Contents:
ABSTRACT
In recent years, dyslipidemia, a major risk factor for cardiovascular diseases is on the rise globally due to sedentary lifestyles and unhealthy diets. Though abundant data pertaining to the factors influencing dyslipidemia, the mechanism of action of various drugs and the pathogenesis of the disease are available in the literature, the disease is poorly understood. Animal models play a crucial role in investigating the pathophysiology and aid in developing effective formulations. Despite extensive research being carried out in the arena of dyslipidemia, there is no adequate knowledge about the most suitable in vivo model. A systematic literature search was carried out to review the animal models such as rats, mice, rabbits and zebrafish models with chemical-induced, diet-induced and drug-induced methods that have been used to study dyslipidemia. This review focuses on the mechanism involved in the dyslipidemia induction techniques explored by researchers along with their applications and limitations. The induction methods reported are expected to provide better insight in selecting an appropriate model to draw precise conclusions.
ABSTRACT
Annona muricata Linn. (A. muricata) is a tropical evergreen fruit tree belonging to Annonaceae family, also referred as graviola, soursop or corossol. The chemical compounds isolated from this plant have linked to the ethnomedicinal properties and its anticancer properties. This review focus to highlight in vitro anticancer potentials of acetogenins isolated from A. muricata, which are potent inducer of Bax-Bak and Caspase-3 related pathways. More than 200 chemical substances that have been isolated and characterised from this plant and the most significant are alkaloids, phenols and acetogenins. A. muricata has a distinct collection of C35 or C37 long chain fatty acid derivatives that are produced from the polyketide pathway and are unique to this family. The main bioactive ingredients bring together many scientific investigations on A. muricata, and acetogenins have been the subject of multiple research and reviews. These acetogenins preferentially destroy cancer cells through the action as a DNA topoisomerase I toxin, prevent cancer cells from entering their G1 phase, activate pathways linked to Bax and caspase-3, and block NADH-ubiquinone oxidoreductase (complex I) in mitochondria, while having no impact on healthy cells. In addition to the in vitro study, further in vivo tests are required to demonstrate these pathways.
ABSTRACT
The Research and Development in benzothiazole-based medicinal ingredients have turn into a hastily on the rise and gradually more lively topic. Broad number of compounds having Benzothiazole (BTZ) moiety are involved in the treatment of a various number of diseases with maximum curative potency. This review is aimed to afford modern progress in the synthesis of Benzothiazole analogues associated to the green chemistry. Literature surveys on scientific national and international journals, books as well as electronic resources were performed. Benzothiazole and its moieties containing various numbers of structural multiplicities play evidence in search of different pharmacological actions. This review steadily grants an all-inclusive review in the progressive developments of Benzothiazole-based compounds of medicinal chemistry as antibacterial, Hepatitis-C virus inhibitors, anti-alzheimer’s disease, anti-inflammatory and analgesic, antioxidant, anti-convulsant, anti-diabetic, anti-histaminic, anti-malarial, anti-depressant and other medicinal agents. The wide field of pharmacological activity in creature benzothiazole derivative indicates that this string of compounds is of an unquestionable curiosity. This review is also believed to be extra efficient in finding pathogenic problems and diagnostic analogues is ready to find new-fangled judgment in the chase for drawing of a reduced amount of toxic and additional active Benzothiazole-based drugs. It is projected that this knowledge would give rise and show enormous impact for the growth of synthetic pathways for benzothiazoles with expansion of novel synthetic approaches.
ABSTRACT
In the present work, a bibliographical survey of the toxicity of some plants of the southern Tunisia’s flora was conducted on several methanoic extracts from miscellaneous toxic plants of the southern Tunisian flora and chosen from among the most used plants in traditional medicine. In Tunisia, a host of extracts from about twenty plants have shown spasmolytic properties, while several extracts from some plants showed a high toxicity and 3 extracts from 2 plants proved curative properties. In this article, we present about ten poisonous plants, classified in alphabetical order of the vernacular name, for which severe poisoning, even fatal, have been reported. It mainly consists in plants with cardiac and/or neurological toxicity. Following a succinct description of the plant, we approach the clinical, therapeutic and analytical aspects.
Introduction
Dioxins represent a category of enduring environmental contaminants that possess the capability to elicit endocrine disruptions and a spectrum of ailments, most notably encompassing malignancies, immunological impairments, and nervous system impairments. These chemical compounds incite the generation of Reactive Oxygen Species (ROS), consequently instigating cellular toxicity through the activation of the Aryl Hydrocarbon Receptor (AHR). Given the significant noxiousness associated with dioxins, it is imperative to implement decisive actions aimed at mitigating ongoing ambient exposure. In spite of advancements in comprehending the origin and fundamental mechanisms of persistent environmental pollutants, the development of efficacious interventions has remained an elusive endeavor.
Objectives
This investigation focuses on the distinct pharmacological mechanisms inherent in polyphenolic constituents that have been hitherto explored in relation to various dioxin-induced toxicities, both in in vivo and in vitro models.
Materials and Methods
Preclinical studies were identified through systematic searches of PubMed, Embase, and the Cochrane Library, while clinical trials were retrieved from ClinicalTrials.gov and PubMed databases.
Results
Preclinical research unveils the significant efficacy of phytochemicals in mitigating dioxin toxicity. Conversely, clinical findings exhibit a mixed spectrum of outcomes, but hold promise for the use of phytochemicals as adjuncts to conventional therapies for diverse dioxin-induced toxicities. These outcomes suggest that polyphenols may exert substantial influence on disease-related mechanisms such as oxidative stress, inflammation, apoptosis, and gene regulation.
Conclusion
In our assessment, this represents the inaugural comprehensive review encompassing in vitro and in vivo investigations concerning the molecular-level interactions between various environmental contaminants and polyphenols. Furthermore, additional clinical investigations are warranted, with a focus on the appropriate patient populations, identification of relevant toxicity biomarkers, and elucidation of the impact of phytochemicals on these parameters.
ABSTRACT
In the pharmaceutical field, various diagnostic tools and delivery systems are available which used for the identification of diseases and treatment. Aquasome is a new type of vesicular drug delivery system. It is a self-assembled nanoparticle with a three-layered structure consisting of a nanocrystalline central core on top of that carbohydrate layer is present that adsorbs the bio-actives or drugs on that layer. A carbohydrate coating protects and preserves the structural integrity of the bioactive. Aquasome has great potential because of its properties. It acts as a carrier for various therapeutic drugs and bioactive materials. This review provides information about aquasome, their historical development, the importance of carbohydrates, their properties, advantages, disadvantages, limitations, characterization techniques, applications, route of administration, patents, marketed products, consequences, challenges, and prospects. Therefore, researchers will benefit from this review, about aquasome, their applications and prospective in pharmaceutical science.
ABSTRACT
The traditional drug discovery process is expensive, time-consuming, and often leads to a high failure rate. The development of numerous new medications in the pharmaceutical sciences is only one example of how the advancement of artificial intelligence has opened up exciting new opportunities for developing intelligent modelling. Machine learning and deep learning are two examples of artificial intelligence that can sift through large datasets in search of promising new drugs. AI algorithms can predict the binding affinity of molecules to specific targets, helping researchers narrow down the pool of potential drug candidates. Pharmacokinetics and pharmacodynamic are essential aspects of drug development. Drug formulation development requires extensive testing and optimization of various parameters. AI models can quickly analyze data from multiple experiments and identify the most promising formulations, saving time and resources. New pharmaceuticals may be developed and brought to market at a reduced cost and in a shorter amount of time with the use of AI-based optimisation approaches. Absorption, Distribution, Metabolism, and Excretion (ADME) are only some of the aspects of pharmacological physiology that may be modelled and predicted with the use of artificial intelligence. By integrating AI models into the drug development process, researchers can gain a deeper understanding of a drug’s pharmacokinetic and pharmacodynamic properties. This knowledge helps in designing drugs with improved efficacy and reduced side effects. So, in present topic authors tried to give insights how AI is playing a transformative role in pharmaceutical sciences. As AI technology continues to advance, the future of pharmaceutical sciences looks brighter than ever.
ABSTRACT
Background
Depression is a common mental illness, with an estimated 3.8% of global population affected. In the pathophysiology of depression, ketamine acts quickly in patients. Treatment with low-dose ketamine upon administration to stressed C57BL/6J mice is now a major translational research area to facilitate further innovation.
Objectives
The present work was aimed to establish a depressant like animal model after 6 days of LPS injection, where LPS did not promote body weight loss.
Materials and Methods
Peripheral administration of low dose of Lipopolysaccharide (LPS) activates cytokines and culminate in a distinct depressive-like behavioral syndrome, measured by increased duration of immobility in the forced swim and anhedonia in sucrose preference tests. Cytokines like TNF-α, IL-6, IL-1β and IFN-γ were determined in brain homogenate and in plasma using western blot performed with automated Jess system (ProteinSimple) and ELISA respectively.
Results
Ketamine prevents development of depressive-like behavior by decreasing swimming behavior and increasing preference to sucrose in stressed animals. Ketamine treatment reduced the LPS induced secretion of IFN-γ (p <0.05 for 30 mpk), IL-6 (p <0.05 for 30 mpk), TNF-α (p <0.0001 for 30 mpk) and IL-1β in plasma. Similarly, ketamine treatment reduced the LPS induced secretion of IFN-γ (p <0.001 for 10 and 30 mpk), IL-6, TNF-α (p <0.01 for 10 and 30 mpk) and IL-1β (p <0.05 for 10 mpk, p <0.0001 for 30 mpk) in brain. The plasma and brain concentrations of ketamine were analysed using LC-MS/MS and Brain/ Plasma ratio (B/P) of ketamine at 10 and 30 mpk were calculated as 0.70 and 0.82 respectively.
Conclusion
In summary, these data emphasizes that ketamine treatment modulate cytokine level, showed good brain to plasma exposure and provides its anti-stress effects in the C57BL/6 mouse strain, which may be possible reason for the anti-depression property and is relevant to human stress-induced depression.
Aim/Background
In this work, a novel method for improving the quality of healthcare in the diagnosis of Interstitial Lung Disease (ILD) using High-Resolution Computed Tomography (HRCT) images is proposed.
Materials and Methods
In contrast to previous research that necessitated the human identification of Regions of Interest (ROI), a two-phase deep learning method is presented. First, multi-scale feature extraction is used to precisely segment the lung in HRCT images using a conditional Generative Adversarial Network (c-GAN). A Support Vector Machine (SVM) classifier classifies the characteristics extracted by a pretrained ResNet50 from the segmented lung image into seven ILD classes in the second step.
Results
The two-step approach that is being offered improves efficiency by doing away with the necessity for ROI extraction. The superiority of the method is demonstrated by performance comparison with patch-based and whole-image-based algorithms. The suggested method reduces false alarms by achieving a maximum classification accuracy of 94.65% for the normal class. Despite having the lowest accuracy (84.12%), the consolidation class performs better than other whole-image-based methods.
Conclusion
The suggested two-stages ILD classifier performs much better due to the step-by-step improvement in the deep learning method. This work lays the groundwork for advanced decision support systems in the pharmaceutical industry and advances pharmaceutical research and education. The method proposed improves knowledge of the pathophysiology of ILD and allows for customized treatment approaches.
Background and Objectives
Hemorrhoids are defined as swollen veins in the anus and lower rectum. Hemorrhoids are a common medical problem and have a negative impact on people’s lives. The drugs that are available on the market are limited, and therefore, the objective of the present research is to develop and evaluate a lidocaine and nitroglycerin ointment combination for enhanced external hemorrhoid treatment.
Materials and Methods
Five formulations of 0.1% lidocaine and 0.1% nitroglycerin ointments (F1-F5) were developed using hydrocarbon bases (B1 and B2), hydrophilic petrolatum B3, hydrophilic B4, and emulsifying base B5. Different physicochemical parameters were conducted to evaluate the quality of the studied formulations.
Results
Cracking was observed for F1 and F2 and phase transitions were noticed for F4 and F5. While, the hydrophilic petrolatum base formulation F3 showed the best physical stability up to one month with high uniformity with a drug content of 107.5% and a calibration curve R=0.9999. Docking study confirmed the activity of lidocaine and nitroglycerin towards hemorrhoids through conventional hydrogen bonds with target proteins 6s3a and 6t3w, respectively. F3 was tested by nine patients who suffered from external hemorrhoids for seven days. Patients reported a decrease in hemorrhoid grain sizes with excellent tolerability.
Conclusion
The developed single formulation of two different drugs, lidocaine and nitroglycerin, has synergistic action and is well-tolerated treatment option for external hemorrhoids, as it not only decreases the hemorrhoid symptoms (pain and itchy) but also eliminates the side effects like headache that arise when the drugs are administered alone.
Background
The combination of two drugs celecoxib + tramadol and diclofenac sodium + tramadol with different mechanisms of action is better for achieving effective pain control.
Materials and Methods
The simple reproducible mathematically modified UV spectroscopic methods were established for concomitant evaluation of the binary combination of celecoxib + tramadol and diclofenac sodium + tramadol formulations. The first technique is predicated on separating the pure zero-order spectra of TDL and CCB from the mixture spectra and quantification at their lambda max. The second and third method involves the ratio absorption difference and ratio first derivative spectroscopic method for quantification of DFS and TDL. Additionally, we followed ICH guidelines to validate these approaches for specificity, accuracy, and precision.
Results
Both formulations were effectively analyzed using the proposed methods, with results falling into the series of 2-50 μg/mL for TDL, and 1-30 μg/mL for DFS and CCB. The good recovery of 98.56% -101.48% with low relative error and percentage relative standard deviation verified the methodologies’ correctness and repeatability. Finally, proposed mathematically modified spectroscopic procedures were exploited for quality control of analytes from formulation and manually prepared mixtures. The determination of % of retrieval of an added known quantity of authentic medications of CCB, TDL, and DFS to the powdered pill served as additional evidence of correctness.
Conclusion
The established UV spectroscopic techniques are simple, rapid, and perfect for simultaneous quantification of CCB, DSF, and TDL from the solid dosage forms. The assay results also confirmed the nonexistence of tablet adjuvants intervention in the quantification of medicines in the tablets Therefore, these approaches can be utilized for systematic quantification of these drugs in the binary formulations without chemical separation.
Background
Bovine Albumin Nanoparticles (BAN) have a high magnetic susceptibility and great potential for biomedical applications.
Aim
Evaluate the in vitro effects of magnetic BAN on mouse renal and submandibular cells.
Materials and Methods
The ferromagnetic iron oxide Nanoparticles (NPs) were lyophilized and diluted in Dulbecco’s modified eagle culture medium. The diameters of the NPs were measured. Mouse renal and submandibular cells were cultured from an initial passage of 3×106 cells in 100 cm2 culture flasks. Bovine Albumin Nanoparticles were applied to the culture at a concentration of 260, 160 and 85 μg/mL to test the number of viable or degenerating cells. Detection of apoptic and necrotic cells were carried out using the color variability and the nucleus morphology, chromatin condensation and fragmentation.
Results
The staining test with acridine orange and ethidium bromide allowed the distinction between viable, necrotic and apoptotic cells in each of the experimental groups. Frequency of cells in degeneration was significantly greater in the BAN-treated groups at concentration 260 μg/mL and 160 μg/mL. The comet assay revealed the frequency of cells with DNA damage; Mouse renal cells have an irregular shape, a large nucleus and numerous cytoplasmic projections. Their cytoplasm is rich in membranous organelles, maintaining the characteristic ultrastructure pattern of secretory cells. Mouse submandibular cells treated with BAN showed no changes in ultrastructure but had agglomerates of NPs inside and a greater amount of BAN agglomerates in the outside.
Conclusion
Results obtained in this article point to the biocompatibility of the sample of magnetic albumin polymers.
Background
The therapeutic efficacy of an active Pharmaceutical ingredient depends on its solubility in body fluids. The low bioavailability of nearly 90% of new active Pharmaceutical ingredients and 40% of the existing molecules is attributed to their poor solubility. The current study aimed to improve the oral bioavailability of lapatinib by designing and optimizing nanostructured lipid carriers for it.
Materials and Methods
The formulation utilized the microemulsion technique as a method of preparation and the Box Behnken design was used for optimization.
Results
The average particle size, drug entrapment, and release, in percentages, were observed to be 237.09 nm, 72.32%, and 74.66% respectively.
Conclusion
In vitro studies proved that NSLC significantly releases a drug more than the marketed formulation.
Background
Even though the natural polymers are biodegradable, non-toxic and cost effective, but these suffer with some of drawbacks like uncontrolled drug release, enzymatic degradation, reduction in viscosity on long term storage, thermal instability etc. The aforesaid limitations can be overcome by grafting of natural polymers to obtain high performance biomaterials for drug delivery system.
Materials and Methods
Purified fenugreek and mesquite gums were grafted with acrylamide using Ceric Ammonium Nitrate (CAN) as free radical initiator. Confirmation of grafting was done by elemental analysis and FT-IR spectroscopy. Grafted copolymers were tested for its biodegradability in microorganisms and toxicity in Drosophila melanogaster. Nine batches of mebendazole tablets (F1 to F9) were prepared using mixture of acrylamide grafted fenugreek and mesquite gum polymer by 32 factorial designs. Compressed tablets were tested for post-compression compendia parameters.
Results
FT-IR confirmed the grafting and compatibility between drug and synthesized copolymers. Synthesised graft copolymers showed significant swelling index, water retention capacity, viscosity, hydration capacity than the pure gum polymers. Compressed tablets showed hardness (5.5 to 6.6 kg/cm2), friability (less than 1%). thickness (3 mm) and complied weight variation test as per compendial standards. Further tablets were coated with Eudragit RS 100 demonstrated small amount of drug release in 5 hr and maximum amount of drug released in colonic region. Hence, after reaching colonic region drug release extended upto 12 hr due to satisfactory drug release by copolymers.
Conclusion
Grafted copolymers were biodegradable, non-toxic and showed higher swelling index then pure polymers. These copolymers can be used as drug release retardant in the tablet formulation.
Aim
Using atenolol as a model active pharmaceutical and galactomannan from the seeds of Trigonella foenumgraecum as a mucoadhesive polymer, an effort was made to develop a gastroretentive bioadhesive floating delivery system to improve the residence time in the stomach.
Materials and Methods
Different formulations were made with Hydroxypropyl Methyl Cellulose (HPMC) and galactomannan. Galactomannan was chosen because of its exceptional swelling properties in aqueous environments. In this investigation, citric acid and sodium bicarbonate were utilized as gas-producing components. Pre- and postcompression evaluations were performed on the manufactured tablets. The floating properties as well as the atenolol release pattern were investigated.
Results
The extracted polymer was characterized using various techniques and found to be similar to literature. The results from GC analysis showed a residual acetone content of 0.127 ppm, indicating that the extracted polymer is safer to use in the formulation of gastroretentive tablets. The physicochemical properties of the manufactured tablets were satisfactory in terms of swelling index, release characteristics, and buoyancy pattern. All of the manufactured batches had adequate in vitro buoyancy. The gastroretentive tablet exhibited axial and radial swelling throughout the in vitro buoyancy test. According to the testing, the formulation remained buoyant for approximately 8 to 12 hr.
Conclusion
According to the results of the evaluation, the manufactured tablet has a pleasing look, is heat stable, and is therapeutically efficient. F3 was determined to be the optimal formulation based on the data collected.
Objectives
Rebamipide, a gastroprotective drug, is used for preventing and treating ulcers but it has low aqueous solubility leading to poor bioavailability (10%). It acts both locally and systemically to provide gastroprotection and ulcer healing effects. The therapeutics of Rebamipide can be improved by enhancing its aqueous solubility and by sustaining its release in the stomach.
Materials and Methods
The above objective was fulfilled by preparing solid dispersion of Rebamipide by solvent evaporation method for aqueous solubility enhancement which was incorporated in floating beads by emulsion gelation method using different concentrations of sodium alginate and olive oil for prolonged gastroretention. The beads were characterized for size, swelling, entrapment efficiency, floating lag time, floating time and in-vitro drug release.
Results and Discussion
The solubility of rebamipide in solid dispersion was found to be 18.66 mg/mL which was much greater than its normal value (1.3 µg/mL). The size of beads varied between 2.03 mm-2.52 mm. The swelling index was found to be 12-28%. Entrapment efficiency was 90.1-96.9% proving excellent entrapment of drug by the method chosen. Floating lag time of optimized formulation (F6) was 3 sec with 90.2% drug release at12 hr showing adequate sustenance of drug release.
Conclusion
The solid dispersion loaded floating beads would prove effective in preventing and treating stomach ulcers because of enhanced aqueous solubility of drug in solid dispersion form resulting in higher drug concentration in gastric fluid, sustained release of drug and greater gastroretention time, giving improved therapeutics both locally and systemically.
Background
Tolperisone Hydrochloride (HCl) is a muscle relaxant that relaxes muscles by acting on the Central Nervous System (CNS). It acts at the spinal cord level by blocking calcium and sodium channels. It primarily inhibits transmitter release from primary afferent terminals through pre-synaptic inhibition via simultaneous action on voltage-gated sodium and calcium channels. Its elimination half-life t is 1.5 to 2.5 hr. To maintain a constant plasma concentration, conventional Tolperisone HCl tablets are administered multiple times in divided dosages, which results in patient noncompliance. This problem can be overcome by preparing Tolperisone HCl sustained-release tablets.
Materials and Methods
Tolperisone HCl sustained release matrix tablet was prepared by utilizing the wet granulation method with Hydroxypropyl Methylcellulose (HPMC K100) and Ethyl Cellulose (EC) in combination at different ratios. Evaluation: The powdered blend was evaluated for adequate flow properties using Carr’s compressibility index, tapped density, bulk density, angle of repose, and Hausner’s ratio before compression. The compressed tablets were then further evaluated for diameter, friability, content uniformity, thickness, hardness, weight variation, and in vitro drug release.
Results
The drug release study showed that HPMC K100 and EC in combination were able to sustain the drug release in acid buffer pH 1.2 for the first 2 hr, followed by phosphate buffer pH 6.8 for the next 12 hr. It is also suggested that if the amount of ethyl cellulose increases, drug release decreases because ethyl cellulose is a water-insoluble polymer. All the formulations show drug release for more than 12 hr.
Background/Aim
The aim of the study was to improve the dissolution profiles of Oxcarbazepine (OXC) from its tablets. This study was done to evaluate the effects of different formulation variables, i.e. type of non-volatile liquid vehicles on oxcarbazepine dissolution rate from its tablets.
Materials and Methods
The liquisolid tablets were formulated with three different liquid vehicles, namely Polyethylene glycol 200, Propylene glycol and 20% Tween 80 aqueous solution. Micro-crystalline cellulose was used as a carrier material, silicon dioxide as a coating material and sodium starch glycolate as super disintegrate. The empirical method introduced by Spireas and Bolton (1999) was applied strictly to calculate the amounts of coating and carrier materials required to prepare fast dissolving tablets of OXC using liquisolid technique. The tablets passed all the routine quality control tests prescribed by official books. In vitro drug dissolution testing of the liquisolid tablets were done and compared with commercial tablets in 1% SLS solution as dissolution media as per USFDA.
Results
It was found that the dissolution rate of oxcarbazepine was highest from liquisolid tablets of oxcarbazepine formulated using PEG 200. Differential scanning calorimetry, PXRD and Fourier transform infrared evaluation of our best tablet Formulation (F2) indicated that there is no physico-chemical interaction between OXC and the excipients.
Conclusion
In vitro dissolution testing, DSC, PXRD and FTIR studies confirmed F2 as the best formulation with respect to drug dissolution rate and revealed that there is no incompatibility between the drug and excipients used in the formulation.
Background
The biochemistry of secondary metabolites of marine origin has been identified as a promising area for obtaining new and potent pharmaceutical agents. These secondary metabolism molecules may have important functions such as anti-biotic and anti-parasitic activity, mediate symbiotic relationships between organisms and even have reproductive functions, representing a great ecological advantage for the survival of marine organisms.
Aim
This study aimed to characterize the secondary metabolites of the sea squirt Diplosoma listerianum and its associated micro-organisms.
Materials and Methods
The squirts were frozen, dried, weighed, roughly crushed and extracted using methanol and dichloromethane (1:1). The crude extract was dissolved in methanol and fractionated in four solvents of increasing polarity: saturated hexane, acetic ester, butyl alcohol and water. The active substances were isolated by liquid chromatography, purified and their structures determined. Bacteriostatic action against the crude extract was assessed using longitudinal in vitro growth in Müller-Hinton broth.
Results
D. listerianum’s crude extract showed antibiotic activity against various pathogenic microorganisms. Analysis of variance and Tukey’s multiple comparison tests indicated significant differences among exposure times. Mouse fibroblasts exposed to the crude extract showed fragmented and sickle-shaped nuclei, visible centrosomes, abnormal multipolar mitotic spindles and endoplasmic reticulum vacuolization. The phytagel assay showed a correlation between the gel’s algal density and associated organism numbers. The protein tyrosine kinase assay showed that the crude extract had enzyme-inhibiting properties. Preparative high-performance liquid chromatography, Sephadex column chromatography, high-resolution electrospray ionization mass spectrometry and electron impact mass spectra identified zeaxanthin, tubastrine (an epidermal growth factor receptor inhibitor), inosine, guanosine, oxazolidin-2-one, LL-PAA216 and 2-aminododecan-3-ol.
Conclusion
Marine biotechnology generates technological products from the diversity of marine organisms and their strategic adaptations to the extreme conditions of the seas and, in turn, presents itself as a promising source of bioproducts and processes, being able to solve issues in areas such as health, food safety, cosmetics, agriculture, pollution control, climate and industry, among others.
Introduction
A major feature of drug-resistant cancer is the overexpression of transcription factors. During the study, reserpine, an indole alkaloid, was examined for its anticancer effects on cancer with drug resistance.
Objectives
The objective of this study was to explore the anti-apoptotic impacts of reserpine in drug-resistant cancer cells by impeding the nuclear translocation of NF-κB and STAT3.
Materials and Methods
For the in vitro study of reserpine’s anticancer activity, human drug resistance cancer cell line KB-ChR-8-5 was selected. A MTT assay was used to evaluate the cytotoxicity of reserpine. Reactive Oxygen Species (ROS), comet test, Mitochondrial Membrane Potential (MMP) and AO/EtBr staining were used to assess cell proliferation, DNA damage and apoptotic activation. Conducting western blot analysis was employed in this research study to examine the effect of reserpine on KB-ChR-8-5 cells express levels of proteins related to apoptosis markers and transcription factor expression.
Results
We found that, reserpine decreased cell viability, increased ROS levels, enhanced DNA damage and decreased mitochondrial membrane potential due to its antioxidant properties. Moreover, the suppression of NF-κB and STAT3 facilitates the upregulation of specific apoptotic proteins, such as Bax, cytochrome C, Caspase-9 and Caspase-3, which simultaneously inhibit cancer growth.
Conclusion
These results imply that reserpine suppressed NF-κB and STAT3 nuclear translocation process, which led to ROS-induced apoptosis and tumour cell death.
Background
Acquired Immunodeficiency Syndrome (AIDS), caused by the Human Immunodeficiency Virus (HIV) was initially associated with rapid disease progression and high mortality rates. However, advances in drug delivery systems have aimed to optimize therapeutic outcomes, especially for medications facing challenges such as toxicity, uneven distribution, instability and formulation complexities.
Materials and Methods
In this study, we introduce TCS-PEG/MMT composites, a novel formulation designed for antiretroviral activity. This formulation consists of a blend of Medical clay (MMT) and Thiolated Chitosan and Polyethylene Glycol (TCS-PEG), which are biodegradable materials. Using Design Expert software, we optimized the loading procedure of lamivudine onto chitosan (X1), MMT (X2) and PEG (X3) to achieve desired Entrapment Efficacy (EE) and particle size (PS). The desirability technique helped determine an optimal formulation with 3 g of chitosan, 3 g of MMT and 2.5 g of PEG.
Results
The optimized formulation exhibited an EE of 79.58% and a PS of 592.32 nm. We conducted comprehensive analyses on the Optimized formulation (O-LMD-NC), including assessments of swelling characteristics, surface morphology, drug loading, entrapment efficiency and particle size. Water absorption of O-LMD-NC samples gradually increased over time, reaching a maximum of 13.5 g/g after 24 hr. In vitro drug release studies confirmed sustained release of lamivudine over a 24 hr period.
Conclusion
Our findings suggest that LMD-loaded polymeric nanocomposites offer a promising approach to enhance the efficacy of AIDS treatment.
Background
In current research, Zinc Nanoparticles (ZnNPs) were synthesized using green synthesis technology. It is the best method which is eco-friendly and cost-effective. The extract of fungus Cordyceps militaris was used for this purpose, which was followed by muffle furnace assisted synthesis of zinc nanoparticles.
Objectives
The main objective of this research work was to assess the anticholinesterase and antioxidant activity mediated Anti-Alzheimer activity of Cordyceps militaris and zinc nanoparticles prepared by green synthesis process.
Materials and Methods
The zinc nanoparticles were prepared by green synthesis process using extract of fungus Cordyceps militaris. Characterization of prepared nanoparticles were done by the Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM), X-ray diffraction (XRD), EDX and Fourier Transform Infrared (FT-IR) spectroscopy for shape and size, Surface Plasmon Resonance (SPR), functional groups, crystallinity. It was observed that SPR peak were formed 375 nm, which was determined through UV-visible Spectroscopy.
Results
SEM and TEM photomicrograph shown particles were formed spherical in the shape with smooth surface having 37.09 nm average particle sizes. SPR for nanoparticles was found at 300 nm. X-ray diffraction analysis confirm crystalline shaped of prepared nanoparticles. Moreover, during the synthesis of nanoparticles, the colour of suspension changed from dark yellow to colourless with development of cloudiness in solution. The different functional groups involved in nanoparticle stabilization were determined using FTIR Spectroscopy.
Conclusion
Furthermore, the Alzheimer activity of plant extracts and ZnNPs have been carried out using the Ellman technique through cholinesterase with small modification. The IC50 value in anticholinesterase inhibitory activity of zinc nanoparticles was found 83.16237 μg/mL while IC50 value of donepezil was found 51.38714 μg/mL which was taken as standard. It was concluded that the result indicated the promising inhibitory potential of cholinesterase activity. The antioxidant assay results with percentage inhibition 127.0308 μg/mL showed the most effective antioxidant property source than aqueous extract of Cordyceps militaris.
Background
The background of this study revolves around Rauvolfia tetraphylla and its potential anti-inflammatory properties. To explore the anti-inflammatory activity of crude extracts obtained from the leaf and fruit of R. tetraphylla, with the goal of identifying natural compounds that could serve as safer and more effective alternatives to conventional non-steroidal anti-inflammatory drugs.
Objectives
Aim of the study is to identify the most potent anti-inflammatory activity from Rauvolfia tetraphylla and optimizing the synthesis using Response Surface Methodology (RSM). The RSM analysis is to determine the influence of selected independent variables on dependent variables of the anti-inflammatory properties of R. tetraphylla, an endangered medicinal shrub.
Materials and Methods
The anti-inflammatory activity of various crude extracts (hexane, chloroform, ethyl acetate and methanol) derived from the leaf and fruit of R. tetraphylla, was investigated using an in vitro assay based on denaturation of protein and utilize Response Surface Methodology to optimize the anti-inflammatory activity of the extracts using bovine serum albumin as the test protein.
Results
The results showed that the ethyl acetate extract of fruit exhibited greatest inhibitory effect. Furthermore, the 3D response surface plot, perturbation plot, and contour plot were successfully obtained, indicating the interdependence of the four factors on the anti-inflammatory activity. By optimizing the parameters, it may be possible to enhance the anti-inflammatory activity, thereby maximizing the plant’s therapeutic potential.
Conclusion
These findings suggest that R. tetraphylla leaf and fruit could serve as a potential source of anti-inflammatory agents with better safety and efficacy profiles compared to Non-Steroidal Anti-inflammatory Drugs.
Aim
The generation of silver nanoparticles via a green synthesis approach with leaf and stem extracts of Canavalia rosea is our prime objective.
Materials and Methods
The fabricated Nanoparticles (AgNPs) are interpreted by Gas Chromatography-Mass Spectrometry (GC-MS), X-ray Diffraction method (XRD), Field Emission Scanning Electron Microscope (FESEM), Energy Dispersive X-ray Analysis (EDAX), UV spectroscopy and photoluminescence. GC-MS analysis revealed a single hit compound and eight hit compounds from the leaf and stem extracts. Also, the insilico molecular docking of these target compounds was performed with Caspase-9, TNF-alpha, HER-2 and ER-alpha receptor proteins to validate the best binding affinity poses. The ability of the target compounds from the leaf and stem extracts to bind to receptor proteins shows that they can stop cell growth, as shown by the higher binding energy values.
Results
The XRD data affirms the peak formation at a 2θ value of 38.86º, which is attributed to the lattice plane at (111). FESEM images validate the shape and structure of leaf-AgNPs and stem-AgNPs, respectively, upon analysis. UV spectrophotometric analysis reveals the surface plasmon resonance peaks of AgNPs. Photoluminescence peaks were observed at 449 nm by the leaf-AgNPs and 449 nm and 504 nm by the stem-AgNPs were documented. The ABTS assay is performed to evaluate the antioxidant effect of AgNPs. Also, the antiproliferative effect of AgNPs was determined by MTT assay at several concentrations from 1.95 µg/mL to 250 µg/mL in the MCF-7 cancer cell line.
Conclusion
The remarkable results suggest that AgNPs could be explored further as a therapeutic agent in pharmacological applications.
Background
The primary challenge facing Tuberculosis (TB) is the growing prevalence of drug resistance and the hepatotoxicity secondary effects of first and second-line anti-TB treatments have reignited interest in exploring new metal drug complexes as possible sources of anti-TB medications.
Aim
To perform in silico studies for Curcumin-metal complexes, synthesis and evaluate their antitubercular activity and cytotoxicity.
Materials and Methods
Designed metal complexes were docked against 2NSD and performed ADMET studies. Based on binding affinity, a series of Curcumin-metal complexes were synthesized, characterized by IR, NMR, MASS, P-XRD and the antitubercular activity was evaluated by MABA and MTT assay for cytotoxicity investigations.
Results and Discussion
The binding energies ranged from -8.0 to -10.1 ‘kcal/mol’. At -10.1 ‘kcal/ mol’, the Curcumin-Cu complex (C1) exhibited the best binding. The synthesized compounds was evaluated against Mycobacterium tuberculosis (H37Rv) using the MABA assay. Curcumin-Cu complex (C1) showed the highest activity and was the most sensitive at 0.8 µg/mL and showed less toxicity with an IC50 of 10.0 and a selectivity index of 4.0. Cytotoxicity was evaluated by the ATCC CCL-81 cell line.
Conclusion
Therefore, we can conclude that the molecular hit will be a good lead to develop novel therapies for tuberculosis treatment.
Background
Polycystic ovarian syndrome is a metabolic disorder majorly caused by the hormonal fluctuations in female and the current scenario explains that adolescents remain predominantly affected with this disorder. Bauhinia variegata assist in the treatment of various ailments and are used as an ingredient in targeting uterine disorders, yet the exact constituent that contributes on activity remains unknown.
Aim
The main aim of our study is to determine the potent phytoconstituent of Bauhinia variegata to fight against the symptoms of PCOS through computational techniques.
Materials and Methods
Five in silico techniques like Molecular docking analysis, Pharmacokinetics, toxicity prediction of the compounds, Biological activity and Molecular dynamics simulation studies were performed to identify the potent phytoconstituent.
Results and Discussion
Molecular docking studies show that the major constituent lupeol had a good binding interaction and high docking score of -10.31 Kcal/mol and -11.52 Kcal/mol with both the proteins 3RUK and 1E3K. Pharmacokinetics, toxicity and biological activity studies reveal that it had ideal drug likeliness properties with proper biological activity values and were found to non-toxic in the analysed parameters. Lupeol complex was found to be potentially stable throughout the molecular dynamic’s simulation for 100 ns.
Conclusion
Thus, through in silico analysis it is evident that from the list of phytoconstituents of Bauhinia variegata, lupeol possess potent activities in mitigating the symptoms of PCOS. Further in vitro and in vivo analysis on PCOS model is expected to yield favourable results.
Background
Rheumatoid arthritis, a global autoimmune affliction affecting 0.3-1% of the population, is characterized by chronic inflammation and systemic symptoms. Dissatisfaction with conventional treatments leads individuals with chronic pain in rheumatoid arthritis to explore alternative medicine. Herbal remedies, including Equisetum arvense extract, are studied for their anti-inflammatory potential.
Aim
This research focuses on evaluating the impact of E. arvense extract on experimentally induced rheumatoid arthritis in rats, presenting a promising alternative for complementary approaches.
Materials and Methods
In the study, rats received oral doses of Equisetum arvense ethanolic extract at 50 mg/kg and 100 mg/kg, followed by induction with Complete Freund’s Adjuvant in the hind paw on day 0. Physical parameters like body weight and paw volume were assessed on days 0, 8, 16 and 22. Hematological parameters, including RBC count, Hb levels, ESR, total WBC count, and platelet count, were measured. Histopathological studies were conducted for a comprehensive assessment.
Results
They showed both doses of Equisetum arvense extract significantly reduced paw volume compared to the CFA-induced group. Extract administration elevated RBC and Hb levels, approaching normalcy. Increases in WBC count and ESR were notably mitigated. Rats treated with the extract demonstrated protection against bone deterioration and reduced soft tissue swelling. Hispathology of tibiotarsal joints E. arvense treated rats exhibited joint protection, reducing cartilage destruction and decreased vascularity.
Conclusion
The Equisetum arvense showed diminished cartilage destruction and decreased vascularity compared to arthritic rats. The Equisetum arvense exhibits potent anti-rheumatoid activity, emphasizing its potential as an alternative therapeutic approach for rheumatoid arthritis.
ABSTRACT
Background
Over the past two decades, Silver Nanoparticles (AgNPs) have demonstrated a wide range of antioxidant and anticancer properties. Vinca alkaloid exhibits the anticancer efficacy by direct metaphase arrest of cell division.
Aim
The present study is to develop a green synthesis method for producing silver nanoparticles using vinca, the antioxidant and anticancer potential was assessed using A549 cells.
Materials and Methods
The synthesized AgNPs were analyzed using Fourier Transform Infrared (FTIR) analysis, UV-visible spectrophotometer (UV), Scanning Electron Microscope (SEM) and Spectra Max i3X energy-dispersive X-ray (XRD) Spectroscopy to determine their physico-chemical and morphological characteristics.
Results and Discussion
The FTIR spectrum of vinca AgNPs exhibited absorption bands at 692 cm-1, 684 cm-1, 611 cm-1, 592 cm-1, 578 cm-1, 554 cm-1, 548 cm-1, 539 cm-1 and 526 cm-1, indicating the presence of silver ion bounded nanoparticles derived from Vinca leaf. These findings suggest that vinca-coated AgNPs possess multiple functions that contribute to their stability. XRD data analysis revealed Bragg’s reflections in the XRD pattern (2θ) at 24.75, 31.59, 37.56, 53.01, 64.93 and 76.27, confirming the crystalline nature of the green synthesized AgNPs. Elemental analysis was conducted to determine the elemental composition of the sample, which indicated that approximately 60% of the prepared nanoparticles were bound with silver ions, supporting the formulation. Antioxidant studies were performed using the DPPH assay at different concentrations of AgNPs, while cell-based cytotoxic assays were conducted using different concentrations of AgNO3.
Conclusion
The results demonstrated that the nanoparticles inhibited the proliferation of A549 cells and reduced cellular motility, indicating their promising anticancer efficacy.
Background
The Olea europaea L. leaves have long been used in treating various illnesses. Its pharmacological activity based on the phytoactive constituents; therefore, optimizing the extraction process should intensify the benefits.
Aim
The study aimed to optimize the extraction process for O. europaea L. leaves, evaluate their antioxidant and anti-inflammatory activities, and explore their influence on the biochemical parameters of diabetic animals.
Materials and Methods
The differential pharmacology of the extracts and combinatorial therapy with the antidiabetic agent; empagliflozin, were explored. The aims were accomplished after several in vitro and animal studies: quantification of flavonoid and phenol content, measurement of the antioxidant activity, identification of the active constituents, and assessment of hepatic and renal functions, lipid profile, and glycemic status. In addition, molecular biology tools were used to measure the expression of the inflammatory mediators IL-6 and IL1beta.
Results
Findings reveal that the hydroalcoholic binary system reinforced by the sonication yields the highest polyphenol (44.40±1.414 mg/g dry extract equivalent to gallic acid) and total flavonoids (31.0700±1.202 mg/g dry extract equivalent to quercetin). Extract by the same system showed high substantial antioxidant activity. HPLC-MS/MS reveals oleuropein and its aglycon, o- and p-coumaric acid, hydroxytyrosol acetate, and betaine compounds. A significant reduction in the average weight was recorded in diabetic mice (29.79±2.88 g) compared to the control (32.61 ±2.57 g). A significant reduction in producing the inflammatory mediators IL-6 and IL1 beta was measured.
Conclusion
Olive leaves are a potential addition to conventional medicines to enhance the health profile of diabetic mice.
Background
One of the organisational strategies to ensure the use of relevant good practises for each stage in the life cycle of pharmaceutical products is the market surveillance program, which aims to demonstrate product specification adherence. It uses analytical pharmacopoeial and literature-based approaches primarily to carry out quality control on the chosen pharmaceutical items.
Aim
Development of a program for analytical control of different medicinal products containing 25 mg hydrochlorothiazide.
Materials and Methods
European Pharmacopoeia and USP HPLC methods for assay and related substances were applied in prescription medicines.
Results
The system suitability tests were evaluated for each method, and the results of each generated group of products were compared. The quantitative content values deviation and the quantitative limitations for each impurity were determined. The deviations are in the range 0.76%-4.01%. Calculated RSD values are below 2%. The results obtained by both methods are within the acceptable limits of 95%-105%. In the European Pharmacopoeia method, the limits of three impurities were determined and seven more were found and marked as unknown. The USP method allows identification of only one impurity.
Conclusion
For the market surveillance program for pharmaceuticals containing hydrochlorothiazide, an analytical control program has been developed. The program combines multiple pharmacopoeial HPLC methods and compares the outcomes with an initial assessment of each method’s applicability for all pharmaceuticals containing hydrochlorothiazide.
Aim
A precise, linear and specific liquid chromatography-tandem mass spectrometry procedure was executed and subjected for validation for the quantification of plasma.
Materials and Methods
The chromatography elution was carried out using a C18-Discovery column of 15 cm in length and 2.1 mm in internal diameter, packed with stationary phase particles of 5 µm size, at a flow rate of 0.80 mL/min. An isocratic elution process was conducted with a mobile phase solution consisting of methanol and 0.10% V/V HCOOH in a ratio of 90:10. The separation of Abametapir and Metformin was achieved by a liquid-liquid extraction process using ethyl acetate as the solvent.
Results
A triple quadrupole mass spectrometer was used for the measurement of ions. Electrospray ionization is a technology that ionizes positively, and it was used in Multiple Reaction Monitoring (MRM) with parent/product ionic transitions m/z 185.1 →106.06 for Abametapir and 130.1 →60.20 for the Metformin internal standard. A calibration graph was constructed with values ranging from 2.05 to 82.00 ng/mL, resulting in the equation y=0.0149x+0.00221, with a r2 value above 0.99. The recovery values of Abametapir exceeded 94.27%, with its accuracy assessed in terms of relative error ranging from -4.04% to 6.52%.
Conclusion
The accuracy, recovery and sensitivity values of Abametapir in the plasma sample, as shown by the established approach, highlight its significance in pharmacokinetic and bioequivalence research.
Objectives
The investigation article intends is to build and validate a more convenient scientific approach to accurately simultaneously determine famotidine and para-amino benzoic acid from their cocrystals
Significance
The zero-order spectra of both drugs demonstrated significant overlap between the two spectra curves; therefore, the simultaneous estimation of two drugs by zero-order spectra method was not feasible. Therefore, to overcome this and facilitate simultaneous analysis of both the therapeutic agent derivative spectrophotometry technique was employed; The sensitivity and selectivity of both the drug mixtures were enhanced by the derivative spectrophotometry technique.
Materials and Methods
First-order derivative spectra were chosen for the quantitative analysis of FMT and PABA in cocrystals. Zero-crossing measurements (both calculated and plotted) were employed to select the wavelength for each drug to carry out quality control analysis. ICH guidelines were referred to validate the technique.
Results
The wavelength 275 nm for FMT was selected referring to zero-crossing points (∆A/∆γ of PABA is zero at 275 nm) and 285 nm was selected for PABA (∆A/∆γ of FMT is zero at 285 nm) and no mutual intrusion was detected and these wavelengths were designated for estimation of these therapeutic agents. The linearity, accuracy, precision, and robustness of the method were validated by satisfying the statistical parameters.
Conclusion
The technique established for the simultaneous assessment of drugs (FMT and PABA) from cocrystals by first-order derivative spectrophotometric technique was validated. The development of the analytical method was reliable, economical, convenient, and environmentally friendly.
Background
Tegafur (TEG) is a prodrug of 5-Fluorouracil (FU) that is mainly employed in the treatment of colorectal tumors combined with Gimeracil (GIM) and Oteracil (OTE) enhances its stability by enhancing the antineoplastic activity and reducing gastric irritation.
Aim
The key focus of this research was to design a rapid Ultra Performance Liquid Chromatography (UPLC) and validate that it is uncomplicated, exact, responsive and reliable for quantifying the concentrations of tegafur, oteracil and gimeracil in both their pure state and pharmaceutical formulations.
Materials and Methods
The UPLC method was developed using HSS C8 (100 mmx2.1 mm, 1.8 µm) column and the mobile phase was composed of phosphoric acid at a concentration of 0.1% v/v, with a pH of 2.0 and methanol in an 80:20 ratios. The process was carried out at a flow rate of 0.2 mL min-1, with injection volume of 5 µL and absorbance maxima of 282 nm. The technique was validated following the ICH standards. UPLC is a superior technique regarding performance thus it was chosen.
Results and Discussion
The elution time obtained was found to be below 2 min for all three drugs. The validated method’s linearity was determined to be between 40 and 240 µg/mL for tegafur, 31.6-189.6 µg/mL for oteracil and 11.6-69.6 µg/ mL for gimeracil. Tegafur, oteracil and gimeracil were found to have Detection Limit (LOD) and Quantitation Limit (LOQ) values of 0.3 μg/mL and 1 μg/mL, 0.2 μg/mL and 0.8 μg/mL, 0.1 μg/mL and 0.3 μg/mL, respectively. The developed method demonstrated high accuracy, as indicated by the RSD being less than 2%.
Conclusion
Thus, it can be employed as a method for evaluating stability and conducting regular quality control inspections for tegafur, gimeracil and oteracil.
Aim
A validated RP-HPLC method was established for the quantification of Amlodipine and Metoprolol succinate according to ICH guidelines.
Materials and Methods
This method utilized a Phenomenex (US) C18 column with dimensions of 250X4.6 mm I.D and a particle size of 5 µm. Employing an isocratic elution technique, the mobile phase comprised pH 3.0 phosphate buffer solution and acetonitrile. Detection occurred at a wavelength of 215 nm and a flow rate of 1 mL/min was chosen to ensure optimal resolution for Amlodipine and Metoprolol succinate.
Results and Discussion
Retention times were noted at 3.137 min and 5.672 min for Amlodipine and Metoprolol succinate, respectively. High correlation coefficients were achieved (0.9995 for Amlodipine and 0.9996 for Metoprolol succinate). The method exhibited precision, with low relative standard deviations of 0.357% for Amlodipine and 0.077% for Metoprolol succinate. In summary, the RP-HPLC method developed was specific, linear, precise and robust.
Conclusion
The devised method was validated in terms of accuracy, precision, linearity, specificity, robustness and ruggedness. All formulations’ sample recoveries were in good accordance with the claims made on their labels
Background
Epilepsy is a neurological disorder characterized by anomalous brain activity, convulsionsandoddbehaviour.Tenpyrrolecarbohydratebasedanalogues(Va-Vj)weresynthesized with amide as intermediate in the current research with the goal of reducing convulsions and seizures.
Materials and Methods
The newly developed compounds were synthesized. Numerous methods (IR, NMR, mass, elemental analysis, etc.,) were used to characterize these substances. Several models were used to test each of these molecules for anticonvulsant activity. By using the rotarod and ethanol potentiation techniques, neurotoxicity was also evaluated. The study meticulously examined each parameter and showed ADME predictions for each of the 10 congeners that were produced. In addition, studies on molecular docking employed the GABA-A target protein.
Results
Anticonvulsant screening results identified compounds Ve, Vd, Vc and Va as the most efficacious of the series. All synthesized equivalents largely passed the neurotoxicity test. The results of molecular docking revealed significant interactions at the active site of GABA-A with Ile C:242, Asp C:424, Phe D:307, Arg C:250 Trp C:241 and Phe C:240 and the outcomes were good and in agreement with in vivo findings.
Conclusion
The study’s findings showed that some substances had promising anticonvulsant properties that were comparable to those of the standard drug. The highly active novel anticonvulsant analogues may therefore represent a possible lead and additional studies may result in a potential new drug candidate.
Background
In present study 1,3,4-oxadiazole derivatives with iso-sterically fused amino acids was attempted to synthesize. As variety of chemical reactions that 1, 3 and 4-oxadiazole molecules can experience, it made them very useful for searching of molecule altogether its high advantaged structure having enormous biological potential. Heterocyclic ring fusion has yielded compounds with a diverse array of biological functions. In the biological system, amino acids are important. With the hope that adding amino acids to an oxadiazole scaffold may result in new molecules that are potentially referred to as unnatural amino acids, this experiment helps to synthesize substances. It is possible to create novel hormones, enzymes and medications using unconventional amino acids.
Materials and Methods
Derivatives were tried to synthesize from two methods, conventional as well as new microwave method in order to find out highest yielding method. Microwave method also referred to as “green chemistry” because it uses no external energy sources to produce any harmful fumes, gases, or heat. The synthesised compounds were analysed for their therapeutic potential, molecular properties and quantum studies.
Results
“Method B” i.e., microwave used method found to be produce high yield. Synthesised derivatives of fused amino acids with 1,3,4-oxadiazole were said to be unnatural amino acids. The compound(s) were analysed using UV, IR, Mass and NMR spectral data. Synthesized compound(s) were experienced for in vitro DPPH activity with quantum studies, antibacterial potential and anti-fungal activity and found that compound 1A and 1B to have promising activity.
Conclusion
The synthesis of fused amino acids is a field of recent study that is gaining interest. Study provides preparation of fused oxadiazole as an Unnatural amino acid and for its similar compound(s). The findings might make a significant contribution to the future development of innovative medicinal medications.
Background
Lamivudine is an Anti-Viral Drug belongs to BCS Class II Drug which exhibits limited solubility and high permeability through oral route.
Aim
The study was designed to predict the solubility potential of Lamivudine loaded Metal Organic Framework complexed with MIL 100 by using microwave assisted chemistry through topical route.
Materials and Methods
In combination of MIL 100 (Fe) we utilize Ferric chloride hexahydrate as metal particle and benzene 1,3,5-carboxyl corrosive as natural linker. The anti-viral drug Lamivudine was used to load in the MIL 100 (Fe). The specific proportion of FeCl3.6H2O and benzene 1,3,5-carboxylic acid was weakened with deionized water. Above combination is put in microwave at 130ºC for 6 min which prompts development of complex called MIL 100 (Fe). Various proportions of Lamivudine medication and MIL 100 (Fe) were taken to prepare the formulations and the effect of drug loading with various ratios were interpreted. Evaluation of MOF was done for drug-excipient compatibly studies and surface morphology for structural analysis.
Results and Discussion
Spectral studies conforms the purity of the sample and from drug-excipient compatibility studies no interactions were noticed. Microwave Assisted Technology can be proven as a best fit model for synthesis of advanced 2D Materials called MOF and drug loading was found to be high at a ratio of Lamivudine: MIL (1:0.5). The particulate studies conform the nanonisation of drug which results in enhanced solubility due to increased surface area of drugs.
Conclusion
Lamivudine loaded Metal Organic Frameworks (MOF) with MIL 100 (Fe) was successfully fabricated with high loading and decreased particle size authenticates the utilization of microwave assisted technology as a promising tool for MOF and with the result of increase in solubility, Lamivudine can be used in a best way as an anti-viral drug in the form of MOF through topical route.
Background
Cancer treatment has witnessed remarkable advancements with the development of targeted therapies, such as anti-HER2 agents and microtubule-damaging drugs. Despite their efficacy, these drugs can be associated with a spectrum of Adverse Drug Reactions (ADRs) that may impact patient safety and treatment outcomes. Data on the safety profile of cancer treatment are scarce.
Aim
This prospective observational study aimed to systematically assess and characterize adverse drug reactions related to anti-HER2 and microtubule-damaging drugs in the clinical setting of a tertiary care hospital.
Materials and Methods
We conducted a comprehensive observational study over a specified period involving patients undergoing cancer treatment with anti-HER2 and microtubule-damaging drugs. A structured data collection process was employed to record patient demographics, treatment regimens, and observed adverse drug reactions. The severity of adverse drug reactions was categorized according to well-established criteria. The data was analyzed using frequency distribution association analysis to identify potential risk variables for adverse drug reactions.
Results and Discussion
Preliminary results from our study displayed an extensive array of adverse drug events associated with anti-HER2 and microtubule-damaging drugs, including cardiotoxicity, neuropathy, and myelosuppression. The degree of incidence and impact of adverse drug reactions varied depending on both patient medications and their variables. Furthermore, certain risk factors, such as age, comorbidities, and concomitant medications, were identified as potential predictors of adverse drug reactions.
Conclusion
This prospective observational study provides valuable insights into the incidence, patterns, and risk factors of ADRs related to anti-HER2 and microtubule-damaging drugs in cancer treatment. The findings will aid healthcare professionals in optimizing treatment strategies, monitoring patients effectively, and managing adverse drug reactions, ultimately providing high-quality care to patients in a tertiary hospital. Advanced research and continuous surveillance are essential to enhance our understanding of these adverse drug reactions and develop strategies for their prevention and management.