Papers by Giriraj Kulkarni
Current drug research reviews, Apr 12, 2021
Objective: To study therapeutic potential of Antileukotriene drug- Camellia sinensis extract co-f... more Objective: To study therapeutic potential of Antileukotriene drug- Camellia sinensis extract co-formulation on histamine induced asthma in guinea pigs. Method: SRSD of Montelukast sodium was prepared by solvent evaporation method. Lyophilized aqueous extract of Camellia sinensis leaves and SRSD mixture was filled in capsule and capsule shell was coated to achieve initial release lag time. In vitro and pharmacokinetic study of capsules was done and compared with commercial tablets. Further role of green tea, as an antioxidant adjunct for asthma management has been analyzed by lung histology, mast cell count and oxidative stress assay in serum of control and experimental animals. Results: The drug release from commercial tablet was immediate and rapid but capsule has shown initial 3.5 hr lag time followed by sustained action up to 8 hr. Pharmacokinetic results shows that studied formulations are bioequivalent with respect to Cmax and AUC, while rest parameters showed significance difference. Mast cells count in lung tissue were increased (p<0.001) in experimental group along with glycoprotein deposition in asthmatic bronchioles. Level of SOD and GPX were decreased (p<0.05) while CAT is increased (p<0.04) in asthma group in comparison to control. Conclusion: In the experimental animal model, co-formulation was effective in modulating allergic inflammation and contributing to a better control of the inflammatory response. Our findings suggest that Camellia sinensis leaves extract may be used as an adjunct for future improvements in asthma treatment and prevention.
Analytical chemistry, an Indian journal, 2010
A simple highly sensitive spectrophotometric method was developed for the quantification of metfo... more A simple highly sensitive spectrophotometric method was developed for the quantification of metformin hydrochloride. The method involves the reaction of the target compound with ninhydrin reagent at specific pH 5.6 to produce a wine red color chromogen. The derivative chromogen exhibits absorption maxima at 567nm. At the specific pH of the reaction where no degradation may occur with that medium the proposed method can be utilized as a stability indicating assay. The different experimental parameters affecting the derivatization reaction were carefully studied and incorporated into the procedure. Under the described conditions the proposed method is linear over the concentration range of 10-70mcg/ml and the coefficient of determinationwere >0.999(n=6) with a relative standard deviation of 0.083% (n=6). The average recovery of the target compound is 99.47% with a limit of quantification (LOQ) of 2.637mcg/ml and the limit of detection (LOD) 0.870mcg/ml. The mechanism of the derivatization reaction is proposed and advantages of the proposed method are discussed.
Polysaccharides, especially from marine algae, find many major applications in the field of biote... more Polysaccharides, especially from marine algae, find many major applications in the field of biotechnology. Their applications in biotechnology are due to their gelling properties and encapsulating capabilities. Agar, agarose, alginates and carrageenan are the polysaccharides that are used commonly in biotechnology. The uses of polysaccharides in biotechnology include gelelectrophoresis, molecular sieving, gene fragment separation, gene mapping and immobilization of cells and enzymes. In this article, the common polysaccharides of biotechnological importance, their sources, structural features and their biotechnological applications are reviewed.
Free Radicals and Antioxidants, Oct 1, 2011
Free radicals are atoms or groups of atoms with an odd (unpaired) number of electrons and can be ... more Free radicals are atoms or groups of atoms with an odd (unpaired) number of electrons and can be formed when oxygen interacts with certain molecules. Free radicals due to environmental pollutants, radiation, chemicals, toxins, deep fried and spicy foods as well as physical stress, cause depletion of immune system antioxidants, change in gene expression and induce abnormal proteins. [1,2] Increased free radical formation may produce a continuous level of oxidative damage [3,4] , which leads to many diseases such as atherosclerosis, cancer, stroke, asthma, arthritis and other age related diseases. [3,5] However, the generated free radicals are removed from the body through the antioxidant defense mechanisms. Antioxidants are considered as possible protection agents reducing oxidative damage of human body from reactive
Current Nutrition & Food Science, May 21, 2015
A (3) 2 -factorial design was employed to optimize extraction of high ester pectin using two inde... more A (3) 2 -factorial design was employed to optimize extraction of high ester pectin using two independent variables (extraction time and temperature) from mango fruit waste i.e. its peels. Citric acid solution (0.5 molar) was used to acidify water at pH 2. Using a new methodology waste management was done by extracting pectin from peels obtained from local juice shops. It was then characterized as pharmaceutical excipient. Combined effects of independent variables on degree of esterification (DE) were investigated and % deviation from predicted response was calculated. The model built for DE shows that both variables have significant effect on response and temperature of extraction medium which has a negative effect on DE. 3-D surface response showed relationship of independent variables on DE. Results showed that batch F4 deviated 10.83% from predicted response and had maximum D.E. (68.97%), followed by F7 which had value of 63.64% with relatively less deviation (0.99%).
Current nanomaterials, Aug 24, 2017
Journal of Drug Delivery Science and Technology
Natural Product Communications
SARS-CoV-2 has been responsible for over 500 million cumulative cases all over the world since De... more SARS-CoV-2 has been responsible for over 500 million cumulative cases all over the world since December 2019 and has marked the third introduction of a highly pathogenic virus after SARS-CoV and MERS-CoV. This virus is in a winning situation because scientists are still racing to explore effective therapeutics, vaccines, and event treatment regimens. In view of progress in current disease management, until now none of the preventive/treatment measures can be considered entirely effective to treat SARS-CoV-2 infection. Therefore, it is required to look up substitute ways for the management of this disease. In this context, herbal medicines could be a good choice. This article emphasizes the antiviral potential of some herbal constituents which further can be a drug of choice in SARS-CoV-2 treatment. This article may be a ready reference for discovering natural lead compounds and targets in SARS-CoV-2 associated works.
Letters in Drug Design & Discovery
: Lung cancer is a leading cause of cancer-related deaths globally. The availability of successfu... more : Lung cancer is a leading cause of cancer-related deaths globally. The availability of successful anticancer agents in the market is limited, and the development process of a new drug molecule is slow and difficult. The currently available commercial formulations are not sufficient to produce the desired therapeutic response within a specific time limit. Therefore, there is an urgent need to develop novel nanocarrier-based therapies to defeat the restrictions of existing therapeutics. Nanoparticles have been investigated as novel formulations but are often inefficient in practical applications. However, several unanswered questions and challenges exist in their clinical development; thus, a better understanding of their influence on cancer biology, stability, and toxicity needs to be gained. This review discusses different types of lung cancers as well as diagnostic approaches to lung cancer. The review also explores the drug targeting mechanisms to cancer cells through nanoparticles and multi-drug resistance-associated challenges in lung cancer therapy. Various nanocarrier systems that are safe and effective for drug delivery in the treatment of lung cancer have been discussed. This communication will be of high relevance to the biological, formulation, and translational scientists working in the field of cancer biology and drug delivery.
Clinical Psychopharmacology and Neuroscience, 2021
Objective: Vascular Dementia (VaD), is associated with metabolic conditions. Diabetes is a major ... more Objective: Vascular Dementia (VaD), is associated with metabolic conditions. Diabetes is a major risk factor for the development of VaD. This study investigates the efficacy of ulinastatin (UTI) and sulforaphane (SUL) in streptozotocin (STZ)-diabetes induced vascular endothelium dysfunction and related dementia. Methods: Single dose STZ (50 mg/kg i.p.) was administered to Albino Wistar rats (male, 200−250 g). Morris water maze and attentional set shifting tests were used to assess the spatial learning, memory, reversal learning, and executive functioning in animals. Body weight, serum glucose, serum nitrite/nitrate, vascular endothelial function, aortic superoxide anion, brains' oxidative markers (thiobarbituric acid reactive species-TBARS, reduced glutathione-GSH, superoxide dismutase-SOD, and catalase-CAT), inflammatory markers (IL-6, IL-10, TNF-, and myeloperoxidase-MPO), acetylcholinesterase activity-AChE, blood brain barrier (BBB) permeability and histopathological changes were also assessed. UTI (10,000 U/kg) and SUL (25 mg/kg) were used alone as well as in combination, as the treatment drugs. Donepezil (0.5 mg/kg) was used as a positive control. Results: STZ-administered rats showed reduction in body weight, learning, memory, reversal learning, executive functioning, impairment in endothelial function, BBB permeability, increase in serum glucose, brains' oxidative stress, inflammation, AChE-activity, BBB permeability and histopathological changes. Administration of UTI and SUL alone as well as in combination, significantly and dose dependently attenuated the STZ-diabetes-induced impairments in the behavioral, endothelial, and biochemical parameters. Conclusion: STZ administration caused diabetes and VaD which was attenuated by the administration of UTI and SUL. Therefore, these agents may be studied further for the assessment of their full potential in diabetes induced VaD.
Medical Hypotheses, 2020
Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on ... more Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre-including this research content-immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
Medicinal Plants - International Journal of Phytomedicines and Related Industries, 2021
Asian Journal of Pharmaceutical Research and Health Care, 2011
A gel forming Polysaccharide gum obtained form the bark of Araucaria bidwilli was employed as a m... more A gel forming Polysaccharide gum obtained form the bark of Araucaria bidwilli was employed as a matrix sustained release tablet formulation of Diclofenac sodium (a non steroidal anti inflammatory agent). The effect of Araucaria bidwilli gum ( Natural ) and Synthetic polymer Hydroxypropyl methyl cellulose ( HPM C K4 M ) on the release of Diclofenac sodium was studied. The FT - IR spectroscopic studies of drug, gum and mixture indicated no chemical interaction . Six formulations were prepared by wet granulation method containing Araucaria bidwilli gum pow der concentration 10 % 20 % & 30 % w \ w and 10 % 20% &30% w \ w of HPMC K4M with sufficient volume of granulating agent Polyvinyl pyrrolene (PVP K 30) , Avicel pH101 as diluents , Magnesium stearate and Aero silis used lubricant and glidant respectively . This study was carried out to find out the difference between synthetic and natural gum and whether synthetic gum can be replaced by natural gums. Physical and techno logical studi...
Basic and Clinical Neuroscience Journal, 2021
Introduction: A neurodevelopmental disorder, autism is typically identified with three primary be... more Introduction: A neurodevelopmental disorder, autism is typically identified with three primary behavioral consequences, such as social impairment, communication problems, and limited or stereotypical behavior. Because of its co-morbidity and lack of therapeutic options, autism is a global economic burden. A short chain of fatty acid, propionic acid is formed biologically by the gut microbiome. Propionic acid levels that are too high can cause leaky intestines, which can lead to autism-like symptoms. Methods: To induce autism, male Albino Wistar rats were given propionic acid (250 mg/kg/po on the 21st, 22nd, and 23rd postnatal days). Rats also received a ryanodine receptor antagonist (Ruthenium red: 3 mg/kg/po; postnatal 21st to 50th day) to see what influence it had on propionic acid-induced autism. Anxiety, social behavior, and repeated behaviors were all assessed, as well as oxidative stress, inflammatory indicators, neuro signaling proteins, and blood-brain barrier permeability. ...
European Journal of Pharmacology, 2020
Autism spectrum disorder (ASD) is a neurodevelopmental disorder with complex aetiology and phenot... more Autism spectrum disorder (ASD) is a neurodevelopmental disorder with complex aetiology and phenotypes. Phosphodiesterase-10A (PDE10A) inhibition has shown to provide benefits in various brain conditions. We investigated the role of a PDE10A inhibitor, papaverine on core phenotypes in prenatal-valproic acid (Pre-VPA) model of ASD. In order to identify probable mechanisms involved, the effects on several protein markers of neuronal function such as, neurogenesis-DCX, neuronal survival-BDNF, synaptic transmission-synapsin-IIa, neuronal transcription factor-pCREB, neuronal inflammation (IL-6, IL-10 and TNF-α) and neuronal oxidative stress (TBARS and GSH) were studied in frontal cortex, cerebellum, hippocampus and striatum. Pre-VPA induced impairments in social behaviour, presence of repetitive behaviour, hyper-locomotion, anxiety, and diminished nociception were studied in male Albino Wistar rats. Administration of papaverine to Pre-VPA animals resulted in improvements of social behaviour, corrected repetitive behaviour, anxiety, locomotor, and nociceptive changes. Also, papaverine resulted in a significant increase in the levels of BDNF, synapsin-IIa, DCX, pCREB, IL-10 and GSH along with significant decrease in TNF-α, IL-6 and TBARS in different brain areas of Pre-VPA group. Finally, high association between behavioural parameters and biochemical parameters was observed upon Pearson's correlation analysis. Papaverine, administration rectified core behavioural phenotype of ASD, possibly by altering protein markers associated with neuronal survival, neurogenesis, neuronal transcription factor, neuronal transmission, neuronal inflammation, and neuronal oxidative stress. Implicating PDE10A as a possible target for furthering our understanding of ASD phenotypes.
This study belongs to identification of suitable COVID-19 inhibitorsCoronavirus became pandemic v... more This study belongs to identification of suitable COVID-19 inhibitorsCoronavirus became pandemic very soon and is a potential threat to human lives across the globe. No approved drug is currently available therefore an urgent need has been developed for any antiviral therapy for COVID-19. For the molecular docking study, ten herbal molecules have been included in the current study. The three-dimensional chemical structures of molecules were prepared through ChemSketch 2015 freeware. Molecular docking study was performed using AutoDock 4.2 simulator and Discovery studio 4.5 was employed to predict the active site of target enzyme. Result indicated that all-natural molecules found in the active site of enzyme after molecular docking. Oxyacanthine and Hypericin (-10.990 and -9.05 and kcal/mol respectively) have shown good binding efficacy among others but Oxyacanthine was the only natural product which made some of necessary interactions with residues in the enzyme require for target in...
Asian Journal of Pharmaceutical and Clinical Research, 2019
Objective: Pharmacokinetic evaluation of montelukast sodium chronomodulated capsules (sustained-r... more Objective: Pharmacokinetic evaluation of montelukast sodium chronomodulated capsules (sustained-release solid dispersion of drug enclosed in pH-sensitive film-coated hard gelatin shell) and marketed tablets has been carried out in this study. Methods: A single oral dose of prepared capsules and marketed conventional tablets was administered in healthy male Dunkin-Hartley albino guinea pigs. Blood samples were collected at different time intervals and plasma concentration of drug was determined by reversed-phase high-performance liquid chromatography. Different pharmacokinetic parameters were assessed from plasma drug concentration-time profile by one-compartment model, first-order kinetics. Results: Pharmacokinetic parameters such as time to reach maximum concentration, elimination rate constant, elimination half-life, and mean residence time data indicates that drug release from chronomodulated capsules is significantly prolonged with initial release lag time of 3.5–4 h in comparis...
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Papers by Giriraj Kulkarni