Current Indian Science - Current Issue
Volume 3, Issue 1, 2025
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Formulation and In-Vitro Evaluation of Vildagliptin Microspheres Using Pectin and Xanthan Gum as Polymers
More LessAuthors: Krishnaveni Manubolu and Raveesha PeerigaIntroductionVildagliptin 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.
AimThis study aimed to formulate and in vitro evaluate the vildagliptin microsphere using pectin and xanthan gum.
Materials and MethodsThe 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.
ResultsThe 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.
ConclusionThis study recorded the successful formulation of vildagliptin microspheres using sodium alginate, pectin, and xanthan beads for the controlled release of vildagliptin.
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Potential of Phytomolecules in Countering Biofilm Formation and Quorum Sensing
More LessThe excessive exploitation of antibiotics for the treatment of bacterial illnesses has resulted in the emergence of several strains that are resistant to different drugs. Due to the widespread occurrence of antibiotic resistance and the emergence of bacterial strains that are resistant to various drugs, significant efforts are being made to identify appropriate alternative medicines to combat harmful microorganisms. Given the observed link between biofilm formation and antibiotic resistance, recent efforts have been directed towards a promising strategy that aims to control and prevent biofilm formation. This strategy involves targeting and inhibiting the quorum sensing system, which has been extensively shown to play a central role in biofilm formation. The conventional approach to controlling infectious disorders involves the use of substances that are designed to either kill or inhibit the growth of bacteria. Bacterial resistance to antibiotics poses a significant challenge to public health. This therapeutic target has been extensively explored globally. However, the scientific data on it are not up-to-date, and only recent studies have begun to explore its potential as a target for combating infectious diseases. An important issue with this strategy is the commonly observed emergence of resistance to antimicrobial agents. This paper aimed to present a comprehensive overview of the quorum sensing system in bacteria, focusing on its role in biofilm formation and the development of antibiotic resistance. Additionally, it provides an update on the significance of targeting this system with natural substances for therapeutic purposes.
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Advancements in Antimicrobial Biomaterials: New Avenues to Ameliorate Wound Infections and Implant-associated Infections
More LessAuthors: Sudip Mukherjee, Dipanjana Patra, Subhankar Maity and Jayanta HaldarThe field of public healthcare has witnessed a transformative shift with the introduction of synthetic biomaterials and biomedical implants, aiming to enhance the interaction between living systems and therapeutic interventions. Despite these advancements, a significant challenge has emerged in the form of microbial colonization and biofilm formation on these materials, leading to an alarming rise in multidrug-resistant infections and subsequent implant rejections. In this review, we present recent breakthroughs in the development of anti-infective biomaterials designed to address wound infections and prevent infections associated with implants. We present various approaches for incorporating antimicrobial properties into diverse wound healing biomaterials such as hydrogels and hemostatic sponges, through covalent and non-covalent modifications or both. Additionally, to counter microbial colonization, we explore different surface modification strategies applied to titanium and catheter implants via covalent grafting as well as physical encapsulation of antibiotics, small molecular biocides, inorganic biocides and antimicrobial peptides. These coatings not only exhibit bacteria-killing capabilities upon contact but also effectively reduce biofilm formation, thereby prolonging the lifespan of implants and devices. Providing an overview of anti-infective biomaterials in clinical pipelines, we discuss the significant challenges hindering the clinical translation of these biomaterials. Finally, we share our perspective on overcoming these obstacles for the successful integration of anti-infective biomaterials into mainstream healthcare practices.
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Chemical Composition and Biological Activities of Natural Essential Oil Extracted from Flowers of Cassia sophera Linn.
More LessBackgroundNatural 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.
MethodsThe 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.
ResultsThe 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.
ConclusionAs 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.
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Phytochemicals for the Improvement of Cognitive Function through Cholinergic Anti-inflammatory Pathway
More LessAuthors: Dhananjay Kumar Singh, Bindu Kumari, Sonal Sinha and Kaneez FatimaCognition is the interdisciplinary scientific study of the brain and its processes, which include the intelligence and behaviour of living beings. Humans are generally equipped with a capacity for cognitive function at birth, but some conditions, such as infection and oxidative stress, lead to impaired cognition. Herbal drugs/phytochemicals are utilized in order to get better cognitive functions and alleviate symptoms associated with impaired cognition function. Yet, there still remains no complete cure for cognitive dysfunction, with most current treatments offering symptomatic relief. This has prompted us to review the importance of phytochemicals and the mechanism by which they may augment cognitive functions. For the present review, a comprehensive literature search was conducted by referring to the research and review articles published by authentic journals and available on web databases. Indeed, numerous plant-based drugs have traditionally been used to combat learning and memory-associated deficits, but many available drugs are potentially toxic alkaloidal cholinesterase inhibitors. Findings by various researchers exhibited that many plant-based drugs act through a different mechanisms, such as inhibition of acetylcholinesterase (AChE), activation of antioxidant defence, and augmenting the blood flow to the brain. The aim of the present review is to highlight the importance of phytochemicals in the modulation of cholinergic anti-inflammatory pathways (CAP) in neurodegenerative disease. For this, available literature was critically analysed. Through a comprehensive review of the recent research findings, this article concludes that medicinal plants serve as reservoirs of various successful drugs for cognition improvement, which belong to different classes of secondary metabolites. We also observe that phytochemicals can modulate cholinergic anti-inflammatory pathways (CAP) in neurodegenerative disease, although the mechanism of action of most natural/herbal extracts and their compounds is not yet fully explored.
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Mitapivat: A Novel Drug Discovery for the Treatment of Hereditary Hemolytic Anaemias
More LessAuthors: Shikha Sharma and Utkarsh SharmaMitapivat (AG-348) is a novel, first-in-class oral small-molecule allosteric activator of the pyruvate kinase enzyme. Mitapivat has been shown to significantly upregulate both wild-type and numerous mutant forms of erythrocyte pyruvate kinase (PKR), increasing adenosine triphosphate (ATP) production and reducing levels of 2,3-diphosphoglycerate. Given this mechanism, mitapivat has been evaluated in clinical trials in a wide range of hereditary hemolytic anaemias, including pyruvate kinase deficiency (PKD), sickle cell disease, and thalassemia.
The technique entails searching numerous search engines, such as PubMed, Science Direct, and Sci Finder, for relevant citations to the current subject matter. This is done in order to obtain the data that is required. In relation to medicine, mitapivat has been examined for its ability to cure a wide variety of inherited haemolytic anaemias in clinical investigations. Some examples of these conditions include pyruvate kinase deficiency (PKD), sickle cell disease, and thalassemias.
It has been demonstrated that mitapivat is both safe and effective in treating adults with PKD in two phases III clinical trials, and the development of the medicine is very close to being finished. Based on these findings, mitapivat may end up becoming the very first medication in the history of the world to receive regulatory approval.
Allosteric activator of pyruvate kinase mitapivat has shown promise in treating various hereditary hemolytic anemias, including sickle cell disease, PKD, and alpha- and beta-thalassemia.
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Surface Solid Dispersion Technique for Solubility Enhancement of Nifedipine
More LessIntroductionPoor 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.
BackgroundNifedipine 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.
AimThe aim of this work is to use the surface solid dispersion approach to increase the solubility of nifedipine.
ObjectiveThe 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.
Materials and MethodsNifedipine 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.
ResultsFormulation 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%.
ConclusionThis 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.
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