IDMA ACG - SCITECH RESEARCH PAPER AWARD 2020 - 2021

In order to encourage R & D in the country, IDMA has instituted “Research Awards for the Best Original Research Papers” published in the “Indian Drugs” every year from the year 1981-82 and the Award for the Best Review Article was instituted in 2001. The Best Original Research Papers are evaluated in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

The Award will be known as ‘IDMA ACG-SCITECH RESEARCH PAPER AWARD’ from this year. The IDMA ACG-SCITECH RESEARCH PAPER AWARD will be in the form of a plaque and a cash award of Rs. 5000/- in each discipline and the Best Review Article Award is in the form of a citation and special cash award of Rs. 7500/-. 

These Awards are presented to the recipients during the IDMA Annual Day Celebrations every year.

REVIEW ARTICLE

Paper : Non-steroidal Human Performance Enhancing Agents
Author(s) : Mehta Gaurav, Joshi Maithili and Joshi Shreerang
Institute : Institute of Chemical Technology, Nathalal Parekh Marg, Matunga (E), Mumbai-400 019, Maharashtra, India
Volume : 57 (12)
Page nos. : 7-25
Abstract : Multiple studies have been conducted, many within the last 3-5 years, to develop a deeper understanding into how certain chemical substances enhance and improve certain aspects of our performance, both mental and physical. The successful synthesis, isolation and purification of such human performance enhancing substances have led to breakthroughs not only in the treatment of debilitating diseases such as Alzheimer’s and Parkinson’s disease, but also have a significant impact on endurance training. While the chief use of such performance enhancing agents is in the treatment of diseases like anaemia, depression, attention deficit and neurodegenerative disorders, such substances are also misused and sometimes abused in sport. This review highlights 6 major substances used as performance enhancers, namely, creatine, racetams, melatonin, caffeine, cholinergics and EPO. The six substances enhance different features of human performance. The chemistry of these substances, their chemical biology, methods of synthesis and latest data obtained from various clinical trials are discussed.

PHARMACEUTICAL CHEMISTRY

Paper : Synthesis, Biological Evaluation And Docking Studies Of Non Hepatotoxic 5-Substituted Thiazolidine-2, 4-Diones As Antidiabetic, Anti-Hyperlipidemic, Anti-Oxidant And Cytotoxic Agents
Author(s) : Shukla Karuna S., Pandey Shailendra and Chawla A Pooja
Institute : Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga - 142 001, Punjab, India
Volume : 57(09)
Page nos. : 19-37
Abstract : A series of eleven thiazolidine-2, 4-dione (TZD) derivatives, were synthesized and characterized by FT-IR, 1H NMR and mass spectral analysis. All the synthesized TZD derivatives were screened for their in vitro and in vivo anti-diabetic and antioxidant, activities and cytotoxicity. In vivo antihyperglycemic effect was assessed by measuring plasma glucose (PG) levels in alloxan-induced type II diabetic rat models. The compound 4h exhibited better blood glucose lowering activity than the standard drug rosiglitazone. The synthesized TZD derivatives were evaluated for hepatotoxicity and pancreatic tissue studies. Antioxidant activity was evaluated by DPPH method and H2O2 method. Compounds 4a and 4b exhibited potent antioxidant activity. Among the tested compounds for cytotoxicity using MTT assay method, compound 4i exhibited better viability and cytotoxicity activity. Thiazolidinedione derivatives were evaluated for their affinity towards target PPARγ, using rosiglitazone as the reference compound molecular docking visualization through FlexX docking program.
From selected anti-diabetic targets, the proposed derivatives exhibited better interaction with PPARγ receptor, where rosiglitazone showed docking score of -19.891 kJ/mol, compound 4h exhibited highest docking score of -31.6068 kJ/mol. The study showed that all the studied compounds were showing higher docking score when compared to control drug rosiglitazone and it could be a remarkable starting point to evaluate structure activity relationships to develop new lead molecules with potential anti-diabetic activities.

NATURAL PRODUCTS/ PHARMACOGNOSY/PHYTOCHEMISTRY

Paper : Enhanced Anti-inflammatory and Anti-migratory effect of Herbal Nano-statins on HEPG2 cancer cells
Author(s) : Mehra Akansha, Chauhan Sonal, Jain V.K. and Nagpal Suman
Institute : Amity Institute of Advanced Research and Studies (Materials & Devices), Amity University, Noida-201 303, UP, India
Volume : 57 (12)
Page nos. : 51-55
Abstract : Mushroom (oyster mushroom, Pleurotus sajor caju) is a rich depository of statins, HMG-CoA reductase inhibitors that also act as anti-cancer agents. In the present study, anti-inflammatory and anti-migratory effects of prior synthesized and characterized herbal nano-statins on HepG2 have been discussed for the first time. The results showed that herbal nano-statins were able to inhibit the NO production in dose dependent manner with 93.72 % inhibition at 80 μg/mL of nano-statins and it attained saturation if the dose is further increased. Bulk statins had less potency to inhibit the production of NO (30 % at 100μg/mL) as compared to nano-statins. Nano-statins and bulk statins also inhibited the migration of cancer cells by 97.86 % and 53.43 %, respectively, at a concentration of 100 μg/mL. This study might bring in more insights to use herbal nano-statins as an alternative treatment to fight against various other types of cancers and other biomedical complications.

PHARMACEUTICAL ANALYSIS

Paper : Sensitive Bio Analytical Method Development For Venetoclax And Validation In Human Plasma By LC-ESI-MS/MS
Author(s) : Potluri H
Institute : Department of Chemistry, Gudlavalleru Engineering College, Gudlavalleru - 521 356, Andhra Pradesh, India
Volume : 57(06)
Page nos. : 32-38
Abstract : A specific and sensitive method of liquid chromatography–tandem mass spectrometry was demonstrated for the experimental determination of venetoclax in human plasma utilising venetoclax-D8 as an internal standard. The column Xbridge C18, 50 × 4.6mm, 5 μm was used for attaining chromatographic separation by utilising 10mM ammonium formate and methanol as isocratic mobile phase in the composition ratio of 20:80 (V/V). The flow-rate selected was 0.7mL/min. Venetoclax and venetoclax-D8 are identified in multiple reaction monitoring (MRM) positive mode with proton adducts at m/z 869.53 →553.21 and m/z 877.14 → 553.23, respectively. For the successful extraction of drug as well as internal standard, Liquid-Liquid extraction technique was efficiently utilised. The developed technique was established in a linear concentration range of 5.0-5000.0 pg/mL along with correlation coefficient (r2) of 0.9994. Intra and inter-day precisions were found to be 0.7 to 1.90% and 0.7 to 2.0 % for venetoclax and venetoclax-D8, respectively. Accuracy was found to be within 98.6 to 101.99% and 99.17 to 101.14 % for venetoclax and venetoclax-D8, respectively. It was observed that throughout the bench top studies, post-operative stability studies and freeze-thawing cycles, venetoclax retained stability.

PHARMACEUTICS

Paper : Formulation and optimization of Ritonavir nasal nanosuspension for brain targeting
Author(s) : Tapasya R. Mulam, Sanjay J. Kshirsagara and Smita P. Kakad
Institute : Department of Pharmaceutics, MET’s Institute of Pharmacy, Bhujbal Knowledge City, Adgaon, Nashik - 422 003, Maharashtra, India
Volume : 58(04)
Page nos. : 28-41
Abstract : Nowadays, HIV associated neurological disorder especially HIV-1 virus infection is enhanced. Current available HIV therapies only reduce the plasma viral level and do not kill the virus completely. Administered dosage form does not reach the central nervous system (CNS) completely by the conventional approach. The oral route of drug administration, causes gastrointestinal irritation, hepatic metabolism and slow onset of action and some methods are invasive, resulting in the patient's non compliance. To overcome these problems, an effective novel formulation that will directly reach the CNS or brain needs to be developed. This study aims to formulate intranasal nanosuspension of ritonavir. Ritonavir is widely used as an antiretroviral agent and it is a protease enzyme inhibitor which is poorly soluble in water. High pressure homogenization technique was used for preparation prepare and optimization of nanosuspension by using 2 factors 3 level full factorial design, which is further characterized for particle size, polydispersity index, zeta potential, pH, drug content, in vitro drug diffusion and ex vivo permeation study. For stability of nanosuspension, lyophilization of optimized formulation was done. A comparison study between plain drug, nanosuspension and the lyophilized formulation was carried out, and it showed a significant increase in drug release from the membrane.

PHARMACOLOGY

Paper : Rapid Green Synthesis of Gold and Silver Nanoparticles Using Ethanol Extract of Kedrostis Foetidissima (Jacq.) Cogn. And Its Anticancer Efficacy Against A549 Human Lung Cancer Cell Lines
Author(s) : Amutha Muthusamy and Lalitha Pottail
Institute : Department of Chemistry, Nallamuthu Gounder Mahalingam College, Pollachi, Coimbatore - 642 001, Tamilnadu, India
Volume : 58(03)
Page nos. : 30-40
Abstract : This study is mainly focused on the synthesis of gold and silver nanoparticles using Kedrostis foetidissima (Jacq.) Cogn, a traditional medicinal plant, their characteristics and their efficacy on Human Lung cancer cell lines (A-549). Gold and silver nanoparticles were synthesised using ethanol extract of K. foetidissima by solar irradiation method. The formation of gold nanoparticles (AuNPs) and silver nanoparticles (AgNPs) were authenticated by UV-Visible, FT-IR, XRD SEM, and TEM analysis. The solar irradiation method yielded beautiful floral shaped AuNPs and spherical shaped AgNPs of the size 8.38 nm and 33.20 nm, respectively. The cytotoxicity effect of these biogenic nanoparticles against A-549 cell lines was monitored through MTT assay. The results have revealed that AgNPs shows significant cytotoxicity (IC50-62.16μg/mL) towards A-549 than AuNPs (IC50- 106.27 μg/mL). The shape dependency of the nanoparticles is also clear from the study.

IDMA ACG-SCITECH RESEARCH PAPER AWARD - 2019

In order to encourage R & D in the country, IDMA has instituted “Research Awards for the Best Original Research Papers” published in the “Indian Drugs” every year from the year 1981-82 and the Award for the Best Review Article was instituted in 2001. The Best Original Research Papers are evaluated in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

From this year, the Award will be known as ‘IDMA ACG-SCITECH RESEARCH PAPER AWARD’. The IDMA ACG-SCITECH RESEARCH PAPER AWARD will be in the form of a citation, plaque and a cash award of Rs. 5000/- in each discipline and the Best Review Article Award is in the form of a citation, plaque and special cash award of Rs. 7500/-.

These Awards are presented to the recipients during the IDMA Annual Day Celebrations every year.

REVIEW ARTICLE

Paper : ‘Drug Delivery to Retina: A Review’
Author(s) : Shelke D. A. and Shirolkar S.*
Institute : Department of Pharmaceutics, Dr. D.Y.Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune - 411018, Maharashtra, India
Volume : 56 (09)
Page nos. : 7-21
Abstract : The drug delivery to posterior segment especially to retina of eye is difficult due to various barriers. The diseases affecting the retina of eye are increasing and hence there is need to develop approaches for drug delivery to retina. This review describes the anatomy of retina, barriers associated with it, and diseases of retina. The drug delivery to retina by systemic, topical, intravitreal injection, intravitreal implant along with advance nanotechnology based and transporter mediated drug delivery is discussed here. The recent technologies in retinal drug delivery are also discussed to give comprehensive recent information about retinal drug delivery.

PHARMACEUTICAL CHEMISTRY

Title : Synthesis and evaluation of some newer quinazolinonyl substituted benzoxazepinyl / benzothiazepinyl indoles as potent anticonvulsant agents
Author(s) : Dr Archana*
Institute : Medicinal Chemistry Laboratory, Department of Chemistry, Meerut College, Meerut - 250 001, Uttar Pradesh
Volume : 56 (03)
Page nos. : 18-24
Abstract : new series of 3-[3-amino-2-methyl-6-substituted quinazolin-4(3H)-onyl chalconyl)-2-substituted indoles (3-8), 3-[3-Amino-2-methyl-6- substituted quinazolin-4(3H) -onyl-benzoxazepin/benzo -thiazepin2-yl] -2-substituted indoles (9-20) and 3-[3-amino-2-methyl-6-substituted quinazolin-4(3H) -onyl-3- (sub-stituted phenylaminomethylene) -benzoxazepin/benzothizepin-2-yl] -2- substitutedindoles (21-44) were synthesised and evaluated for anticonvulsant activity. All these compounds were screened in vivo, for their anticonvulsant activity and acute toxicity. Coumpund 44 , 3-[3-amino-2-methyl-6-bromoquinazolin4(3H)-onyl-3- (chlorophenylaminomethylene)- benzothiazepine-2-yl]-2-chloroindole, was found to be most potent compound of this series , more potent than standard drug phenytoin sodium. The homogeneity of all the compounds have been established by elemental analysis, IR and 1 H-NMR spectroscopy.

NATURAL PRODUCT

Title : Extraction, quantitative determination and spectral identification of Carnosic Acid – a diterpene antioxidant from Rosmarinus officinalis
Author(s) : Usha Rani N.*and Prasad Rao P.T.S.R.K.
Institute : Department of Freshman Engineering, Prasad V. Potluri Siddhartha Institute of Technology, Vijayawada - 520 007, Andhra Pradesh
Volume : 56 (05)
Page nos. : 7-13
Abstract : Carnosic acid is a benzenediol abietane diterpene having antioxidant and other medicinal activities. The medicinally active compound carnosic acid was isolated from leaves of the herb Rosmarinus officinalis. A simple solid-liquid extraction with solvent acetone in Soxhlet extractor was used for the extraction of compound from the plant source. The purity of the compound was studied using thin layer chromatography (TLC) and liquid chromatography-mass spectroscopy (LCMS) studies and the results were compared with standard carnosic acid. The result proves that the isolated compound was found to have 98.10% purity and no other impurities were observed. The molecular structure of the isolated compound was derived using spectral studies like UV, IR, NMR, C13 and mass spectroscopy. The spectral study proves that the compound has a molecular structure of 332 g/mol and molecular formula of C 20 H 28 O 4 .The molecular mass, formula and the molecular structure of the isolated compound was found to be similar to that of standard carnosic acid.

PHARMACEUTICS ANALYSIS

Title : Quantification of Hydrazine Hydrate in Imatinib Mesylate at Genotoxic Level by Chromatographic Method
Author(s) : Sojitra C., Agarwal S.*, Dholakia C., Sudhakar P. and Singh K. K.
Institute : New Drug Discovery, Zydus Research Centre, Cadila Healthcare Ltd. Ahmdabad, Gujarat
Volume : 56(12)
Page nos. : 45-52
Abstract : Hydrazine hydrate has genotoxic effect in nature and so it should be controlled down as Potential Genotoxic Impurity (PGI). Being polar molecule, hydrazine hydrate (N2H4.H2O) has no chromophores present in structure which can follow Lambert beer law, thus it is difficult to analyze. The present work described an accurate and highly sensitive reversed-phase liquid chromatography-UV derivatization method for determination of hydrazine in imatinib mesylate drug substance. The method of quantification was developed by attaching chromophores to hydrazine with derivatization, which helped to increase sensitivity. The derivatization of hydrazine hydrate was performed using 1% methanolic solution of benzaldehyde which acts as derivatizing agent. The derivatized product 1,2-dibenzylidenehydrazine gives maximum absorbance at 300 nm and at this wavelength no interference of solvents and other impurities are noted. Limit of detection for developed method was 0.002 µg/g. The developed method was validated to determine hydrazine content and can be used in quality control for commercial batch release of imatinib mesylate drug substances with a genotoxic specification limit level 1.87 µg/g by HPLC.

PHARMACEUTICS

Title : Synergistic Effect of Nigella Oil And Clotrimazole as Ethosomal Gel for Improved Treatment of Fungal Infections
Author(s) : Momin M.*, Butte K. and D’Souza A.
Institute : SVKM’s Dr. Bhanuben Nanavati College of Pharmacy, Mithibai College Campus, V. M. Road, Vile Parle (W), Mumbai – 400 056, Maharashtra
Volume : 56 (04)
Page nos. : 45-49
Abstract : The aim of this research work was to develop an ethosomal gel containing nigella oil encapsulated with clotrimazole (CLT) for improved antifungal activity. The ethosomes were prepared using soya lecithin (SpC) and Nigella oil (NO) as lipids by thin film hydration and they exhibited a particle size of 136±69 nm with an entrapment efficiency of 65.44±1.08 %. CLT ethosomal gel exhibited controlled release of CLT with a steady flux of 7.20mcg/cm 2 /h across cellophane membrane. The ethosomal gel was stable for 180 days with no significant change in physiochemical parameters. In vitro antifungal activity demonstrated a synergistic action of CLT and NO against the fungal strains compared to plain CLT and NO. This signifies that the combination of NO and CLT in an ethosomal gel has tremendous potential to serve as a synergistic topical anti-fungal preparation than simple ethosomal formulation of CLT.

PHARMACOLOGY

Title : Synthesis and Biological Evaluation of 2-Phenylpyrido [2,3-D] Pyrimidine Derivatives as Cyclin-Dependent Kinase (CDK) Inhibitors
Author(s) : Panchabhai V. B.*, Ingole P. G. and Butle S. R.
Institute : School of Pharmacy, SRTMU Campus, Vishnupuri, Nanded, Maharashtra
Volume : 56 (05)
Page nos. : 50-58
Abstract : We report a novel scaffold of 2-phenylpyrido[2,3-d]pyrimidine derivatives designed as structural analogues of dinaciclib. Sixteen derivatives were synthesised and evaluated for their CDK2/5 inhibition activity. Compounds 4-(2-(3-methoxybenzylidene)hydrazineyl)-2-phenylpyrido[2,3-d]pyrimidine (7i) and 4-(2-(3-nitrobenzylidene)hydrazineyl)-2-phenylpyrido[2,3-d]pyrimidine (7n) show promising IC50 and kinase selectivity. These compounds also show moderate anti-proliferative activity in the colon cancer HCT116 and breast cancer MCF7 cell lines. In molecular docking studies with CDK2, compounds 7i and 7n show binding similar to dinaciclib..

IDMA RESEARCH PAPER AWARDS - 2017

In order to encourage R & D in the country, IDMA has instituted “Research Awards for the Best Original Research Papers” published in the “Indian Drugs” every year from the year 1981-82 and the Award for the Best Review Article was instituted in 2001. The Best Original Research Papers are evaluated in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

The Best Research PaperAward is in the form of a citation and a cash award of `3000/- in each discipline and the Best Review Article Award is in the form of a citation and special cash award of `5000/-.

These Awards are presented to the recipients during the IDMA Annual Day Celebrations every year.

REVIEW ARTICLE

Paper : Lymphatic Delivery: Concept, Challenges And Applications
Author(s) : Bora C. R., Prabhu R. H. and Patravale V. B.*
Institute : Department of Pharmaceutical Sciences & Technology, Institute of Chemical Technology, Matunga, Mumbai – 400 019
Volume : 54 (08)
Page nos. : 5-22
Abstract : The lymphatic system is an additional circulatory system throughout the entire body. It plays a critical role in the recognition of immune system and response to disease. Lymphatic delivery has attracted a lot of attention for providing preferential chemotherapy and enhancing bioavailability of drugs that undergo hepatic first-pass metabolism. The anatomy and physiology of the lymphatic system, routes of administration and different physicochemical parameters of drug/carriers are overviewed. There are numerous challenges in targeting drugs and bioactives to specific sites, maintaining the desired action and crossing all the physiological barriers. Lymphatic delivery for various diseases employing various nanocarriers emerges as a new technology to provide a better therapeutic and diagnostic outcome.

PHARMACEUTICAL CHEMISTRY

Paper : Synthesis, Spectral Studies, Structural Evaluation and Antimicrobial Activity of Some Novel Cr(III) Complexes Containing Tetradentate Macrocyclic Ligands
Author(s) : Shukla S., Gautam S. Chandra S. and Kumar A.*
Institute : Department of Chemistry, Dyal Singh College, University of Delhi, Lodi Road, New Delhi - 110 003
Volume : 54 (06)
Page nos. : 20-29
Abstract : A string of novel coordination compounds of Cr(III) complexes have been derived and characterized from the macrocyclic ligands (L 1 -L 2 ) carried out by condensation reaction between ligands and the subsequent metal salt. The chemical composition of ligand was determined by analytical and spectral techniques i.e. elemental analysis, IR and Mass spectrocopy. Spectral techniques revealed tetradentate [N 4 ] the nature of ligand and its coordination mode to metal ion through nitrogen donor atoms. Metal complexes were characterized by elemental analyses, molar conductance, magnetic susceptibility measurements, IR, electronic spectra, ePR studies. The geometry of these complexes was ascertained by molecular modelling study by using Gaussian 09 program. All metal complexes were found to exhibit octahedral geometry around the metal ion. The newly synthesized macrocyclic ligands and metal complexes were subjected for antimicrobial screening to determine the inhibition and control against tested microorganisms, bacteria ( S.lutea , S.aureus, S.albus and E.coli ) and fungi ( A.fulviceps, U . hordei, A. niger and P.catinus ) by using disc diffusion method and agar plate technique, respectively. The experimental results suggest that metal complexes exhibit enhanced inhibition zone than free macrocyclic ligand.

NATURAL PRODUCTS

Paper : Chemical Examination of Chloroform Fraction of Cleome felina L. f.
Author(s) : Manjuparkavi K. and Jayanthi G.*
Institute : PG and Research Department of Botany, Vellalar College for Women (Autonomous), Erode - 638 012, Tamil Nadu
Volume : 54 (12)
Page nos. : 28-33
Abstract : The present investigation, the phytochemical composition of the chloroform fraction of Cleome felina L.f. by Gas Chromatography Mass Spectroscopy (GC-MS) analysis revealed totally 30 constituents. The major constituents are octadecane, 9-octadecenamide, (z)- , 2-tert-butyl-4-isopropyl-5-methylphenol, hexadecane, dodecane, 1-iodo-, tricosane, 2,6,10,14,18,22-Tetracosahexaene, 2,6,10,15,19,23- hexamethyl-, (all-e)-, 3-Tetradecene, (z)-, decane, 2-methyl- , 1,2-benzenedicarboxylic acid and bis(2- methylpropyl) ester.

PHARMACEUTICS

Paper : Development, Characterization and Brain Distribution Studies of Nanostructured Lipid Carrier Containing Saquinavir Mesylate for Nasal Administration
Author(s) : Mahajan H. S.* and Patel M. I.
Institute : R. C. Patel Institute of Pharmaceutical Education & Research, Near Karvand Naka, Shirpur - 425 405, Dist: Dhule, Maharashtra.
Volume : 54 (09)
Page nos. : 38-47
Abstract : The aim of the present study was to formulate saquinavir mesylate loaded nanostructured lipid carriers (SQVM-NLC) and evaluate its brain distribution after nasal administration. NLCs reveal some advantages for drug therapy over conventional carriers, including increased solubility, the ability to enhance storage stability, improved permeability and bioavailability, reduced adverse effect, prolonged half-life, and tissue-targeted delivery. SQVM-NLCs were prepared by hot high pressure homogenization and subsequent stabilization by lyophilization. QVM- NLC developed showed a particle with the size of 124.4 nm, polydispersity index of 0.267, entrapment efficiency of 73% and the zeta potential of -24.9 mV. The results from Scanning Electron Microscopy (SEM), powder X-ray diffraction (XRD)and differential scanning calorimetry (DSC) demonstrated that SQVM was present in NLC in an encapsulated molecule form. Mucosal toxicity study on sheep nasal mucosa showed no significant adverse effect of SQVMloaded NLC. SQVM-NLC showed slower release compared with saquinavir mesylate suspension in vitro. In vivo brain distribution studies demonstrated desired drug concentration in brain after intra nasal administration of SQVM-NLC than PDS. The results of the study also suggest that SQVM-NLC could be a promising drug delivery system for antiretroviral therapy

PHARMACEUTICAL ANALYSIS

Paper : Development and Validation of LC-MS/MS Method for The Simultaneous Determination of Pioglitazone and Voglibose in Human Plasma
Author(s) : Hemavathi G.* and Hipparagi S. M.
Institute : Department of Pharmaceutical Chemistry, KLE Academy of Higher Education & Research, (KLE University), Bangalore - 560 010, Karnataka
Volume : 54 (08)
Page nos. : 62-73
Abstract : A reliable, simple, robust and sensitive LC-MS/MS (Liquid Chromatography tandem Mass Spectrometric) method has been developed and validated that employs protein precipitation extraction method for the simultaneous determination of Pioglitazone and Voglibose in human plasma by using miglitol as internal standard. Chromatography conditions included an isocratic mobile phase composing of 5 mM ammonium formate buffer: acetonitrile in the ratio 50:50 V/V. the column used was Welchrom XB C18, with specifications of 50×4.6 mm, 5 μm, at a flow rate of 0.80 mL/min. the retention time of Pioglitazone, voglibose and miglitol occurred at ‾2.83, 0.8 and 0.70 min, respectively and the total chromatographic run time was 4.0 min. Pioglitazone and voglibose achieved a linear response function in human plasma at 1.07-958 ng/mL & 2.02-203 ng/mL respectively. Pioglitazone and voglibose attained an intra and inter-day accuracy and precision at 0.93 – 7.54% and 0.96 - 5.39%; 0.74 - 7.1 and 0.9 - 3.75% range respectively. the International Conference on Harmonisation of technical Requirements for Registration of Pharmaceuticals for Human Use guidelines were used as the bench mark for validating the method.

PHARMACOLOGY

No award this year.

IDMA ACG-SCITECH RESEARCH PAPER AWARD - 2018

In order to encourage R & D in the country, IDMA has instituted “Research Awards for the Best Original Research Papers” published in the “Indian Drugs” every year from the year 1981-82 and the Award for the Best Review Article was instituted in 2001. The Best Original Research Papers are evaluated in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

From this year, the Award will be known as ‘IDMA ACG-SCITECH RESEARCH PAPER AWARD’. The IDMA ACG-SCITECH RESEARCH PAPER AWARD will be in the form of a citation, plaque and a cash award of Rs. 5000/- in each discipline and the Best Review Article Award is in the form of a citation, plaque and special cash award of Rs. 7500/-.

These Awards are presented to the recipients during the IDMA Annual Day Celebrations every year.

REVIEW ARTICLE

Paper : Recent Advancements in Graphene Biosensors for the detection of Pathogens - A Review
Author(s) : Chaudhari A.* Jagdale P., Goswami P. and Kerawalla M. A. K.
Institute : Department of Pharmaceutical Science and Technology, Institute of Chemical Technology, Mumbai, Maharashtra, India
Volume : 55 (08)
Page nos. : 7-16
Abstract : Due to increasing rate of growth of pathogens throughout the world, there have been many epidemics in the recent past like Zika virus, Ebola virus and dengue fever. In many cases, the physicians were not able to treat the infected patients early enough to save their lives. One of the major reasons for this was because the physicians were only approached by the patients when some major symptoms developed.Or even if they approached the physician, the pathogen was detected very late due to the techniques used, that were slow, expensive, not very accurate and not simple. The techniques didn’t have a low detection limit as well, therefore it was almost impossible to detect the pathogen at a very early stage. To resolve these problems, extensive research is being carried out on graphene based biosensors. Graphene is a one atom thick single layer of sp2 hybridized carbons molecules. The extraordinary physical properties that it has, makes it an ideal material for the fabrication of biosensors. When the biosensors fabricated from graphene were tested, they delivered superior results and detected pathogens at a very low detection limits. In this review, we discuss the recent advancements within the field of graphene based sensors used primarily for the detection of pathogens. Further, the fabrication of the sensors for the detection of each pathogen has been discussed. The first section introduces graphene, its physiochemical properties. The second part focuses on the basic idea with which the graphene biosensor is designed. The third section discusses the detailed concept behind the detection of each pathogen covered in this review. Various methods for graphene modification have been discussed including functionalization using polymers and use of dopants with metal/metal oxide nanoparticles. And finally, the review concludes with the future applications and usefulness of graphene biosensors.

PHARMACEUTICAL CHEMISTRY

Title : Structure Elucidation and Biological Investigation of Inorganic Coordination Compounds Derived From Citraconic Anhydride and 5-Amino-1,3,4-Thiadiazole-2-Thiol Organic Moiety
Author(s) : Gautam S., Singh J., Kumar. A., Ravikant and Chandra S.*
Institute : Department of Chemistry, Zakir Husain Delhi College, University of Delhi, JLN Marg, New Delhi-110002, India
Volume : 55 (07)
Page nos. : 36-48
Abstract : The increasing clinical and microbiological resistance of fungi and bacteria enhanced discovery of several fungicidal and bactericidal drugs. Now it is necessary to discover novel drugs which can kill microorganisms but following the condition that these drugs should not be harmful for the host. In this research work we synthesized some novel transition metal complexes (inorganic coordination compounds) of ligand citraconicanhydride-bis(5-amino-1,3,4-thiadiazole-2-thiol) which act as antifungal and antibacterial agents. Ligand is synthesized by the condensation reaction of citraconicanhydride and 5-amino-1,3,4- thiadiazole-2-thiol, in ethanolic medium. Structure of ligand and complexes have been characterized by melting point, elemental analysis, 1H-NMR, mass, electronic spectra, molar conductance, magnetic moment, infra-red, uv-visible, electron paramagnetic resonance and molecular modeling study. Biological investigation of all synthesized compounds has been carried out by using pathogenic fungi C.albicans, C.krusei, C.parapsilosis and C.tropicalis and bacteria E. coli and S. aureus at different concentrations of compounds. Results of biological investigation by using well diffusion method show that metal complexes were more potent than free ligand. Results from biological investigation studies have also shown that complexation of metals with ligand serves to improve their activity.

NATURAL PRODUCT/ PHARMACOGNOSY/PHYTOCHEMISTRY

Title : In vitro Hypoglycemic Effects of Caesalpinia Bonducella and Myristica Fragrans Seed Extracts
Author(s) : Bhutkar M. A.*, Bhinge S. D., Randive D. S., Wadkar G. H., and Todkar S. S.
Institute : Rajarambapu College of Pharmacy, Kasegaon, Dist – Sangli – 415 404, Maharashtra, India
Volume : 55 (02)
Page nos. : 57-62
Abstract : The present investigation was undertaken to assess the hypoglycemic potential of Caesalpinia bonducella (C.bonducella) and Myristica fragrans (M.fragrans), employing various in vitro techniques. The extracts of seeds of C. bonducella and M. fragrans were studied for their effects on glucose adsorption capacity, in vitro glucose diffusion, in vitro amylolysis kinetics and glucose transport across the yeast cells. It was observed that the plant extracts under study adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. There were no significant (p≤0.05) differences between their adsorption capacities. The results of amylolysis kinetic experimental model revealed that the rate of glucose diffusion was found to be increased with time from 30 to 180 min and both the plant extracts demonstrated significant inhibitory effects on movement of glucose into external solution across dialysis membrane as compared to control. Also, the plant extracts promoted glucose uptake by the yeast cells. It was observed that the enhancement of glucose uptake was dependent on both the sample and glucose concentration. C. bonducella extract exhibited significantly higher (p≤0.05) activity than the extract of M. fragrans at all concentrations. The results of the study verified the hypoglycemic activity of the extracts of C. bonducella and M. fragrans. However, the observed effects exhibited by the extracts of seeds of C. bonducella and M. fragrans need to be confirmed by using different in vivo models and clinical trials for their effective utilization as therapeutic agents in better management of diabetes mellitus.

PHARMACEUTICS

Title : Box–Behnken Method To Optimize Lornoxicam Proniosomes: Preparation, In Vitro Characterization And Analgesic Activity
Author(s) : Vijaya Sri K.*, Sandhya D., Manchala M. and Dashamukhi R. S.
Institute : Malla Reddy College of Pharmacy, (Affiliated to Osmania university), Maissamma Guda, Secundrabad - 500 014, Telangana, India
Volume : 55(06)
Page nos. : 21-33
Abstract : The objective of present investigation was to develop and evaluation of proniosomes as the carrier of lornoxicam for topical delivery. lornoxicam-loaded proniosomes were prepared by coacervation phase separation method. The Box–Behnken design used in this study helped in identifying the factors affecting drug entrapment efficiency and drug diffusion. Proniosomes were evaluated for appearance, pH, viscosity, entrapment efficiency and in vitro drug diffusion studies. The optimized formulations were further evaluated to vesicle size, shape, zeta potential, percutaneous permeation and analgesic effect. The vesicles were found to be unilamellar, spherical in shape. The analgesic effect of lornoxicam proniosomal gel showed better therapeutic activity.

PHARMACEUTICAL ANALYSIS

Title : Simultaneous Determination and Quantitation of Metformin and Teneligliptin in human plasma by LC-ESI-MS/MS with an application to pharmacokinetic studies
Author(s) : Mandal P., Dan S., Ghosh B., Barma S., Bose R. and Pal T. K.*
Institute : Dept. of Pharm. Tech., Jadavpur University, Kolkata - 700 032, India , TAAB Biostudy Services, Kolkata, West Bengal - 700 069, India
Volume : 55 (04)
Page nos. : 28-38
Abstract : ‘Gliptins’ is the nickname given to a group of anti-diabetic medicines-DPP-4 inhibitors, such as sitagliptin, vildagliptin, sexagliptin, linagliptin, alogliptin and teneligliptin, which are used with metformin for combination therapy of type 2 diabetes mellitus. Advantages of this combined therapy are low risks of hypoglycemia and weight gain compared with other classes of anti-diabetic drugs. In the present study efforts, were made to develop and validate a bioanalytical method for simultaneous estimation of metformin and teneligliptin in human plasma by LC-MS/MS with an application to quantification of plasma samples obtained from the comparative pharmacokinetic studies on healthy human volunteers. The developed method for simultaneous determination and quantification of teneligliptin and metformin in human plasma was also validated as per the US-FDA guidelines. The validation parameters were found to be within the specified regulatory limits, hence the method acceptable. The present method had a short run time (3.5min) and easy extraction process. Therefore, developed method was found to be simple, specific, highly selective, sensitive and reproducible. This was applied for the analysis of volunteer plasma samples obtained from comparative pharmacokinetic study. On the basis of comparison of AUC0-t, the relative bioavailability of test preparation was found to be 97.64% and 91.37% for teneligliptin and metformin, with respect to that of the reference preparation.

PHARMACOLOGY

Title : Bioprospecting of marine halophyte Salicornia europaea L. And evaluation of its biological potential with special reference to anticancer activity
Author(s) : Samuel P.*, J. Vijaya kumar, Selvarathinam T., R. Deena dhayalan and K. Amirtharaj
Institute : Department of Biotechnology, Ayya Nadar Janaki Ammal College (Autonomous), Sivakasi - 626 123, Tamil Nadu, India
Volume : 55 (05)
Page nos. : 47-56
Abstract : The study was caried out with the intention to bring out the biological prospective nature of the marine halophyte Salicornia europaea L. The bioactive phytochemicals of the halophyte were extracted. The chemicals in the crude extract were evaluated for cytotoxic activity against MCF7 cell line by MTT assay. The marine halophyte a was collected, washed and chopped into 5cm long parts and shade dried for 20 – 25 days in a dark room. The dehydrated and bleached plant material was subjected to Soxhlet extraction. Two solvents, viz methanol and ethyl acetate, were used to prepare decoction. The extracts were dried using rotary vacuum evaporator. chemical screening by GC-MS unveiled the presence of 32 compounds in ethyl acetate and 29 in methanol. The 3D structures of the phytochemicals were retrieved from Pub Chem. cytotoxic study showed promising results. The IC50 values of the individual extracts were evaluated and ethyl acetate extract exhibit minimum IC50 value and it was estimated to be 97.9μg/mL wereas methanol extract exhibit a minimum IC50 value of 117.1μg/mL. Hence, the study concludes that S. europaea L. provides a promising source of lead compounds that could be exploited in near future to treat cancer.

IDMA RESEARCH PAPER AWARDS - 2016

In order to encourage R & D in the country, IDMA has instituted “Research Awards for the Best Original Research Papers” published in the “Indian Drugs” every year from the year 1981-82 and the Award for the Best Review Article was instituted in 2001. The Best Original Research Papers are evaluated in the following disciplines:

  • Pharmaceutical Chemistry
  • Natural Products
  • Pharmaceutics
  • Pharmaceutical Analysis
  • Pharmacology

The Best Research PaperAward is in the form of a citation and a cash award of `3000/- in each discipline and the Best Review Article Award is in the form of a citation and special cash award of `5000/-.

These Awards are presented to the recipients during the IDMA Annual Day Celebrations every year.

REVIEW ARTICLE

Paper : Nuclear medicine: An evolving medical specialty
Author(s) : B. Ranganathan
Institute : Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham University, Health Sciences Campus, Kochi - 682 041, Kerala, India
Volume : 53 (02)
Page nos. : 5–14
Abstract : Historically considered a subspecialty under radiology, nuclear medicine has grown in stature by leaps and bounds as it has managed to carve out a niche for itself within the realms of medical practice. Treated as an independent specialty in modern medicine, nuclear medicine concerns itself with the application of radioactive substances in the diagnosis and treatment of disease. It is deemed a worthy exercise to take a closer look at this discipline and understand its nuances as the numbers of both diagnostic and therapeutic nuclear medicine procedures performed steadily increase across the globe. This review, by shedding light on the unique field of nuclear medicine, is a concerted attempt to sensitize our pharmaceutical community to the discipline. Apart from opening up the world of radiopharmaceuticals and updating the status of nuclear medicine in developing nations, this piece attempts to trace the evolution of nuclear medicine and represents a tribute to Dr. Henry N. Wagner Jr., the doyen of American nuclear medicine, whom the author was fortunate enough to meet during his stint as a postdoctoral fellow in nuclear medicine at the Department of Radiology, The Johns Hopkins School of Medicine.

PHARMACEUTICAL CHEMISTRY

Paper : Biological Evaluation Of Novel A-Heteroaryl/Arylazo 2-Naphthol Analogs And The Transitional Metal Complexes Derived From 4-((2-Hydroxynaphthalen-1-Yl) Diazenyl)-1, 5-Dimethyl-2-Phenyl-1h-Pyrazol-3(2h)-One
Author(s) : Sahoo J.*, Sahoo S. and Paidesetty S. K.
Institute : Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Siksha‘O’Anusandhan University, Bhubaneswar – 751 003, Odisha, India
Volume : 53 (07)
Page nos. : 15-24
Abstract : Eight different aryl / heteroarylazo substituted 2-naphthol congeners and complexes of the composition [M (L) 2 (H2 O) 2 ]. x H2 O where L is deprotonated ligands such as 4g (ligH): 4-((2-hydroxynaphthalen-1- yl) diazenyl)-1, 5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one and M= Cu(II), Ni(II) and Co(II) have been synthesized. The structures of the synthesized compounds have been confirmed by different modern analytical techniques. The results of antimicrobial activities of the novel synthesized 2-naphthol congeners reveled that the 4-carboxyphenylazo substituted 2-naphthol analog 4h showed significant antibacterial activity against Escherichia coli, Salmonella enterica ser.typhi, Salmonella enterica typhimurium, Shigella flexneri, Pseudomonas aeruginosa, Vibrio cholera, Micrococcus luteus, Pectobacterium carotovorum, Bacillus subtilis and Staphylococcus aureus in comparison to standard. However the nickel complex of 4g showed significant antifungal activity against T. rubrum and C. glabrata. The novel synthesized azo molecules may be suggested for the establishment of new search for antimicrobial agents and to create an opportunity in new drug discovery and medicinal research.

NATURAL PRODUCTS

Paper : Comparative TLC and RP-HPLC fingerprinting Analysis of Three Sources of Mayurasikha: an Ayurvedic Drug
Author(s) : Telagari M., Hullatti K. K.*, Jalalpure S. S. and Peram M. R.
Institute : Department of Pharmacognosy, KLE University’s College of Pharmacy, Belagavi - 590 010, Karnataka, India
Volume : 53(04)
Page nos. : 47-53
Abstract : A simple TLC and precise RP-HPLC method was developed and validated to standardize the three ambiguous botanical sources of Mayurasikha with the help of two active markers (stigmasterol and oleanolic acid) compounds. TLC study of the three plant extracts showed spots with different Rf Values. In HPLC analysis, separation was through a Phenomenex Luna C18 column with mobile phase consisting of acetonitrile: water 87:13 (v/v) at 210 nm. The retention times of stigmasterol and oleanolic acid were about 2.36 and 7.53 min resp. and the developed method shown good sensitivity, significant linearity (r2 ≥0.9992) over the concentration ranges 2 ̶12 and 50 ̶ 500 µg/ml. The mean percentage recovery of stigmasterol was found to be 97.46 ̶100.31% and for oleanolic acid 99.32 ̶ 99.64%. Hence, the combination of TLC and RP-HPLC fingerprinting and quantitative analysis can be handy in identification and quality evaluation of the three ambiguous sources of Mayurasikha.

PHARMACEUTICS

Paper : Design and optimization of oral bioadhesive nanocurcumin delivery using novel hydrophilic carrier for cancer treatment: An alternative to parenteral chemotherapy
Author(s) : Kendre P. N. and Chaudhuri P. D.
Institute : Sanjivani College of Pharmaceutical Education and Research, Koparagaon, Dist. Ahmednagar – 423 603, Maharashtra
Volume : 53(08)
Page nos. : 24–36
Abstract : Present study involves the design and optimization of oral bioadhesive delivery system of curcumin. Solid dispersion of curcumin was developed using novel hydrophilic carrier, Gelucire® 50/13, by melt granulation technique. Based on HPMC K 100 LV(X1) and carbopol 934P (X2), bio-adhesive tablets containing curcumin solid dispersion was developed by direct compression, using central composite designs for two factors at three levels. Tablet formulation was optimized for t50%, Rel24h and bioadhesive strength. The drug release mechanism was found to be by fickian diffusion, approaching zero-order kinetics. Average plasma uptake of curcumin was found to be 0.289µg/mL as compared to plain curcumin tablet formulation. The results were found highly significant (p<0.05). The swelling matrices behavior over the time period studied showed that the gelling layer thickness increases continuously. From this study, it may be concluded that the oral controlled bioadhesive curcumin delivery may be an alternative to parenteral chemotherapy.

PHARMACEUTICAL ANALYSIS

Paper : Development And Validation Of A HPLC Method For Direct Estimation Of Ciclopirox Olamine In Ex Vivo Transungual Permeation Studies
Author(s) : Chouhan P. and Saini T. R.*
Institute : Industrial Pharmacy Research Lab, Department of Pharmacy, Shri G. S. Institute of Technology and Science, Vallabh Nagar, Indore - 452 003, (M.P.), India
Volume : 53(03)
Page nos. : 32-39
Abstract : A new hPLc method was developed for direct estimation of ciclopirox olamine in ex vivo transungual permeation samples by suppressing the chelating property of ciclopirox using disodium EDTA in mobile phase and endcapped hPLc column to reduce silanophilic interaction with drug. chromatographic separation was achieved on hypersil® Phenyl BDS column (250mm × 4.6mm, 5µm) using disodium EDTA in water (0.96 in 1000): acetonitrile: acetic acid (60:40:0.1, V/V/V) as mobile phase at a flow rate of 1mL/min, and estimated at 305nm. The method was validated for specificity, accuracy, precision, linearity, LOD, and LOQ. Ciclopirox was specifically quantified at 7.491min in the presence of forced degradation products. Linearity was established between 1-10µg/mL with a correlation coefficient of 0.999. The LOD and LOQ were 0.5 and 1µg/mL, respectively, which proved the ability of developed method to analyze ciclopirox in low concentration samples. The method could be successfully applicable in analyzing ex vivo transungual permeation study samples of ciclopirox olamine.

PHARMACOLOGY

Paper : In Vitro screening of Caesalpinia bonduc and Ficus benghalensis for inhibitory activity on Matrix Metalloproteinases (MMP-2 and MMP-9)
Author(s) : Bhanwase A. S.*, Alagawadi K. R. and Bhat K. G.
Institute : Department of Pharmaceutical Chemistry, KLEU’S College of Pharmacy Belgaum - 590 010, Karnataka, India
Volume : 53(04)
Page nos. : 58–62
Abstract : Proteolytic enzymes released by the host cells are associated with the tissue destruction in inflammatory disease condition. Matrix metalloproteinases (MMPs) have primary role in this process, as they degrade most of the extracellular matrix components. In the present study hydroalcoholic extract and fractions of Caesalpinia bonduc L. and Ficus benghalensis L. were screened for their in vitro inhibitory activity on MMP-2 and MMP-9. Screening was carried out by using gelatin zymography assay. Matrix metalloproteinases were extracted from the human tonsil tissue. The test samples were treated with the extracted MMPs and percentage inhibition was determined by using gelatin zymography. Hydroalcoholic extract of C. bonduc (CB-1) showed 99% inhibition of MMP-9 and 98% inhibition of MMP-2. However, hydroalcoholic extract of F. benghalensis (FB-1) showed 86.66% inhibition of MMP-9 and 89% inhibition of MMP-2. The inhibition of MMPs was decreased with increase in polarity of the solvents used for the successive fractionation in case of C. bonduc. However some polar and non-polar constituents might be responsible for inhibition of MMPs in case of F. benghalensis. MMP-2 appears to be more sensitive than MMP-9.
  1. IDMA RESEARCH PAPER AWARDS - 2015
  2. IDMA RESEARCH PAPER AWARDS - 2014
  3. IDMA RESEARCH PAPER AWARDS - 2013
  4. IDMA RESEARCH PAPER AWARDS - 2011

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