Current Indian Science - Current Issue

The worldwide increase of antimicrobial resistance in ESKAPE pathogens, which includes Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter sp., constitutes a substantial public health hazard, constraining treatment alternatives and elevating morbidity and mortality rates. As traditional antibiotics diminish in efficacy, phytochemicals are capturing interest due to their varied antibacterial characteristics and decreased susceptibility to developing antibiotic resistance. Phytochemicals, such as alkaloids, terpenes, phenolics, flavonoids, and organosulfur compounds, have multi-target processes that might provide innovative strategies for addressing infections caused by ESKAPE pathogens.

The investigation sought to evaluate the effectiveness and mechanisms via which different phytochemicals could hinder and destroy the resistance pathways of ESKAPE bacteria, emphasizing their potential to serve as therapeutic agents in combating antimicrobial resistance.

Investigation demonstrates that some phytochemicals may disrupt many bacterial functions, such as cell wall production, membrane integrity, quorum sensing, and biofilm development in ESKAPE pathogens. For example, carvacrol from essential oils has shown efficacy against S. aureus by reducing staphyloxanthin synthesis and altering regulatory proteins, including SarA. Furthermore, conessine has altered resistance in A. baumannii by inhibiting the AdeIJK efflux pump. Flavonoids like resveratrol and curcumin have shown synergistic benefits with conventional antibiotics by improving their effectiveness while minimizing toxicity. These chemicals address several resistance pathways, impairing the ability of infections to build resistance.

Phytochemicals provide an opportunity to facilitate the development of novel therapies targeting antimicrobial resistance in ESKAPE bacteria. Extensive efficacy and distinctive multi-target mechanisms of phytochemicals provide them promising candidates for combination therapy, possibly reinstating antibiotic effectiveness and decelerating the development of resistance. Additional investigation into the increase of bioavailability and clinical usage is essential to fully exploring the medicinal potential of phytochemicals.

To overcome the drugs’ low bioavailability and/ or solubility, the development of novel oral delivery approaches using lipid-based formulations has been of growing interest. Curcumin being a Class IV drug, has poor solubility and poor permeability. One of the biggest obstacles to its use in therapeutic treatment is this.

In order to increase drug bioavailability, this research aimed to create Solid Dispersion Lipid Particles (SDSLs), in which Solid Dispersion (SD) was enclosed in solid lipid particles as the drug's core packaging.

For this, Curcumin (CUR) was selected as a model drug, PEG 6000 was used as a polymer, Stearic acid was used as the lipid phase, and Poloxomer 188 was used as a surfactant. Different batches of SD were formulated by solvent evaporation method. SDSLs were prepared by the melt-emulsification ultrasonication method and characterized for their % yield, % drug loading, % drug encapsulation efficiency, zeta potential, FTIR spectroscopy, XRD studies, in vitro drug release, and ex vivo permeation.

The optimized formulation showed the highest % EE and sustained in vitro drug release. The release mechanism was Super Case II, and the Higuchi equation was the best fit for the data.

SDSLs have sustained release effects and demonstrated enhanced ex vivo permeability which could lead to improved bioavailability. These studies demonstrate that SDSL could be a promising oral formulation for enhanced bioavailability.

Among fertile women, Polycystic Ovarian Syndrome (PCOS) is a prevalent metabolic and endocrine condition. This disorder is characterised by hyperandrogenism (high levels of male hormones), recurrent anovulation (ovulation failure), and polycystic ovaries. Infertility, hirsutism, and irregular menstruation are typical symptoms. The primary objective of this review is to provide a current and comprehensive approach to treating PCOS.

The databases PubMed, Frontiers, ScienceDirect, Springer, Wiley, and MDPI were utilised for the literature search. We used keywords, such as PCOS, hirsutism, medicinal plants, obesity, anovulation, and related variations to identify relevant articles and materials.

The findings indicated that several herbal remedies, such as Saraca asoca, Moringa oleifera, Asparagus racemosus, Glycyrrhiza glabra, Panax ginseng, and Cimicifuga racemosa, as well as various natural compounds, including glycosides, anthraquinones, chlorogenic acid, apigenin, epigenin, and flavonoids, show preliminary evidence supporting their potential in the management of PCOS.

Herbal treatments are appealing because they are natural and may have fewer side effects. Several herbs have shown promise in managing PCOS symptoms. While traditional treatments for PCOS remain important, the growing interest in complementary and alternative therapies highlights the need for further research into the efficacy and safety of medicinal plants. Alternative approaches may include lifestyle modifications, nutritional supplements, and the use of herbal remedies.

This review primarily focuses on evaluating the efficacy of herbal medicines in the management of PCOS. The drawbacks of traditional therapy are driving an increase in interest in alternative treatments for PCOS management. New scientific findings and their application in conventional therapy suggest that they may play a crucial role in the overall treatment of this complex illness.

Urinary Tract Infections (UTIs) represent one of the most common microbial diseases affecting individuals across age groups. This study aimed to investigate the microbiological profile and antibiotic utilization patterns among UTI patients at a tertiary care hospital.

A prospective observational study was conducted at the Maharishi Markandeshwar Institute of Medical Science and Research (MMIMSR), Mullana, Ambala. The study duration was from January 1, 2021, to April 30, 2021. A total of 323 patients aged 12 years and above with culture-confirmed UTIs receiving antimicrobial treatment were included. Data collected included demographics, urine culture results, and antimicrobial susceptibility patterns.

Out of 323 urine samples analyzed, 165 (51.08%) showed significant microbial growth. The majority of positive cases were from females (54.7%) and patients aged 50–70 years. Escherichia coli (44%) was the most prevalent organism, followed by Enterococcus spp. (11.14%), Klebsiella pneumoniae (8.9%), Pseudomonas aeruginosa (8.04%), and Staphylococcus aureus (6.19%). Gram-negative isolates exhibited high resistance to ampicillin (70%) and nalidixic acid (10.5%), but were more sensitive to nitrofurantoin (10.8%), imipenem (8.6%), and meropenem (7.4%). Gram-positive organisms showed sensitivity to tigecycline (6.5%), linezolid (7.1%), and sulfamethoxazole (7.7%).

The study demonstrates a significant prevalence of multidrug-resistant pathogens in UTIs. Escherichia coli remains the most frequent uropathogen. The findings underscore the importance of regular microbiological surveillance and sensitivity profiling to inform empirical treatment decisions. The inclusion of patients aged 12 and above ensures broader representation across age demographics.

UTIs in tertiary care settings are predominantly caused by Escherichia coli, with varying levels of antibiotic resistance. Local sensitivity patterns should guide empirical treatment. The implementation of antimicrobial stewardship programs is essential to combat the rising trend of antimicrobial resistance.

Diabetes mellitus is a chronic metabolic disorder characterized by persistent hyperglycemia and associated complications, including cardiovascular disease, neuropathy, and renal impairment. While conventional therapies such as insulin and oral hypoglycemics manage glycemia, they often fail to address the underlying metabolic disturbances or prevent long-term complications. This has prompted interest in complementary approaches, including traditional herbal formulations.

A comprehensive literature review was conducted across PubMed, Scopus, Google Scholar, and the AYUSH Research Portal for the period 1951–2024. Search terms included ‘Nishamalaki Churna,’ ‘Amla,’ ‘Haridra,’ ‘diabetes,’ ‘oxidative stress,’ and ‘insulin resistance.’ Classical Ayurvedic texts were reviewed alongside experimental and clinical studies. The inclusion criteria encompassed peer-reviewed research on Nishamalaki Churna (NAC) or its components (Emblica officinalis and Curcuma longa) in the context of diabetes.

Amla improves insulin sensitivity and reduces oxidative stress due to its high antioxidant and vitamin C content. Haridra, rich in curcumin, exhibits anti-inflammatory and insulin-sensitizing effects. In combination, NAC demonstrates synergistic action, improving glucose metabolism and metabolic regulation. Preclinical studies report decreased blood glucose and HbA1c, enhanced antioxidant enzyme activity, and inhibition of carbohydrate-digesting enzymes. Clinical trials have revealed improvements in fasting/postprandial glucose levels, lipid profiles, and symptomatic relief, with minimal side effects.

NAC offers a multifaceted therapeutic effect through antioxidant, anti-inflammatory, and metabolic regulatory mechanisms. Its polyherbal composition provides a synergistic approach distinct from single-agent pharmaceuticals. However, challenges in formulation standardization and the need for large-scale clinical validation persist.

NAC holds promise as a safe, complementary intervention in type 2 diabetes management, warranting further clinical investigation.

This study aims to identify and evaluate novel KRAS G12C inhibitors using in-silico methods, focusing on molecular docking and ADMET profiling to optimize binding affinity, pharmacokinetics, and safety profiles.

The KRAS G12C mutation is a key driver of oncogenesis in aggressive cancers, including non-small cell lung cancer. Although inhibitors such as sotorasib have been developed, challenges like hepatotoxicity and resistance limit their clinical use.

This study seeks to design and assess potential KRAS G12C inhibitors with superior binding interactions and pharmacokinetic properties compared to existing drugs.

Molecular docking simulations were conducted to evaluate the binding affinities of inhibitors, followed by ADMET profiling to assess pharmacokinetics, drug-likeness, and toxicity.

Novel compounds, such as CID_137278727, demonstrated higher binding affinities (-10.8 kcal/mol) and favourable ADMET profiles compared to sotorasib (-8.1 kcal/mol). Key interactions with residues GLU62, TYR96, and CYS12 were identified, though hepatotoxicity remains a concern.

In-silico approaches have identified promising KRAS G12C inhibitors with enhanced efficacy and pharmacokinetics, highlighting the potential of computational methods in advancing targeted therapies for KRAS-driven cancers.

The presence of synthetic dyes like Congo Red in wastewater poses serious and persistent environmental health hazards as a result of their toxicity and stability. Therefore, developing an efficient and reusable adsorbents for the elimination of dye is quite important in order to address water pollution challenges.

The study aims to classify the efficacy of sodium borohydride-reduced Bent/Fe NPs and crude bentonite in removing Congo Red dye from aqueous solutions.

Sodium Borohydride was utilized in order to synthesize Bent/Fe NPs, dragging its reducing capacities in order to enhance its adsorption properties. Batch adsorption experiments were performed in order to estimate the removal efficacy under multiple conditions consisting of initial dye concentration, pH and contact time. Adsorption isotherms and kinetics were analyzed using Freundlich and pseudo-second-order models.

Bent/Fe NPs exhibited significant removal efficiency, reaching up to 91.97% removal of Congo Red dye with an initial concentration of 40 mg/L in alkaline conditions. Adsorption data was found to align well with the Freundlich isotherm model, signifying heterogeneous adsorption sites. It also fitted well with pseudo-second-order kinetic model indicating that chemisorption is the dominant mechanism taking place. Also, the adsorbent displayed excellent reusability, preserving substantial efficiency up to three cycles.

Sodium borohydride reduced Bent/Fe NPs offer an assuring, efficient and reusable solution for Congo Red dye removal from aqueous solution. The high adsorption capacity and, its affinity with alkaline conditions and its excellent reusability make them a feasible choice for wastewater treatment applications.

Asparaginase, an enzyme that changes L-asparagine into L-aspartic acid, has attracted a lot of interest recently due to its potential to prevent the development of cancer.

In the present study, the endophytic fungi isolated from wild mushrooms were tested for their ability to produce extracellular L-asparaginase.

The isolated organism was identified as Rhizomucor variabilis strain CBS 103.93 by morphological and molecular identification. The enzyme and substrate incubation time of 10 minutes showed the highest production of L-asparaginase at 3.850 U/mL. Rhizomucor variabilis strain CBS 103.93 exhibited the highest enzyme activity on the fourth day of the incubation period at pH 7.0. The most beneficial carbon source was found to be mannitol, and substrate concentration at 1.5% resulted in maximum enzyme production. Inorganic nitrogen (NH4)H2PO4 and organic nitrogen source peptone exhibited maximum enzyme activity. Rhizomucor variabilis strain CBS 103.93 species produced the enzyme under optimal conditions, and a 5-fold increase (from 3.850 U/mL to 19.25 U/mL) was achieved after optimization in submerged fermentation.

The optimization processes are beneficial for the industrial production of L-asparaginase for use in the pharmaceutical and food industries. Hence, it is possible to say that it may find its future application in the pharmaceuticals industry and food industry.

Vildagliptin is a dipeptidyl peptidase 4-related inhibitor that is often utilised in the treatment of type-2 diabetes. It is possible that sustained therapeutic levels of vildagliptin for a prolonged length of time might be achieved by controlled release of the drug in the gastrointestinal system, which would result in an improvement in the efficacy of treatment. Due to their high biocompatibility and biodegradability, biopolymers, such as alginate (sodium), pectin, and xanthan gum, are frequently utilized in drug delivery systems. This is because these biopolymers are good alternatives for the development of controlled-release formulations.

This study aimed to formulate and in vitro evaluate the vildagliptin microsphere using pectin and xanthan gum.

The delivery of vildagliptin was accomplished by the development of beads that were constituted of sodium alginate-pectin and sodium alginate-xanthan gum. Adjusting the proportions of sodium alginate, pectin, and xanthan gum resulted in the production of pH-sensitive beads throughout the synthesis. This was accomplished through the use of a calcium chloride (CaCl2)-induced ionic gelation approach.

The FTIR revealed the compatibility of medicines and polymers. The synthesized beads were tested for scanning electron microscopy, differential scanning calorimetry, drug content, swelling ratio, and in vitro dissolution analysis. The microscopic pictures showed beads of spherical shape and mostly semi-spherical with a broken and rough surface. Swelling was found to be pH-dependent, indicating that water absorption might be minimal in an acid medium and high in an alkaline pH condition. The in-vitro dissolving study depicted controlled drug release.

This study recorded the successful formulation of vildagliptin microspheres using sodium alginate, pectin, and xanthan beads for the controlled release of vildagliptin.

Natural essential oil comprises a galaxy of low-molecular-weight (usually less than 500 daltons) and volatile phytoconstituents that exhibit a handful of biological and pharmaceutical properties; they exhibit several applications chiefly in agriculture, cosmetic, perfumeries, and food industries.

The extraction of essential oil from fresh flowers of C. sophera was performed by hydrodistillation, and the determination of its chemical composition was carried out by Gas Chromatography/Mass Spectrometry (GC-MS). The antibacterial activity of the essential oil was executed by the disc diffusion method against the four pathogenic bacteria. 1,1-Diphenyl-2-picrylhydrazyl (DPPH) was also performed for free radical scavenging assay, and a scanning electron microscopic study was also executed to get an idea of the effect of C. sophera essential oil on bacterial morphology.

The GC/MS analysis indicated that the essential oil is constituted primarily of aromatic compounds (68.75%), and the principal compounds are the dialkyl phthalates esters (58.32%). The zones of inhibition range from 8-16 mm in the case of Gram-negative E. coli, whereas, in Gram-positive S. aureus, these range from 7-13.5 mm. The Minimum Inhibitory Concentration (MIC) was found to be 0.3 mg/mL against all the Gram-negative bacteria tested and 0.4 mg/mL against the Gram-positive bacteria S. aureus. The oil also showed moderate antioxidant properties by scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical with an IC50 value of 126 μg/mL.

As per the present study, the essential oil of C. sophera flowers may be suggested as a new potential source of natural antimicrobial and antioxidant agents.

Poor solubility is a common challenge in pharmaceuticals, hindering oral bioavailability. High throughput screening has led to an increase in poorly soluble drug candidates. Enhancing solubility and dissolution rates is crucial for drug development. Various methods, including solid dispersion, aim to improve solubility. A solid dispersion formulation process involves dispersing one or more active chemicals in a solid state within an inert carrier or matrix. It can be made using solvent, melting, or melting-solvent procedures, among other techniques. By increasing the surface area and dispersibility of poorly soluble pharmaceuticals, this method improves their solubility and rate of dissolution, ultimately leading to an improvement in bioavailability.

Nifedipine solid dispersion emerged in the late 1970s to address its poor solubility and erratic bioavailability for cardiovascular treatment. Researchers explored methods like fusion, solvent evaporation, and melt extrusion to enhance its solubility and dissolution rate. Over the years, these efforts resulted in commercial products, highlighting the importance of solid dispersion in improving drug delivery and patient outcomes for nifedipine therapy.

The aim of this work is to use the surface solid dispersion approach to increase the solubility of nifedipine.

The objective of the study is to develop surface solid dispersion formulations of nifedipine, evaluate their physicochemical properties, assess solubility enhancement, analyze dissolution behavior and stability, and determine the potential of this technique to enhance the pharmaceutical performance of nifedipine.

Nifedipine was dissolved in the solvent-ethanol, and a carrier was then added at various drug-to-carrier ratios. The mixture was allowed to sit for an hour before the solvent was evaporated on a water bath at 40-42ºC with occasional stirring. The resulting dried mass was pulverized, sieved, and then dried further at 40ºC for 3 hours. For further study the powder was stored in desiccators.

Formulation S3 shows better increase in the solubility by solid dispersion technique, increases solubility from 0.002576 ± 0.00013 to 0.04379 ± 0.00013. Dissolution profile data found to be improved from 98.45 ± 0.41 to 99.57 ± 0.088%.

This study explores the challenge of poor solubility in pharmaceutical formulation, focusing on Nifedipine. Surface solid dispersions (SSDs) are investigated as a solution, with various polymers showing promise in enhancing solubility. SSDs, particularly with sodium starch glycolate (SSG) as a carrier, significantly improve solubility, as confirmed by saturation solubility studies. Evaluation indicates SSD efficacy, with S3 emerging as a promising formulation. This study underscores the potential of SSD technology in addressing solubility challenges and improving drug bioavailability.