Browsing by Author "Sukhbir Singh"

Now showing 1 - 7 of 7
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    Advances in Magnetofection & − Magnetically Guided Nucleic Acid Delievery:a Review
    (Chitkara University Publications, 2013-05) Sandeep Arora; Girish Gupta; Sukhbir Singh; Neelam Singh
    The aim of this work was to investigate the effects of the nature and concentration of cellulose derivatives on the release kinetics of ibuprofen from hydrogel matrices using a response surface method (RSM). A series of cellulose derivatives, as methyl, hydroxyethyl, hydroxypropyl and hydroxypropyl methyl celluloses (MC, HEC, HPC and HPMC) were used as polymer platforms and their impacts on drug release were studied and compared to those obtained with a reference formulation prepared with HEC. It was shown that the use of HPMC in the gel formulation contributes to the improvement of drug release and consequently its biodisponibility. Indeed, the increase in HPMC concentration forms a controlled system release because polymer chains relaxation. The drug is released under the effects of two phenomena: diffusion and relaxation of polymeric chains. Thus, the kinetic release passes from the kinetics of case II towards Fickian diffusion.
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    Design, Synthesis and Antidiabetic Activity of Novel Sulfamoyl Benzamide Derivatives as Glucokinase Activators
    (Chitkara University Publications, 2018-11-02) Ajmer Singh Grewal; Kapil Sharma; Sukhbir Singh; Vikramjeet Singh; Deepti Pandita; Viney Lather
    The present work has been planned to design, synthesize and evaluate the antidiabetic potential of a series of sulfamoyl benzamide derivatives as potential glucokinase (GK) activators. A new series of sulfamoyl benzamide derivatives was synthesized starting from 3-nitrobenzoic acid and characterized. In silico docking studies were performed to determine the binding interactions for the best fit conformations in the allosteric site of GK enzyme. Based on the results of in silico studies, the selected molecules were tested for their antidiabetic activity in animal studies (alloxan induced diabetic animal model). Compound 7 exhibited highest antidiabetic activity in animal studies. The results of in vivo antidiabetic activity studies were found to be in parallel to that of docking studies. These newly synthesized sulfamoyl benzamide derivatives thus can be treated as the initial hits for the development of novel, safe, effective and orally bioavailable GK activators as therapeutic agents for the treatment of type 2 diabetes.
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    Development, physicochemical characterization and in-vitro evaluation of herbal sunscreen lotion
    (Chitkara University Publications, 2015-11-17) Sandeep Arora; Neelam Sharma; Akanksha Mahajan; Jaspreet Kaur; Sukhbir Singh
    Ultraviolet radiations have shorter wavelengths and can reach earth’s surface through penetrating clouds. UV-A rays leads to aging while UV-B rays causes burning of skin. Sunscreens protect the skin from harmful effects of sun including appearance of erythema, premature photo-ageing and facilitate to diminish the manifestation of facial red veins and blotchiness. In this investigation, herbal sunscreen was prepared using Shea butter, almond oil, raspberry oil, jojoba oil, zinc oxide and titanium dioxide as active ingredients. Fabricated lotions were evaluated for physicochemical parameters i.e. color, pH, viscosity and spreadability. Sun protection efficacy of lotion was determined in term of sun protection factor (SPF) by in-vitro spectrophotometric method. Total 10 formulations were made with different compositions F1-F10. The pH of formulations ranges from 6.10 (F6) to 8.34 (F5). The viscosity of formulations ranges from 1500 (F1) to 3586 (F10). The spreadability of formulations ranges from 10.56±0.8 (F1) to 30.65±0.7 (F10). The physicochemical parameters of formulation F6 and F10 were found to be in controlled range justifying its compatibility with skin and confirming good cosmetological property. Stability study of optimized lotion was performed after storage of formulation at 25°C and 60 % RH as well as 40°C and 75 % RH for three months. Stability of lotion was evaluated on the basis of changes in physicochemical parameters i.e. color, pH, viscosity and spreadability and SPF. F10 has SPF value of 15.71±0.07 (medium protection sunscreen). The optimized formulations might provide good moisturizer, emollient, anti-ageing and anti-wrinkle effect with good sun protection.
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    Formulation, Optimization and Evaluation of Sustained Release Microspheres using Taguchi Design
    (Chitkara University Publications, 2014-05) Sukhbir Singh; Sandeep Arora; Neelam; Dharna Allawadi
    The aim of present study is to prepare microspheres of eudragit RL 100 loaded with Nefopam Hydrochloride by single emulsion solvent evaporation technique. Taguchi L9 orthogonal array design has been used to optimize the composition and operating conditions for preparation of formulations. Nine batches (F1-F9) were prepared by taking three independent variables (X1- drug: polymer ratio, X2- stirring speed and X3- stirring time) at three levels (+1, 0, -1). Response variables studied for batches (F1-F9) were mean particle size (μm) (Y1), drug entrapment efficiency (% w/w) (Y2) and drug loading (% w/w) (Y3). Drug- polymer compatibility study was carried out by DSC and FTIR spectroscopy and indicates no physicochemical interaction. Microspheres were analyzed for morphological characteristics, mean particle size, drug entrapment efficiency, drug loading and in-vitro drug release. Percentage cumulative drug release for optimized batch F5 was found to be 85.421 ± 0.054 and followed higuchi model for release of drug.
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    In Silico Designing of Novel Thiazolidine-2-one Derivatives as Dual PDE4/7 Inhibitors for Inflammatory Disorders
    (Chitkara University Publications, 2017-11-02) Ajmer Singh Grewal; Neelam Sharma; Sukhbir Singh; Sandeep Arora
    Phosphodiesterase 4 (PDE4) and phosphodiesterase 7 (PDE7), members of PDE super family, catalyse metabolism of secondary messenger cyclic adenosine monophosphate leading to augmented inflammatory processes in pro-inflammatory and immune-modulatory cells. Dual inhibitors of PDE4/7 are a novel class of drug candidates which can regulate pro-inflammatory as well as function of immune T-cell and are particularly beneficial for the treatment of various inflammatory diseases devoid of unwanted actions. Intense efforts have been directed towards the development of effective dual inhibitors of both PDE4 and PDE7, but not much success has been reported till yet. The aim of present study was to design some newer substituted thiazolidine-2-one derivatives as dual inhibitors of PDE4/7 using structure based rational drug design approach. A new series of thiazolidine-2-one analogues were designed and molecular docking was performed using AutoDock Vina to explore the bonding interactions of the designed molecules with the amino acid residues in the active site of target proteins. The docking study indicated that all the substituted thiazolidine-2-one derivatives have appreciable binding interactions with protein residues of both PDE4 and PDE7. The newly designed compounds could be used as lead molecules for development potent and non-toxic dual inhibitors of PDE4/7 for the management of various inflammatory conditions.
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    Molecular Docking Evaluation of Some Natural Phenolic Compounds as Aldose Reductase Inhibitors for Diabetic Complications
    (Chitkara University Publications, 2017-11-02) Ajmer Singh Grewal; Neelam Sharma; Sukhbir Singh; Sandeep Arora
    The enzyme aldose reductase (AR) is a member of aldoketoreductase super-family which catalyzes the formation of sorbitol from glucose through polyol pathway of glucose catabolism. Reduced sorbitol production via polyol pathway due to AR inhibition is a target of choice for controlling major complications of diabetes. Epalrestat is the only commercially available inhibitor of AR till date,thus, there is a great need to search for more economical, nontoxic and safer inhibitors of AR enzyme. Flavonoids, the polyphenol compounds in plants have been reported for inhibitory effects against AR. The objective of this study is to explore the binding modes of natural phenolic compounds with AR to design safer natural drugs as alternatives to synthetic drugs. We conducted a molecular docking study on some natural phenolic compounds with AR enzyme in complex with the synthetic inhibitor. The overlay of the docked pose of the selected natural phenols with the ARreference inhibitor complex showed that the selected natural compounds have the similar binding pattern with the active site residues of the enzyme as that of co-crystallized inhibitor. The results of docking study showed the best binding affinity of AR with that of 2-(4-hydroxy-3-methoxyphenyl) ethanoic acid and butein, having the lowest binding free energy of –9.8 kcal/mol and–9.7 kcal/mol, respectively. This information can be utilized to design potent, economical and non-toxic natural AR inhibitors from natural phenols for the therapeutics of diabetic complications.
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    Molecular Docking Studies of Phenolic Compounds from Syzygium cumini with Multiple Targets of Type 2 Diabetes
    (Chitkara University Publications, 2018-11-02) Ajmer Singh Grewal; Neelam Sharma; Sukhbir Singh; Sandeep Arora
    Treatment of type 2 diabetes without any side effects is still a challenge to the medical system. This leads to increasing demand for natural products with antidiabetic activity with fewer side effects. Syzygium cumini is a traditional herbal medicinal plant and is reported to possess a variety of pharmacological actions. It contains various types of chemical constituents including terpenoids, tannins, anthocyanins, flavonoids and other phenolic compounds. Some flavonoids and other phenolic compounds from S. cumini were reported in literature to have type 2 antidiabetic potential. The main objective of the current investigation was in silico screening of some phenolic compounds from S. cumini against multiple targets associated with type 2 diabetes to explore the mechanism of antidiabetic action and prediction of binding mode using molecular docking studies. In silico docking studies were performed for the selected molecules in the binding site of multiple targets associated with type 2 diabetes (α-glucosidas , dipeptidyl peptidase 4, glycogen synthase kinase 3, glucokinase and glucagon receptor). Amongst the compounds tested in silico, rutin showed appreciable binding with multiple targets of type 2 diabetes including α-glucosidase, dipeptidyl peptidase 4, glycogen synthase kinase 3, and glucagon receptor. Catechin was found to inhibit both α-glucosidase, and dipeptidyl peptidase 4. This information can be utilized for the design and development of potent multi-functional candidate drugs with minimal side effects for type 2 diabetes therapeuticsa.