Day 2 :
Keynote Forum
Bhubaneswar Mandal
Associate Professor
Keynote: Novel and innovative strategies for peptide based drug design against Alzheimer’s disease
Time : 324143
Biography:
Bhubaneswar Mandal has completed his PhD from EPFL, Lausanne, Switzerland under the supervision of Professor Manfred Mutter. Then he earned prestigious MariernCurie Fellowship and worked as a Post-Doctoral Fellow with Professor Herbert Waldmann and Professor Hans-Dieter Arndt, Max-Planck Institute for Molecular Physiology,rnDortmund, Germany. Then he joined IIT Guwahati as an Assistant Professor. Presently, he is an Associate Professor there. He is working on novel strategy developmentrnfor drug design against amyloidoses and industrially useful reagent development for various organic transformations. He has published 28 papers in reputed internationalrnjournals.
Abstract:
Alzheimer’s Disease (AD), a common amyloidosis, has no cure yet. Pathological investigations revealed existence of numerousrnplaques in the Alzheimer’s patients’ brain composed of Amyloid-β (Aβ) peptides, derived from Amyloid Precursor Proteinsrn(APPs). Although the mechanism of plaque formation is unknown, AD is believed to be caused by the aggregation of misfoldedrnAβ peptides. β-breaker peptides have been developed that disrupt amyloid aggregates (plaques) in vitro as well as in vivo. We haverndeveloped two novel and innovative strategies for β-breaker peptide design. First one is based on the concept of β-sheet breaker α/βrnhybrid peptides (BSBHps); and the second one on the concept of β-Breaker Di-Peptides (BBDPs). We have demonstrated that suchrnwell designed peptides are capable of inhibition of amyloid formation of Aβ peptide. Also, they disrupt preformed toxic fibrillarrnaggregates into non toxic species in vitro. Such peptides may be useful for designing novel drugs against diverse amyloidoses includingrnAlzheimer’s disease, Parkinson’s disease and diabetes type II. Recent advancements in this direction of research will be discussed inrnthe Pharma Summit-2015.
- Pharmaceutics and Novel Drug Delivery Systems
Pharma Analytical Techniques and Instrumentation
Current Trends in Pharmacology
Pharmacognosy and Phytochemistry
GMP, GCP and Quality control
Session Introduction
Suhas Narayan Sakarkar
Smt. Sharadchandrika Suresh Patil College of Pharmacy, India
Title: Impact of zeta potential on pharmaceuticals
Biography:
Suhas Narayan Sakarkar holds MPharm and PhD degrees and has experience of nearly 18 years in industry and academics. He pursued PhD in Pharmacy in 2000. To his credit are many published papers in national and international journals as well granted patent. He attended many conferences of national and international repute. He has guided nearly 55 students in PG course and guiding 3 PhD students. He has been invited as Speaker in many conferences and chaired few sessions. He also is a Reviewer for three to four peer reviewed journals. The area of research is basic sciences in pharmacy, zeta potential, crystallization, using chamber permeation studies. Now, he is working as Professor and Principal in Smt. Sharadchandrika Suresh Patil College of Pharmacy, Chopda, Jalgaon.
Abstract:
Zeta potential is the surface charge of the particle, hence any interaction on the particle surface from external or internal environment leads to changes in surface properties and so the particle properties, which ultimately affects system stability. The zeta potential of the system depends on the adsorption and desorption properties of various drugs and excipients involved in the system. The stability of colloid or emulsion is dependent upon adsorption of ions (or polymers), chelating or complexing agents from the bulk of the suspending agent. Stability depends on the magnitude of zeta potential which depends on type on moiety, hydrocolloid, ionic/non-ionic surfactants. Further, the rate of change of zeta potential of the system with time is the major concern for determining the stability issues. Moreover, electrostatic interaction assists drug adsorption onto porous silicon nanoparticles, which can then be parenterally administered. Parenteral stability specifically depends on the composition of solution which is influenced by pH, ionic strength, types of buffers, protein concentration and the presence of various other additives. Systematic research in zeta potential led India to gain 1000$ research grant in seventies for cosmetic industries abroad. Investigations, for real time studies between dynamic environments of multicomponent systems by measuring zeta potential distributions of individual components and their mixtures is now on the recent trends. Hence, zeta potential is one of the essential tools for predicting the molecular interactions which assists in formulating more better formulations to meet the needs of global market.
Ramasare Prasad
Indian Institute of Technology Roorkee, India
Title: A novel anti-bacterial and antifungal protein from Euphorbia hirta
Biography:
Ramasare Prasad completed his Graduation in Chemistry (Hons) and Doctorate in Molecular Biology from Jawaharlal Nehru University, New Delhi, India, 1993. During year 1994, he joined Professor Wilmont, Parasite Molecular Biology Unit, at University of Georgia, Athens, Atlanta, USA, as Post-Doctoral Fellow. He joined as Faculty in Department of Biotechnology, Indian Institute of Technology Roorkee, India, since 1997 (Assistant Professor and Associate Professor) and has been Professor since 2012 onwards and also had been Head of Department from January 2012 to Feb 2015. Presently, he is the Professor and Leader of the of Molecular biology and Proteomics unit. He has published 55 papers in reputed journals and has been serving as an Editorial Board Member of repute.
Abstract:
In recent years, there has been sudden increase in bacterial and fungal infections mainly due to infection caused by opportunistic and drug-resistant pathogens particularly in immuno-compromised host and patients who has gone for transplant surgery. A therapeutic molecule with inherent properties of both antimicrobial as well as immuno-modulatory activity will be more effective in controlling and treating the antimicrobial infections in general and in immuno-compromised hosts in particular. As such, novel molecules will have dual action; the first is by killing the pathogen and secondly by boosting the immune system of the host. But finding such molecules is a difficult task. However, the observation that several antimicrobial proteins/peptides besides their antimicrobial action also found to have imuno-modulatory effects provide strong basis that such proteins do exist in nature. Keeping this fact in mind, an attempt has been made in the present study to search for such a novel protein from Euphorbia hirta a well-known medicinal plant. A novel protein with antimicrobial and immuno-modulatory activities has been isolated and purified from E. hirta leaves. Characterization of purified protein by different biochemical methods (SDS PAGE and HPLC) and biophysical methods (N-terminal sequencing, and mass spectrometric technique, revealed that it is 53 kDa monomeric proteins. It found to have potent antimicrobial and immuno-modulatory activities as confirmed by various standard assays, TEM and SEM and in vitro and in vivo studies. Attempt was made to identify the protein using bioinformatics tools. The results and finding will be presented and discuss.
Amit Sharma
I S F College of Pharmacy, India
Title: Formulation development and evaluation of colon targeted matrix tablets of Arteether
Biography:
Amit Sharma has completed his Master’s degree from Rajiv Gandhi University of Health Sciences, Karnataka and is doing PhD from Uttrakhand Technical University. He is the Head, Department of Pharmacy Practice, I S F College of Pharmacy, Moga. He has published more than 13 papers in reputed journals and is serving as an Editorial Board Member of repute.
Abstract:
Malaria is a serious endemic disease in many parts of the world, affecting 5% of the world’s population. About 40% of the world’s population is at stake of malaria. Arteether is a well known antimalarial mainly used in the treatment of cerebral malaria as well as chloroquine resistance malaria. But the main problems associated with arteether are its low solubility (≅17 μg/ml) and ≅40 % degradation in stomach. Due to these limitations, arteether is available only as intramuscular injection. The aim of present study is to formulate the colon targeted matrix tablets for improvement of colonic bioavailability of arteether by enhancing the solubility with cyclodextrin inclusion complex and preventing its degradation in stomach. Inclusion complexes of arteether with β-cyclodextrin in 1:1 molar ratio were prepared by techniques like co-evaporation and spray drying. The prepared complexes were characterized by using H-NMR, FTIR, differential scanning calorimetry, mass spectroscopy and PXRD. Complexation with β-CD in co-evaporation technique showed the maximum enhancement in solubility, i.e., 77.05 folds, in presence of PVP. This complex with better properties was further selected for preparation of colon targeted matrix tablets to prevent the degradation of arteether in stomach with improved solubility and better colonic bioavailability.
Gauri Patel
Karmic Lifesciences Consulting Services, India
Title: Role-play of GxP standards in growth of Indian pharmaceutical industry: Recent trends in GCP and GLP requirements
Biography:
Gauri Patel brings in over 10 years’ experience in Clinical Research. She is a Certified SQA [RQAP-GCP; RQAP-GLP] Professional. She has over 10 years of Quality Assurance experience, dealing with Quality Monitoring of procedures to ensure regulatory compliance for clinical, bio-analytical, and statistical phases of clinical trials and facing regulatory inspections. With a firm understanding of allover (GMP, GCP+GLP) applicable guidelines and regulations, her core strength areas are compliance assessment (monitoring; auditing; inspecting) and applied expertise (evaluation and advisory, remediation) towards achieving regulatory compliance. During later part of her career, she has been a Speaker at various forums and has conducted quite a few GxP workshops for industry. Prior to Karmic Lifesciences, she has worked in Quality Assurance for Cliantha Research Ltd., and additionally, was instrumental in pioneering and establishing training systems for the organization.
Abstract:
The Indian pharmaceutical industry has achieved an eminent global position in pharma sector and has been witnessing phenomenal growth in recent years. It is well known that India is emerging as a world leader in generic pharmaceuticals production, supplying 20% of the global market for generic medicines. Indian pharmaceutical sector accounts for about 2.4 per cent of the global pharmaceutical industry and is expected to expand at a CAGR of 15.92 per cent to US$ 55 billion by 2020 from US$ 20 billion in 2015. The Indian pharmaceutical industry is one of the most attractive investment destinations in the world, with ever increasing returns, lowering risks and anticipated multifold growth. It is estimated that around 40 per cent of the generic drugs in the US come from India. Given the demanding nature of inspections, recent enforcement actions and the public scrutiny that each warning letter is subjected to, there can be no compromise with the quality requirements or regulatory necessities. Special attributes are the data integrity issues that have become a recurrent theme in the FDA’s inspection of Indian facilities. The challenge to the pharmaceutical industry is, therefore, to develop quality systems, compatible with GxP principles, that not only cover formal quality items but also ensure good scientific and technical performance. The pharmaceutical industry is one of the most regulated activity sectors. The regulation includes specific quality systems such as Good Laboratory Practice (GLP), Good Clinical Practice (GCP) and Good Manufacture Practices (GMP). Revisiting the regulations (GCP & GLP) with focus on recent updates and their causes will definitely help pharmaceutical industry in achieving goal of delivering better medications globally.
Divya Vohora
Jamia Hamdard, India
Title: Anti-epileptic drugs induced secondary osteoporosis: Multi-factorial mechanisms and current status
Biography:
Divya Vohora, MPharm, PhD, is currently Professor for Department of Pharmacology and in-charge of Pharmaceutical Medicine program, Faculty of Pharmacy and Assistant Dean Students Welfare at Hamdard University, New Delhi. She has more than 15 years of teaching/research experience with 82 publications (including 2 books, 5 book chapters and 75 research papers in reputed national and international journals). She is a member of many learned societies, professional bodies, expert committees and on Editorial Board and reviewer for more than 30 reputed journals.
Abstract:
Long term association exists between antiepileptic drug (AED) therapy and bone diseases. There is a lattice of the pathophysiological mechanisms of AED-induced bone disease that can be either independent or dependent on each other. Hepatic induction of cytochrome P450 leading to increased metabolism of vitamin D is the principle mechanism reported. Others include secondary hyperparathyroidism, calcitonin or vitamin K deficiency, deprived estrogen levels etc. A better understanding of these mechanisms can aid clinicians in identifying and monitoring vulnerable patients and in defining the optimal therapy for all affected patients. Bisphosphonates, a standard form of treatment for post-menopausal osteoporosis, are potent inhibitors of bone resorption and given the findings of increased bone resorption associated with AEDs, may represent an effective treatment for bone disease in patients receiving AEDs. Similarly, raloxifene, a selective estrogen receptor modulator, may be a potential therapeutic option in view of the fact that AEDs causes estrogen deficiency. Thus, studies were designed to investigate the effect of anti-osteoporotic therapies, in comparison with CVD supplementation, on AEDs-induced bony alterations in mice. Further, the effect of these therapies on seizures and on the antiepileptic efficacy of AEDs was investigated. Our results suggest a potential for bisphosphonates and raloxifene in the management of PHT and/or SVP-induced bone disease and thus merits further investigation to provide an evidenced-based approach for their use. Further, with the newer AEDs gaining importance, our future experiments would focus on comparing them with the conventional AEDs and to examine their impact on multiple aspects of bone health.
Om Prakash
R&D Center of AVA Cholayil Health Care Pvt. Ltd, India
Title: Future innovation needed drug discovery in the next decade
Biography:
Om Prakash is the Deputy General Manager-NPD at R&D Center of AVA Cholayil Health Care Pvt. Ltd. Chennai. He has published more than 20 papers in reputed journals and scientific conferences and also worked as Research Scientist at R&D Center of The Himalaya Drug Company, Bangalore. He is having more than 11 year experience in developing safe, clinically proven, efficacious new products.
Abstract:
It is not surprising that throughout history man has searched for remedies to fight against disease. Historically speaking, man has explored nature to satisfy two major needs – food and herbs for alleviating pain and suffering. Ancient civilizations had comprehensive treatises where herbs or mixtures of them represented the ‘‘corpus therapeuticum’’ to alleviate and treat disease. The challenge of discovering novel therapeutics is not getting any easier. One might imagine that with advances in technology, would come concomitant reduction in the discovery process. I know that I really don’t need to state that this is far from the truth. With significant uncertainty characterized by higher R&D costs, depleted pipelines and financial restrictions, the pharmaceutical industry can no longer function on its old model of closed innovation, stricter regulatory environments and the overall current economic downturn. This makes demands of all pharmaceutical companies to find better ways to increase their output of new drugs, through innovation, to both treat patients and meet their shareholders’ expectations. Pharmaceutical companies must find a better way to increase their output of truly new drugs for the benefit of patients and for their business survival. Here, we shall be elucidating a general perspective from within pharmaceutical research as it pertains to research advances in chemistry, biology, pharmacology, pharmacokinetics and toxicology that, if well integrated, stands to put the industry on a productive path. We should understand a new models like open innovation and ‘innovation ASAP’ (iASAP; asking powerful questions, seeking the outliers, accepting defeat and populating astutely).
Chintankumar J Tank
Dr Subhash Technical Campus, India
Title: Transdermal drug delivery of Fluvastatin Sodium: Effect of permeation enhancers and pressure sensitive adhesive
Biography:
Chintankumar J Tank is BPharm, MPharm (Pharmaceutics) and PhD. He is presently working as a Head, Faculty of Pharmacy and Associate Professor at Dr Subhash Technical Campus, Junagadh. He has 8 years of teaching experience. He has an experience of teaching various subjects of pharmacy. His area of interest is Transdermal Drug Delivery System, Niosomes & Nanoparticles. He has authored the book on the topics of “Pharmaceutical Microbiology and Biotechnology Iâ€. He has attended many seminars and conferences in national and international repute and also published papers in well reputed national & international journals. Recently, he has fetched the grant from GUJCOST to organize national level symposium.
Abstract:
The study was aimed to investigate transdermal permeation of Fluvastatin Sodium (FVS) from monolithic matrix system of polyacrylate based pressure sensitive adhesive. Effect of concentration of Durotak 87-9301 (DT 9301) on adhesion characteristics and selection of suitable penetration enhancer were also points of interests in present work. Different concentrations of DT 9301 & Eudragit RL 100 (E RL 100) were used as different PSA compositions. The transdermal patches were prepared by solvent casting method. Oleic acid, oleyl alcohol, transcutol P and isopropyl myristate were evaluated as permeation enhancer. The prepared formulations were evaluated for in vitro drug release study and physicochemical quality attributes. Combination of oleic acid and DT 9301 has shown maximum effect on drug release in comparison with other permeation enhancers studied. PSA composition with 46.5% w/w of DT 9301 & 26.5% w/w of E RL 100 was found to be optimum for targeted flux of FVS. Pharmacokinetic model fittings on optimized formulations indicated diffusion controlled drug release pattern based on Higuchi’s model. Skin irritation study indicated no sign of irritation for selected formulation, revealed applicability of the patch for one day treatment. Optimized formulation provides its possibility to formulate in the area of 5.42 cm2 based on the flux of F9 to attain and maintain input rate of FVS over a period of 24 h. It was possible to use E RL 100 with DT 9301 to make blend of polymers in order to achieve high release of fluvastatin sodium and sufficient self-adhesiveness of matrix patch.
Nura Suleiman Gwaram
Umaru Musa Yar’adua University, Nigeria
Title: Protein-ligand inhibition towards acetylcholinesterase and cyclooxygenase-2 leading to Anti- Alzheimer’s disease
Biography:
Nura Suleiman Gwaram has completed his PhD from University of Malaya and Postdoctoral studies from High Impact Research (HIR), University of Malaya dated March 2014–November 2014. He is currently a Lecturer at Department of Chemistry, Umaru Musa Yar’adua University. He has published more than 35 papers in reputed journals and has been serving as an Examination Officer for Department of Pure and Industrial Chemistry Faculty of Natural and Applied Sciences, Umaru Musa Yar’adua University, P.M.B. 2218 Katsina, Nigeria.
Abstract:
The common feature of Alzheimer’s Disease (AD) is inflammation in the brain which can either be the cause of the disease or an effect of the disease. In this work, molecular docking of some compounds was conducted to study their protein-ligand binding interactions towards acetylcholinesterase and cyclooxygenase-2 inhibition. Understanding of cholinesterase structure and their inhibition is important for effective drug design and treatment of AD. However, Cyclooxygenase-2 (COX-2) inhibitors have been associated with the reduced risk of AD. The molecular docking simulation of the complex involved in protein-ligand interactions formed showed ligands docked well in the active-site gorge, with the monohydroxyphenyl and dihydroxyphenyl moieties interacting with residues in the PAS and ABP, respectively. A careful observation of the interactions at the PAS showed the presence of a hydrogen bond between the 2-hydroxyl groups. In silico molecular modelling revealed that the compounds may position themselves in the enzyme’s active-site gorge interacting with residues in the peripheral anionic subsite (PAS) and acyl binding pocket (ABP).
Satyendra Deka
Assam down town University, India
Title: Synthesis and characterization of some novel isoxazolines for In-vitro antiplatelet aggregation activity
Biography:
Mr. Satyendra Deka has completed his M. Pharm at the age of 30 years from Rajiv Gandhi University of Health Sciences, Karnataka and awarded Gold Medal for topping in the final M. Pharm and securing 10th Rank of the University. Now he is pursuing Ph.D. from Srimanta Sankaradeva University of Health Sciences, Assam. He is the Assistant Professor of Institute of Pharmacy, Assam down town University, Assam. He has published more than 18 papers in reputed journals and serving as a member of different organization.
Abstract:
A large number of medicinal compounds which have been discovered belong to a major class of heterocycles containing Nitrogen and Sulphur. Isoxazolines are five-member heterocyclic compound containing nitrogen and oxygen. Organic compounds containing 2-isoxazolines forms a significant group of drugs which exhibit an array of biological activities ranging from antibacterial, antifungal, diuretic, analgesic, anti-inflammatory, anti-tubercular, antitumor, anti pyretic, CNS depressants and so on. In view of the above observations we have synthesized 2-isoxazolines with various substitutions at fifth position. The starting material para-methoxy acetanilide (GSM) was synthesized by refluxing para anisidine with acetic anhydride for 30-45 min. GSM (01- 13) was synthesized by reacting GSM with various substituted aromatic benzaldehyde (01-13). The title compounds GSM (01a-13a) was synthesized by reacting GSM (01-13) with hydroxylamine hydrochloride. The newly synthesized compounds were characterized by MP, TLC, UV, IR, NMR and Mass spectra. The title compounds were screened for their in-vitro antiplatelet aggregating activity using Heparin as standard at concentration of 30, 50, 80 and 100μgm/ml. In conclusion, from the in-vitro antiplatelet activity results, it was observed that electron withdrawing groups on the aldehydic phenyl ring of the compounds influenced the activity. Among all the compounds tested, compounds GSM-03a, GSM-07a, GSM-12a with 2’-nitro, 2’-chloro, 4’-chloro substitution and GSM-11a with -H showed more significant activity. Compounds GSM-02a, GSM- 06a, GSM-08a with 3-nitro, 2-OH, 4-OH respectively showed mild to moderate activity compared to standard Heparin. Remaining compounds did not show any activity as compared to that of standard.