined by MTT assay.
Results
Compounds C5 and C8 exhibited a better binding score -8.4k/cal compared to other analogues. Synthesized compounds C5 and C8 inhibited Aβ25-35-induced apoptosis in SH-SY5Y cells and protected neural cells from damage.
Conclusion
The MTT assay confirmed that compounds C5 and C8 significantly reduced Aβ25-35-induced toxicity among human neuroblastoma SH-SY5Y cells, demonstrating its neuroprotective properties.
Aim
Factor Vila is a glycosylated disulfide-linked heterodimer that belongs to the serine protease family involved in the coagulation process. Inhibition of factor Vila is one of the crucial targets for novel anticoagulant agents. Coagulation factor Vila inhibition has recently attracted attention as an intriguing antithrombotic therapeutic strategy. With the aid of X-ray crystallography and structure-based design, we were able to discover a novel series of N-phenyl-2-(phenyl-amino) acetamide derivatives that exhibited a remarkable affinity for factor Vila.
Materials and Methods
The synthesis of 22 compounds was based on the Schotten-Baumann reaction. The synthesized compounds were confirmed by physicochemical, spectroscopic and elemental analysis. In vitro, anticoagulant activity was evaluated using prothrombin determination method.
Results
Compounds 4, 7, 15, 16 and 19 demonstrated good inhibitory anticoagulant activities in vitro and showed good docking score in silico. N-phenyl-2-(phenyl-amino) acetamide provides a good template for the synthesis of novel and potent anticoagulant derivatives.
Conclusion
N-phenyl-2-(phenyl-amino) acetamide derivatives can be serving as potential drug compounds for coagulation disorders. The objective of this study was to employ in silico molecular docking and in vitro anticoagulant activity to design and synthesize structure-based new factor Vila inhibitors with enhanced potency.
Background
As clinical responsibilities continue to grow, it becomes essential for clinical pharmacists to acquire advanced competences, such as patient monitoring, patient-specific drug therapy design and evaluation, and collaboration with healthcare professionals. Pharmacy schools aspire to equip young pharmacists with competencies relevant to their current needs through the clinical practice courses they offer. Therefore, investigating the impact of clinical practice from the students’ perspectives is crucial.
Aim
The study aims to explore the influence of experiential learning provided in Pharmaceutical Care (PC) courses on students’ level of perceived professional readiness, clinical problem-solving, reasoning, and decision-making skills.
Materials and Methods
This study is a cross-sectional survey. Data were collected from a total of 278 students of PC courses using two questionnaires: Perceptions of Preparedness to Provide Pharmaceutical Care (PREP) scale and the Clinical Pharmacist Competencies Self-Evaluation Questionnaire (CPCSE).
Results
The reliability coefficients of the PREP and CPCSE questionnaires were calculated as 0.95 and 0.98, respectively. There was a statistically significant difference between the semesters in the students’ readiness perceptions, and the students’ perceptions were at the highest level at the end of the PC practices (p <0.00). A statistically significant linear relationship was found between the students’ perception of readiness at the end of the 9th semester and their problem-solving and decision-making competencies (r = 0.534 p<0.000).
Conclusion
The results of the study highlight possible areas for curricular improvement. Given that the students deemed themselves to be least prepared for the administrative procedures, the curriculum should be reconsidered in this respect. The findings derived from the competency survey further underscore the necessity for curriculum modifications about drug administration and collaboration.
Aim/Background
The purpose of the current study is to understand the COVID-19 pandemic as the greatest psychological challenge that humankind has ever faced. COVID-19 started in China in December 2019 and has conquered the whole world today. Everyone is responding to this pandemic in their own unique way and psychologically facing a global threat in the process. This paper seeks to examine how COVID-19 has psychologically affected the education sector. The purpose of the study is to analyze the prevailing situation and to study the impact of COVID-19.
Materials and Methods
ANOVA is used as a tool to analyze the impact of school closures on different levels of students in India and to determine the effectiveness and efficiency of the education sector in India.
Results
The major findings are that due to COVID-19 the number of students affected at different levels (pre-primary students, primary students, lower secondary students and upper secondary students) whereas whether students are male or female COVID-19 have an impact on different levels of students. The experience gained during this tough period will sow seeds for both health awareness and an understanding of the importance of remaining healthy to tackle any such future impediments.
Conclusion
The paper sheds light on the psychological challenges in the Indian education sector and the various steps adopted by the Indian government to ensure the nation to survive and overcome the prevailing COVID-19 situation.
Background
The “more-is-better” antimicrobial prescribing philosophy besides resistance is a significant contributor to suffering and death in children. Only a few nations have given comprehensive and comparable statistics on pediatric antimicrobial usage. However, such pediatric research is scarce in India, which necessitates antimicrobial pharmaco-surveillance.
Materials and Methods
The retrospective antimicrobial drug use study was conducted in a rural children’s hospital of south India. The antimicrobial pediatric prescription was investigated using WHO/INRUD prescribing indicators and classified according to the WHO ATC index. The antimicrobial use was calculated by using DDD and its deviation if any to prescribed daily dose was determined.
Results
Pneumonia was the most common illness and the main reason for hospitalization in 38% of infants and toddlers. A total of 79.66% antimicrobial agents were administered intravenously. Ceftriaxone (n=40, 33.9%) was the commonly used antimicrobial agent, with a PDD:DDD value of 0.84.
Conclusion
The pediatric antimicrobial utilization was adequately studied which found no discrepancies, but on contrary it was observed that prescribing practices was not consistent with WHO core prescribing indicators. This necessitates the implementation of pediatric antimicrobial stewardship programs.
Background
“Pre-eclampsia” is one of the most dangerous pregnancy complications, increasing the risk of both the mother and the baby dying prematurely. Because there have been conflicting findings on whether folic acid can reduce the incidence of pre-eclampsia, we conducted a randomized clinical trial of high-dose folic acid administration to pregnant women at a high risk of pre-eclampsia.
Materials and Methods
The study was a randomized clinical trial involving 1500 pregnant women. These women were randomly assigned into the Folic acid group (n=750) and Placebo group (n=750). From randomization (gestation period of 8 to 16 complete weeks) to birth, group 1 received 4mg of folic acid and group 2 received placebo per day. Participants were also analyzed for compliance over ≤50%, 50-<75% and ?75%. Four follow-ups were scheduled at 24-26, 34-36 gestational weeks, after birth and 42 days post-partum. The primary outcome measure was the incidence of pre-eclampsia. In contrast, secondary outcome measures included early pre-term birth, stillbirth, neonatal death, perinatal mortality, early-onset sepsis and admission to NICU for 24 hr or more.
Results
The present investigation showed that the incidence of pre-eclampsia was significantly lower in the folic acid group compared to placebo group (5.3% vs 10%) with a Risk Ratio (RR) of 0.53 95% Confidence Interval (CI): 0.53 to 0.79. Similarly, the incidence of secondary outcomes was also reduced in the folic acid group compared to the placebo group.
Conclusion
The results of the study lend support to the idea that pregnant women with “hypertension” should take high-dose folic acid supplements as a prophylactic measure against pre-eclampsia.
Background
Obesity is typically characterized by excess deposition of adipose tissue. Along with dietary management, increase in physical activity, lifestyle modification, surgical intervention, drug treatment is also available which aid in weight loss. However, most of these drugs exhibit side effects like insomnia, irritability, epigastric discomfort, constipation, some are even habit-forming drugs. Hence, the present study was designed to screen, evaluate and discover newer safer anti-obesity drugs from plant sources.
Materials and Methods
In this study, the aqueous and 90% alcoholic extracts of roots of Bauhinia variegata Linn. were prepared and evaluated for their anti-obesity activity. Obesity was induced using the cafeteria diet in female Albino Wistar rats weighing 150-200 g. The parameters evaluated were body temperature, body weight, serum biochemical parameters, internal organ weight and histology of liver tissue.
Results
The results of the study show that the extracts were capable of reducing body weight, inducing thermogenesis and maintaining serum biochemical parameters. Among the extracts the aqueous extract of roots of Bauhinia variegata Linn. has shown better pharmacological activity than the alcoholic extract. Therefore, this group of animals were subjected to histological studies which showed only mild fatty liver change when compared to the positive control group.
Conclusion
Further studies are required for evaluating the mechanism of action, isolating the compound/s responsible for the activity, structurally elucidating the same to then formulate it into anti-obesity drug with enhanced efficacy.
Aim
The objective of this study is synthesis of 1,2,4-triazole derivatives, evaluation there in vitro antimicrobial activity and showing the molecular docking.
Materials and Methods
Two series of 5-alkylthio-3-aryl-4-phenyl-1,2,4-triazoles were successfully synthesized. The 1,2,4-triazole thiol was produced via cyclization reaction using the hydrazide compounds (2-hydroxybenzohydrazide and 5-bromofuran-2-carbohydrazide), which were then employed as nucleophilic species to attract various kinds of alkyl halides to synthesis the final compounds. All produced compounds underwent spectroscopic characterization and tested their antibacterial and antifungal activities. With synthetic ligands, molecular docking studies were conducted against the proteins 1AJ0, 1JIJ, and 4ZA5 to identify the crucial interactions underlying antimicrobial activity.
Results
UV-visible, FTIR, 1H-NMR and CHNS analysis were confirmed the chemical structures and purity. Initial antibacterial screening results showed that several produced compounds 1e, 1f, 2e, and 2f have good inhibitory effects, whilst some compounds 2e demonstrated high antifungal activity when compared to the control drug fluconazole. Two active substances, 1e and 2e, showed a moderate level of toxicity, with LD50 values of 3.5 and 2.3 g/kg, respectively. The strongest compounds, 1e, 1f, 2e, and 2f, demonstrated high binding energy antibacterial and antifungal activity, which were supported by docking analysis.
Conclusion
Triazole derivatives were synthesized by multi-reaction steps with high yields. Some synthesized triazole derivatives showed promising antibacterial and antifungal activities as compared with parent compounds and standard drugs. The results of antimicrobial activities of compounds were enhanced by good affinity of molecular docking of these compounds with the active site of proteins as compared with standard drugs amoxicillin and fluconazole.
Aim/Background:
Our objective is to describe the patterns of prescribing drug combinations and lifestyle modification in which therapy focuses on SGLT2 and DPP4 inhibitors and dose variation according to the blood glucose level and the effective therapy in patients with T2DM.
Materials and Methods:
Using both prescription and questionnaire analysis, a cross-sectional study conducted in Odisha, including 100 diabetic subjects, is considered to evaluate effective combination therapy by comparing different glycemic indexes with Lifestyle modification.
Results and Discussion:
Age and duration of detection of diabetes are the factors through which the gender basis comparison is made and comparing the glycemic index according to different consultations, the drug therapy is considered so as to achieve safe and no or less hypoglycemia. Males (52%) constituted more than female (48%) respondents. The presence of T2DM was responded by 57%, whereas 68% suggest there is no permanent cure for T2DM. The lifestyle changes with medicine, in control of T2DM has been reported by 59% of respondents. There is a significant change (p≤0.005) in FBS and PPBS levels as compared from 1st visit to 5th visit with the effective combination of Metformin and teneligliptin.
Conclusion:
DPP4 inhibitor and SGLT 2 inhibitor are the newer antidiabetic drugs used as add-on therapy to minimize different risk factors and enhance the quality of life. It is essential to consider diabetes education to improve knowledge of the risk factors associated with type 2 diabetes.