Scientific Program

Conference Series Ltd invites all the participants across the globe to attend Pharmaceutical Summit and Expo New Delhi, India.

Day 3 :

  • Track 1: Pharmaceutics and Novel Drug Delivery Systems
    Track 2: Pharma Analytical Techniques and Instrumentation
    Track 4: Nanotechnology
    Track 12: Medicinal Chemistry and Drug Discovery
Location: Radisson Blu Hotel New Delhi Paschim Vihar
Speaker
Biography:

Magdy El-Salhy is Professor of Gastroenterology and Hepatology at Bergen University, and consultant gastroenterologist at Stord Hospital, Norway. He is a member of the Editorial Boards of 10 international journals, and is associated editor-in chief of World Journal of Gastroenterology. Furthermore, he is on the referee list of a large number of international journals. He has evaluated grant applications for national and international research foundations. El-Salhy has also attended and contributed to several national and international meetings as invited speaker, or chairman. He authored over 200 publications, which include original articles, invited reviews, book chapters, and books. His work has been cited in 4105 scientific articles. In 2013 -2015, four of his highly cited papers are in the top 1% of world publications. His research field for the last 40 years has been the neuroendocrine system of the gut, from basic science to clinical applications.

Abstract:

The diagnosis of irritable bowel syndrome (IBS) in clinical practice is a diagnosis of exclusion, whereby diagnostic tests and invasive investigations are conducted to exclude other gastrointestinal diseases. Attempts have been made to achieve a positive diagnosis based on symptoms assessment such as the Rome III criteria. However, symptom-based diagnosis is not widely used in everyday clinical practice. Searches for biomarkers for the diagnosis of IBS that reflect pathological states have not yielded any useful candidates. The duodenum contains the largest number of endocrine cells in the gastrointestinal tract, followed by the rectum. The densities of four of the five duodenal endocrine cell types have been found to be reduced in patients with sporadic (non-specific) IBS. Chromogranin A (CgA) is a common marker for gastrointestinal endocrine cells. It has been thought that the cell density of CgA the duodenal endocrine cells, can be used as a biomarker for the diagnosis of IBS. Receiver operator characteristic (ROC) revealed areas under the ROC curve (ROCAUC) values of 0.97, and positive likelihood (+LH) and negative LR(-LH) of 18,5 and 0,14, respectively. This biomarker is simple, inexpensive, and easy to perform, and does not require sophisticated equipment or considerable experience. The density of PYY cells is reduced in the rectum of sporadic IBS patients, whereas that of somatostatin is increased. As biomarkers for the diagnosis of IBS, rectal PYY has a ROCAUC values of 0.96 and +LH and –LH 7.56 and 0.18, respectively. The corresponding values for somatostatin are 0.93, 7.20, and 0.23. These biomarkers erform well in differentiating IBS from health and are better than Rome III criteria, which has +LH and –LH of 3.53 and 0.39, respectively. Moreover, these biomarkers reflect an anatomical lesions occurring in the gastrointestinal tract of IBS patients, namely gastrointestinal endocrine cells.

Speaker
Biography:

Abstract:

Functional and smart polymers are currently playing a significant role in formulations of controlled drug delivery systems due to their responsive behavior towards environmental stimuli. The delivery systems must be non-toxic, non-immunogenic and must be having optimum trapping and release properties for an active agent. To be more effective and economical the controlled devices should be able to release active agent in a control and site specific manner The physical and chemical properties of the polymers provide opportunities to design therapeutic devices for various applications. Though various delivery systems based on electrical, mechanical and viral systems have been fabricated with great successes but these delivery systems have shown poor transfection efficiency and found to be immunogenic; hence delivery systems based on functional polymers such as poly(ethylene glycol) and dendric poly(amidoamine) found to be of great significance. The delivery systems using natural and biodegradable polymers such as chitosan, pectin and polysaccharides proved to be more are acceptable due to their biocompatibility and biodegradability in physiological fluids in comparison to synthetic polymer systems. Considering the importance of natural polymers, the pH and ion responsive drug delivery systems have been designed using different forms and derivatives of the chitosan. These delivery systems have been tested for efficiency of loading and delivery of active agents as a function of solution pH and ionic strength of the medium. The naturally occurring chitosan has provided enormous opportunities for controlling its properties to fabricate control site specific delivery systems. The degree of deacetylation in chitosan proved to be significant in controlling its stimuli responsive properties for drug delivery systems. The nano sized chitosan delivery systems found to be more therapeutic in comparison to macro and micro sized delivery devices for controlled and sustained delivery of the active agents. The role of various parameters would be discussed and highlighted in this talk.

Speaker
Biography:

Dr. Dafny received his M.S. and Ph.D. degrees from Hadassah Medical School in Jerusalem in 1965 and 1969, respectively followed by post-docs at Caltech, UCLA, and Columbia. He is currently a professor of Neurobiology at the University of Texas Medical School at Houston.

Abstract:

Methylphenidate (MPD) is one of the most widely prescribed psychostimulants for the treatment of attention deficit hyperactive disorder (ADHD) in children and adults. MPD binds to presynaptic catecholamine transporters in the CNS and prevents reuptake of norepinephrine and dopamine from the synaptic cleft. Unlike the psychostimulants cocaine and amphetamine, MPD does not exhibit direct actions on the serotonin transporter. Studies investigating MPD tend to focus on its effects on the CNS dopamine circuit, however there is evidence suggesting that MPD affects the serotonergic system as well. This study aimed to investigate the role of the dorsal raphe, a major source of serotonergic innervation in the mammalian brain, in the response to acute and chronic MPD exposure. The hypothesis of the study is 1) the dorsal raphe (DR) participates in MPD action, 2) the same chronic MPD dose in some adolescent animals will elicit behavioral sensitization and in others behavioral tolerance and 3) the DR neuronal activity recorded from adolescent animals expressing behavioral sensitization to chronic MPD will have a significantly different response to MPD exposure than those DR neurons recorded from animals expressing behavioral tolerance to chronic MPD. Freely behaving animals previously implanted bilaterally with permanent electrodes were used. Behavioral and DR electrophysiological activity were concomitantly recorded following acute and chronic MPD exposure using an open field assay and a wireless recording system over 10 experimental days. Four groups of animals were used: one control group (saline) and three experimental groups treated with 0.6, 2.5, and 10.0 mg/kg MPD respectively. The animals received daily MPD or saline injections on experimental days 1-6, followed by 3 washout days and MPD rechallenge dose on experimental day (ED)10. The same chronic dose of MPD resulted in either behavioral sensitization or tolerance. DR neurons responded to acute MPD in a dose dependent manner. Neuronal activity recorded from the DR units of rats expressing behavioral sensitization to chronic MPD exposure exhibited a significantly (p < .05) different response to MPD rechallenge on ED10 compared to the DR neuronal activity recorded from animals that expressed behavioral tolerance to chronic MPD. This correlation between behavioral response and DR neuronal activity following chronic MPD exposure indicates that the DR is involved at least in part in the acute effects of MPD as well as the chronic effects of MPD (expression of sensitization and tolerance) in adolescent rats. The study confirms our hypothesis.

Rajendra Sharma

Himalayan Institute of Medical Sciences, India

Title: Newer drug delivery system - Pros & Cons
Speaker
Biography:

Abstract:

Drug delivery is the method or process of administering an active pharmaceutical ingredient [API] to achieve a therapeutic effect in humans and animals. Due to drawbacks associated with conventional therapies i.e. fluctuation in plasma concentration, decrease concentration of drug at site of action, increase cost of therapy and decrease patient compliance, new drug delivery systems [NDDS] to optimize therapy with established drug are required. Drug delivery technologies are patent protected formulation technologies that modifiy drug release profile, pharmacokinetic parameters for improving product efficacy and safety as well as patient convenience and compliance. Various drug delivery techiniques include oral, ohphthalmic, transdermal, pulmonary, intravaginal/intravesical, implant, prodrug, gene therapy, targeted drug delivey systems etc. NDDS are therefore help increase therapeutic efficacy, patient compliance and decrease adverse drug reaction as well. However NDDS has its own limitation and drawbacks i.e. NDDS are costly. Talking about particulate carrier system i.e. nano-particle, liposomes etc, particulate nano-carriers have been praised for their advantageous drug delivery properties in the lung, such as avoidance of macrophage clearance mechanisms and long residence times, however instilled non-biodegradable polystyrene nano-spheres with small diameters and thus large surface areas have been shown to induce pulmonary inflammation. Similarly in polymeric prodrug system, prodrug are used which get bio transformed in the drug within the body hence the use of prodrug as drug depends upon the body’s ability to release the drug in the body [inter individual variations in drug response]. It may be concluded that drug delivery therapeutic system is defined as drug containing preparation or device that release one/more drug at predetermined rate over a fixed period of time either systemically or at specified site (target organ) and with the vast database of different studies the science of site specific or targeted delivery of these drugs will become wiser and manifestation of these strategies in clinical practice seems possible in near future.

Speaker
Biography:

Dr Nasim has completed his PhD from Patna University and postdoctoral studies from IIT Delhi, Supercomputing facility for bioinformatics and computational biology (SCFBIO-IITD). He is the assistant professor in chemistry at Jamia Millia Islamia (Central University). He is working in the field of Drug design and focussing on the development of antimalarial and anti-neurodegenerative agents.

Abstract:

Malaria is a leading cause of human deaths affected by parasitic infection in tropical and subtropical reasons. Out of the four plasmodium species responsible for this disease in human Plasmodium falciparum is the most deadly. Due to the widespread resistance of the current antimalarial drugs, intense research efforts are focused on identification of new potent antimalarials. We report here, a structure based drug discovery strategy for design and synthesis of a series of potent and novel triazine based antimalarials. The X-ray structure of Plasmodium falciparum phosphoethanolamine methyltransferase (PfPMT) is used as a target as it is unique to the parasite. Trisubstituted triazine and its anlaogs are produced by an inexpensive three to four step synthesis giving excellent yields. Parasite growth inhibition assays further confirmed the activity of the molecules to be in 5 to 0.8 µM range showing selectivity towards the parasite over mammalian cells. Molecular dynamics simulations on the PfPMT-inhibitor complex shed light on the inhibition mechanism for further optimization of the lead compounds.

Speaker
Biography:

Dr. Bhubaneswar Mandal has completed his PhD from EPFL, Lausanne, Switzerland under the supervision of Prof. Manfred Mutter. Then he earned prestigious Marie Curie Fellowship and worked as a post-doctoral fellow with Prof. Herbert Waldmann and Prof. Hans-Dieter Arndt, Max-Planck Institute for Molecular Physiology, Dortmund, Germany. Then he joined IIT Guwahati as an assistant professor. Presently he is an associate professor there. He is working on novel strategy development for drug design against amyloidoses and industrially useful reagent development for various organic transformations. He has published 28 papers in reputed international journals.

Abstract:

Alzheimer’s disease (AD), a common amyloidosis, has no cure yet. Pathological investigations revealed existence of numerous plaques in the Alzheimer’s patients’ brain composed of Amyloid-β (Aβ) peptides, derived from amyloid precursor proteins (APPs). Although the mechanism of plaque formation is unknown, AD is believed to be caused by the aggregation of misfolded Aβ peptides. β-Breaker peptides have been developed that disrupt amyloid aggregates (plaques) in vitro as well as in vivo. We have developed two novel and innovative strategies for β-breaker peptide design. First one is based on the concept of β-sheet breaker α/β hybrid peptides (BSBHps, left panel of the Figure) and the second one on the concept of β-breaker di-peptides (BBDPs, right panel of the Figure). We have demonstrated that such well designed peptides are capable of inhibition of amyloid formation of Aβ peptide, also they disrupt preformed toxic fibrillar aggregates into non toxic species in vitro. Such peptides may be useful for designing novel drugs against diverse amyloidoses including Alzheimer’s disease, Parkinson’s disease and diabetes type II. Recent advancements in this direction of research will be discussed in the Pharma Summit-2015.

Gannu Praveen Kumar

Sahasra Institute of Pharmaceutical Sciences, India

Title: The Global Strategies and Innovations in the Pharmaceutical Industry
Speaker
Biography:

Gannu Praveen Kumar, Professor and Principal in Sahasra Institute of Pharmaceutical Sciences since April 2014, graduated from H.K.E’s society college of Pharmacy, Gulbarga University in 1997, post graduation from BITS, Pilani in 1999 and PhD from UCPSC, Kakatiya University in 2009. He has published in both National and International journals and compiled few chapters for text books. He received Gem of India award in the year 1999. He was selected as a best academician in 2001 and 2011. He is an advisor for few pharmaceutical companies. He visited foreign countries like London, Dubai, Singapore, Malaysia and Spain as invited speaker.

Abstract:

Continuous innovation is one of the pharmaceutical industry’s most defining characteristics. New medications can be crucial for maintaining the quality of human life, and may even affect its duration. The global pharmaceutical market is expected to reach $1.1 trillion by 2015. Pharmaceutical innovation is marching towards an orderly, predictable process. It follows a technology push model dependent on a meandering path of scientific breakthroughs with uneven timing and hard to foresee outcomes. Technological competency, decades of rigorous research, and profound understanding of unmet customer needs, while necessary, may prove insufficient for market success as the critical decision for commercialization remains outside the firm. Drug innovation as a business process requires savvy strategic, organizational and managerial decisions. It is already enjoying intensive research coverage, giving rise to abundant but relatively dispersed knowledge of the mechanisms driving drug discovery and development. A comprehensive overview of the process of drug innovation from a business and academic perspective is explained. The evolving organizational forms and models for collaboration, summarize significant empirical regularities, and highlight differences in market positions related to firms’ strategic orientation, innovation emphasis, attitudes to risk, and specialized resources are highlighted. As a guide to future research, critical drivers and modes for drug innovation are systematized in a unifying framework of characteristics and process decisions, and multiple areas in need of further scrutiny, analysis, and optimization are suggested. Because of its rich potential and high significance, research on drug innovation seems poised to gain increasing momentum in the years to come.

Speaker
Biography:

Belayneh Kefale has completed his B.pharm at the age of 22 years from Wollo University, Ethiopia and Gobezie Temesgenhas completed his B.pharm at the age of 23 years from Jimma University and his MSc in clinical pharmacy in Jimma University School of Medicine. Belayneh Kefale ia a research coordinator for pharmacy department and he has published more than 30 papers in reputed journals and serving as an editorial board member of repute. Gobezie Temesgen is a unit leader for clinical pharmacy in Ambo University and also has 35 papers published in reputed journals.

Abstract:

Background: The term diabetes mellitus describes metabolic disorders of multiple etiologies characterized by hyperglycemia with disturbances of carbohydrates, fat and protein metabolism resulting from defects in insulin secretion, insulin action or both. Anti-diabetic medications are integral for glycemic control in diabetes. Non adherence to drugs can alter blood glucose levels, resulting in complications. The objective of this study was to determine the magnitude of non-adherence and its contributing factors among diabetic patients attending the diabetic clinic in Adama hospital. Methods: This descriptive cross-sectional study was carried out among patients with diabetes mellitus attending the diabetes mellitus clinic of Adama referral hospital. Every other patient was selected and data regarding their medication adherence was collected using a structured interview. Data analysis was carried out using SPSS-16. Result: The response rate from this study was 98.3%. A total of 270 patients were interviewed; 51.5% were males. A total of 68.1% of the patients included in the study were married. 14% were younger than 40 years of age, 50% were between 40 and 60 years of age. 21.8% of the participants ascribed their non-adherence to forgetting to take their medications. Patients with duration of diabetes ≤ 5 years (82.07%) were more compliant to their medication than those with >5 years 60.8%, which was found to be statistically significant (P=0.003). Insulin 47% and glibenclamide plus metformine 43.7% were the most commonly prescribed mono and combination therapies respectively. Common co morbid conditions include, Hypertension 148(54.82%), Visual impairment 89(32.96%). The proportion of male patients adherent to their anti-diabetic medications was found to be lower 69.78% compared to the female patients (74.81%), but the difference was not statistically significant (p>0.05). Conclusion: Most diabetic patients are currently being managed with the most effective available drugs. However as the result from this study indicates the desired blood sugar level could not be controlled and maintained adequately. This was because of poor adherence with the prescribed drug regimen and poor knowledge and practice of successful self management.

Speaker
Biography:

Nura Suleiman Gwaram has completed his PhD at the age of 32 years 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:

Acetylcholinesterase inhibitors with antioxidant activities are considered potential treatments for Alzheimer’s disease (AD). Laboratory findings have shown that oxidative stress may play an important role to the pathogenesis of AD. Mainly from in vitro studies, phenolic componds have been reported to have antioxidant. Therefore, the risk of AD disease might be decreased by intake of antioxidants that neutralize the unfavorable effects of oxidative stress. A number of morpholine derivatives have been described as analgesics and local anesthetics. Understanding of cholinesterase structure and their inhibition is important for effective drug design and treatment of AD. Condensation reaction between 4-(2-aminoethyl)morpholine and 4-(2-aminopropyl)morpholine with 2,4-dihydroxybenzaldehyde or 2,4-dihydroxyacetophenone yields the corresponding ligands. In the crystal structures, one oxygen atom of hydroxyl group connect the adjacent hydrogen aton of the amine group via O1…H1 interactions to form a six membered ring and morpholine moety adopt a chair transformation. Molecular docking is done by using Autodock 4.2, setting at 160x180x176 Gridbox, centered at 115.955, 105.139, -139.962 with 0.375Å spacing. •Ligand is docked well in the hydrophobic pocket of TRP86, TYR119, GLY120, GLY121, TYR124, SER125, GLY126, ALA127, LEU130, TYR133, GLU202, SER203, TYR337, PHE338, HIS447 and GLY448. There are 3 intermolecular hydrogen bonds between: (1)TYR124:OH - LIGAND:O18 (distance: 2.91336 Å) (2) LIGAND:H19 - TYR124:OH (distance: 2.05211 Å) (3) LIGAND:H20 - GLN71:OE1 (distance: 1.92168 Å). In silico molecular modelling revealed that the compounds may positioned themselves in the enzyme’s active-site gorge, interacting with residues in the peripheral anionic subsite (PAS) and acyl binding pocket (ABP).

Speaker
Biography:

Abstract:

The purpose of this study was to produce oral controlled release organogel of methimazole to lengthen drug retention time. This dosage form is associated with many advantages like solves problems of frequent dosing and patient incompliance. Preformulation studies and drug excipient studies were carried out for methimazole and excipient. Controlled release organogel were prepared by heating method. One factor response surface methodology was applied to formulate formulations (F1-F14) with different concentration of 12- Hydroxy stearic acid and different rate of cooling (Gradual cooling and rapid cooling) at five levels using quadratic model. Prepared formulations were subjected to various evaluation tests. The optimized batch was derived statically by using Design expert 8.0. Controlled release organogel formulated using optimized formula was then evaluated for various parameters. Results of preformulation studies were observed between methimazole and excipients by Differential scanning calorimetry and Fourier transfer infrared spectroscopy. The drug release profile was 89.00% at 10hr. and 98.02% at 12hr. The results showed significant bias between predicted and actual response for the optimized formula. The result of the present investigation suggested that organogel prepared by using 12-Hydroxy stearic acid as an organogelator and soybean oil as base can be clearly useful for controlled release formulation to provide alternative in delivery of methimazole.

Speaker
Biography:

Dr. Sidharth Mehan, (Ph.D, M.Pharm, CFN) is an Associate Professor of Pharmacology at Rajendra Institute of Technology & Sciences, Sirsa, Haryana, India. He is a editorial board member and reviewer of various Pharmaceutical and Therapeutic Committee nationally and internationally like ARDSI (Alzheimer’s and Related Disorders Society of India) of various national and international journals and magazines. He is young neuropharmacologist, published various research, review and conference papers extensively and lectured worldwide. He did major contributions to describe the course of neurodegenerative disorders liken Alzheimer’s, Huntington’s, Parkinson’s and the effect of medical conditions on the course of neuropathy pain, renovascular diseases as well as to explore the novel therapeutic strategies and phytochemicals in the development and drug discovery in the field of molecular pharmacology.

Abstract:

Various extracellular signals regulates intracellular functions like neuron excitability, neurotransmitter biosynthesis and release, neuronal growth, differentiation, neurite growth, synaptic plasticity and cognition through secondary messenger’s Cyclic AMP (cAMP). Secondary messengers subsequently activate target enzymes Protein kinase A (PKA) & Protein kinase G (PKG) that activate cyclic AMP responsive element binding protein (CREB) which regulate synaptic plasticity, learning and memory, restore energy levels, reduce excitotoxic damage prevent Aβ toxicity inhibit apoptotic and necrotic cell death and also increase synaptic strength. Forskolin activates the enzyme adenylyl cyclase and increases intracellular levels of cAMP. cAMP is an important second messenger necessary for the proper biological response of cells to hormones and other extracellular signals. It is required for cell communication in the hypothalamus/pituitary gland axis and for the feedback control of hormones. Cyclic AMP acts by activating cAMP-sensitive pathways such as protein kinase A. Various natural products in which one of them Forskolin-An Example of Innovative Drug Research on Natural Products. Applied with rolipram, forskolin provides a route to inhibition of colon cancer cell growth and survival. These two drugs also work together to induce long-term potentiation in neuronal populations. To date, there have been more than two clinical studies examining the effectiveness of forskolin as a weight loss aid. Clinical Studies with Forskolin Eye-Drops in Patients with Open Angle Glaucoma. Forskolin may be helpful in controlling the underlying cause of glaucoma. Increase skin's natural resistance to burning under UV light. Forskolin can also be used to promote nerve repair by increasing cAMP concentrations. Forskolin can activate or upregulate the proliferation of Schwann cells in culture, together with Fibroblast growth factor or Transforming Growth Factor-Beta. Various experimental studies are underway in using Forskolin as an adjuvant in treatment for diseases such as Parkinsons and/or nerve damage caused by trauma/accident. Based on important and versatile role of Forskolin, it is a matter of research to investigate the role of cAMP mediated CREB activation via Forskolin.

Speaker
Biography:

Abstract:

The diabetes constitutes a true problem of public health in the world. It results in a sugar rate abnormally raised, measured in blood in several months of intervals. It is about a chronic metabolic disease which occurs when the pancreas does not secrete insulin: insulino-dependent diabetes (type I) which generally touches the young subject before 30 years or when the pancreas does not produce sufficient insulin and that the secretion of this one is overdrawn; form diabetes found at the adults and the obese ones: noninsulino-dependent diabetes (type II). Indeed, vis-a-vis the noted dissatisfaction of the modern remedies, the traditional phytotherapeutic tracks seem to reinforce an interesting potential, of which the process of development, plant with phytomédicament, through adequate scientific processes, could offer a credible alternative, in favour of the communities.

Speaker
Biography:

Abstract:

Unfractionated heparin (UFH) has been conventionally used during coronary angiography (CAG). However, no data is available for the dosage required. Vascular complications are still frequent in special group of patients. The objective of this study was to determine the incidence of bleeding, vascular, and ischemic complications using three different heparin regimens after successful coronary angiography. This study enrolled 105 patients divided into three groups: Group 1: (n=35 patients) receiving a dose of 5000 IU (systemic heparinization), Group 2: (n=35 patients) receiving a dose of 5000 IU of heparin on the flush saline and Group 3: (n=35 patients) control group will receive flush saline i.e. normal saline flush. All patients included in the study will be subjected to Full history taking, Complete general and local examination of the heart and blood vessels, 12 leads resting ECG, Routine laboratory investigations including fasting blood sugar, liver and kidney function tests, complete blood picture, Lipid profile and coagulation profile. Descriptive statistics was done including mean, standard deviation and percentage. Comparison between groups was done using one way analysis of variance and comparison between the parametric variables was done using chi-square test. Results of the current study showed that there was no significant difference between the three groups regarding the number of diseased vessels or the incidence of slow coronary flow or incidence of normal coronary arteries (P > 0.05). The clotting time and PTT were not significantly different in the three groups before coronary angiography (P > 0.05). After coronary angiography, clotting time and PTT were significantly higher among group I and II than that of group III (P < 0.05). Comparison between before and after coronary angiography in group I and II, the results showed that the clotting time and PTT increased significantly after the procedure (P < 0.05) while, in group III there were no significant difference between before and after the procedure (P > 0.05). The sheath removal duration was significantly higher among group I and group II than that of group III (P < 0.05). There were no major complications recorded in any of the patients in the three groups. Routine elective coronary angiography may be performed without the use of UFH was found to be safe however further detail study is recommended.

  • Pharmaceutics and Novel Drug Delivery Systems

Chair

Kailash Chandra Gupta

Co-Chair

Ramasare Prasad

  • Pharma Analytical Techniques and Instrumentation

Chair

Kailash Chandra Gupta

Co-Chair

Ramasare Prasad

  • Pharmacy Practice

Chair

Kailash Chandra Gupta

Co-Chair

Ramasare Prasad

  • Medicinal Chemistry and Drug Discovery

Chair

Kailash Chandra Gupta

Co-Chair

Ramasare Prasad

  • Pharmaceutics and Novel Drug Delivery Systems
    Pharma Analytical Techniques and Instrumentation
    Nanotechnology
    Medicinal Chemistry and Drug Discovery

Session Introduction

Wolfgang Lechner

Karl-Franzens University, Austria

Title: Hospital-pharmacie: Compatibility of active components in parenteral infusions
Biography:

Wolfgang Lechner has completed his studies for pharmacy and has been promoted as Mag. Pharm. at Karl-Franzens Universität in 1985 and continued with Postdoctoral Research in a pharmaceutical laboratory of the same university with HPLC (High Pressure Liquid Chromatography). He was CEO of different pharmacies in Austria and is now the Owner of a provincial pharmacy.

Abstract:

Parenteral medication today is standard procedure in clinical therapy not only in hospitals but also in the ambulant and practical sector. Extremely important is this kind of application for intensive care because it is the only way to provide medication and nutrition. Frequently, physicians and care personnel are not aware that drugs strongly differ in pH-value and solubility and arbitrary mixing can cause serious consequences and a worse outcome for the patients. Incompatibilities are unwanted physical-chemical reactions of a drug with a solvent which take place before or during an application. These reactions are not to be mistaken as interactions which change the effect of a drug by impact of another substance. Physical or “manifest” incompatibilities usually can be seen as a change of colour, separation, tarnish or precipitation caused by a change of proportion between ionisation and solubility. Chemical or “concealed” incompatibilities are characterized by chemical disintegration and macroscopically not recognizable. Analytical methods (i.e., HPLC) have to be used. For a secure parenteral therapy critical or problematical situations have to be identified before the application which is a major task for pharmacists with their widespread chemical-pharmaceutical knowledge. Our aim is to achieve a clearly arranged tool for the wards to enable the daily application of parenteral medication through central or peripheric-venous catheters in an easy and safe way.

Biography:

Bhubaneswar Mandal has completed his PhD from EPFL, Lausanne, Switzerland under the supervision of Professor Manfred Mutter. Then he earned prestigious Marie Curie Fellowship and worked as a Post-Doctoral Fellow with Professor Herbert Waldmann and Professor Hans-Dieter Arndt, Max-Planck Institute for Molecular Physiology, Dortmund, Germany. Then he joined IIT Guwahati as an Assistant Professor. Presently, he is an Associate Professor there. He is working on novel strategy development for drug design against amyloidoses and industrially useful reagent development for various organic transformations. He has published 28 papers in reputed international journals.

Abstract:

Alzheimer’s Disease (AD), a common amyloidosis, has no cure yet. Pathological investigations revealed existence of numerous plaques in the Alzheimer’s patients’ brain composed of Amyloid-β (Aβ) peptides, derived from Amyloid Precursor Proteins (APPs). Although the mechanism of plaque formation is unknown, AD is believed to be caused by the aggregation of misfolded Aβ peptides. β-breaker peptides have been developed that disrupt amyloid aggregates (plaques) in vitro as well as in vivo. We have developed two novel and innovative strategies for β-breaker peptide design. First one is based on the concept of β-sheet breaker α/β hybrid peptides (BSBHps); and the second one on the concept of β-Breaker Di-Peptides (BBDPs). We have demonstrated that such well designed peptides are capable of inhibition of amyloid formation of Aβ peptide. Also, they disrupt preformed toxic fibrillar aggregates into non toxic species in vitro. Such peptides may be useful for designing novel drugs against diverse amyloidoses including Alzheimer’s disease, Parkinson’s disease and diabetes type II. Recent advancements in this direction of research will be discussed in the Pharma Summit-2015.

Speaker
Biography:

Nasimul Hoda has completed his PhD from Patna University and Postdoctoral studies from IIT Delhi, Supercomputing facility for bioinformatics and computational biology (SCFBIO-IITD). He is the Assistant Professor in Chemistry at Jamia Millia Islamia (Central University). He is working in the field of Drug design and focussing on the development of antimalarial and anti-neurodegenerative agents.

Abstract:

Malaria is a leading cause of human deaths affected by parasitic infection in tropical and subtropical reasons. Out of the four plasmodium species responsible for this disease in human Plasmodium falciparum is the most deadly. Due to the widespread resistance of the current antimalarial drugs, intense research efforts are focused on identification of new potent antimalarials. We report here, a structure based drug discovery strategy for design and synthesis of a series of potent and novel triazine based antimalarials. The X-ray structure of Plasmodium falciparum phosphoethanolamine methyltransferase (PfPMT) is used as a target as it is unique to the parasite. Trisubstituted triazine and its anlaogs are produced by an inexpensive three to four step synthesis giving excellent yields. Parasite growth inhibition assays further confirmed the activity of the molecules to be in 5 to 0.8 μM range showing selectivity towards the parasite over mammalian cells. Molecular dynamics simulations on the PfPMT-inhibitor complex shed light on the inhibition mechanism for further optimization of the lead compounds.

Speaker
Biography:

Driekus Grooff is currently Lecturer of physical chemistry at Nelson Mandela Metropolitan University, Port Elizabeth South Africa. He obtained his PhD in 2010 at North-West University, Potchefstroom, South Africa. His research focuses on solid-state properties and stabilities of pharmaceutical compounds. Collaborative research with the Center of Excellence for Pharmaceutical Sciences at North-West University is currently ongoing. Research outputs in international journals such as Journal of Pharmaceutical Sciences and Thermochimica Acta have emphasized various aspects of solid-state chemistry and include pharmaceutical technology, analytical and physical chemistry.

Abstract:

A variety of Active Pharmaceutical Ingredients (API’s) can exist as hydrate forms. The conditions that facilitate hydrate formation include factors such as humidity exposure during storage, pharmaceutical processing and dosage forms capable of transferring water to API. It is mainly the thermodynamic water activity of the surrounding medium (solution, vapour phase, etc.) that determines whether a given hydrate structure can be formed. Studies that evaluate hydrate structure and stability will be beneficial to the understanding of hydrate formation and influence on physico-chemical properties. Thermal analysis has been widely used for characterization of pharmaceutical hydrates in terms of structural and stability investigations. For hydrate compounds the use of Thermo-Gravimetric (TG) analysis had explored both isothermal and non-isothermal heating regimes for the investigation of thermally stimulated dehydration kinetic parameters. Knowledge of dehydration kinetic parameters under a controlled heating program offer unique insight to drug-water association as the kinetic information mostly relate to structural features and intermolecular forces operating with the parent anhydrate drug form. This study report findings of dehydration kinetic parameters from two structurally relates macrolide antibiotics in an attempt to correlate observed kinetic behaviour to the structural characterization of the hydrate compounds.

Gannu Praveen Kumar

Sahasra Institute of Pharmaceutical Sciences, India

Title: The global strategies and innovations in the pharmaceutical industry
Speaker
Biography:

Gannu Praveen Kumar is a Professor and Principal in Sahasra Institute of Pharmaceutical Sciences since April 2014, graduated from H K E’s society college of Pharmacy, Gulbarga University in 1997, Post-Graduation from BITS, Pilani in 1999 and PhD from UCPSC, Kakatiya University in 2009. He has published in both national and international journals and compiled few chapters for text books. He received Gem of India award in the year 1999. He was selected as a Best Academician in 2001 and 2011. He is an Advisor for few pharmaceutical companies. He visited foreign countries like London, Dubai, Singapore, Malaysia and Spain as Invited Speaker.

Abstract:

Continuous innovation is one of the pharmaceutical industry’s most defining characteristics. New medications can be crucial for maintaining the quality of human life, and may even affect its duration. The global pharmaceutical market is expected to reach $1.1 trillion by 2015. Pharmaceutical innovation is marching towards an orderly, predictable process. It follows a technology push model dependent on a meandering path of scientific breakthroughs with uneven timing and hard to foresee outcomes. Technological competency, decades of rigorous research, and profound understanding of unmet customer needs, while necessary, may prove insufficient for market success as the critical decision for commercialization remains outside the firm. Drug innovation as a business process requires savvy strategic, organizational and managerial decisions. It is already enjoying intensive research coverage, giving rise to abundant but relatively dispersed knowledge of the mechanisms driving drug discovery and development. A comprehensive overview of the process of drug innovation from a business and academic perspective is explained. The evolving organizational forms and models for collaboration, summarize significant empirical regularities, and highlight differences in market positions related to firms’ strategic orientation, innovation emphasis, attitudes to risk, and specialized resources are highlighted. As a guide to future research, critical drivers and modes for drug innovation are systematized in a unifying framework of characteristics and process decisions, and multiple areas in need of further scrutiny, analysis, and optimization are suggested. Because of its rich potential and high significance, research on drug innovation seems poised to gain increasing momentum in the years to come.

Biography:

Subham Banerjee is designated as an Innovation Awardee in Devices, now pursuing his Post-Doctoral Research work at ID3S Laboratory, Center for Bio-design, Translational Health Science and Technology (THSTI), Ministry of Science & Technology, Government of India, Faridabad, Haryana. Recently, he has completed his PhD degree from the joint collaboration of DRDO, Ministry of Defence, Government of India, Tezpur, Assam and BIT, Mesra Ranchi, Jharkhand. He has published more than 25 papers in a peer-reviewed journals, published one book chapter and filed two Indian patents. He is a Life-Time Member of India Science Congress Association.

Abstract:

LNFs have emerged as potential drug carriers to improve Gastrointestinal (GI) absorption and oral bioavailability of several ATDs, especially lipophilic drug like rifampicin. These lipid based nanoformulations may also be used for sustained drug release of such ATDs. The two newer generations of LNFs, namely, Solid Lipid Nanoparticles (SLNs) and Nanostructured Lipid Carriers (NLCs) having capability as oral drug carriers to improve poor and variable oral bioavailability, poor GI absorption, solubility and chemical instability related several issues associated with ATDs that has been perceived as a major bottleneck in successful treatment of Tuberculosis (TB). In these regard, LNFs based drug delivery strategy has been a boon to current pharmacology and biopharmaceutical enhancement of drug performance. Moreover, it is possible to design lipid based drug delivery systems capable of targeting phagocytic cells which are infected by intracellular pathogens, such as mycobacteria. LNFs based delivery systems based on nanotechnology offer wide opportunities for improving the therapy for a range of diseases including TB.

Biography:

Monika Jadhav has completed MPharm from Pune University and has a teaching experience of 2.5 years as Assistant Professor. She is currently working at Shri D D Vispute College of Pharmacy & Research Center, Navi Mumbai. She has published 05 research articles from which 03 are international publications. And she is also one of the Reviewer Board Members of International Journal of Pharmaceutical Chemistry and Analysis, Innovative Publication.

Abstract:

A QbD and lifecycle management approach to analytical method development and qualification results in a better understanding and fewer failures of analytical methods due to more robust methods which produce consistent, reliable, quality data throughout the lifecycle. This, in turn, leads to less method transfer failures and method “incidents” when used in the routine environment. As the MNC’s are now applying Quality by Design (QbD) to process development, it is now being recognized that this is also the way forward to improve and standardize approach to analytical procedures. The recent focus within the pharmaceutical industry and associated regulatory bodies on QbD approaches to analytical method development are a positive sign that both the industry and regulators are acknowledging the importance of understanding the contribution of measurement uncertainty to drug processes and products. The benefits of applying QbD principles to analytical methods include identifying and minimizing sources of variability that may lead to poor method robustness and ensuring that the method meets its intended performance requirements throughout the product and method lifecycle. The ultimate goal is to highlight that QbD concepts and terminology can be applied to analytical methods and to suggest how adoption of a QbD approach might be used to develop more robust analytical methods and effective control systems. At the same time, these efforts aim to support more advanced regulatory approaches to change management.

Biography:

M N Motiwala has completed her Master in Pharmacy (Pharmacognosy & Phytochemistry) from R T M Nagpur University in 2009. She has additional qualification as Diploma in Clinical Pharmacy and Diploma in Industrial Relation and Personnel Management. Presently, she is working as Assistant Professor at Dadasaheb Balpande College of Pharmacy Besa, Nagpur, Maharashtra. She has published various articles in national and international journal. She has delivered oral presentation entitled “Effect of piperine on bioavailability of paclitaxel” at Current Drug Development International Conference, 2010, in Thailand.

Abstract:

The leaves of Cajanus cajan has been traditionally used by Indian village people in wound healing, jaundice, hypocholestrolemia and inflammation. The phytoconstituents of C. cajan includes flavonoids and stilbenes. Wound healing is a complex process that includes inflammation, tissue formation, and remodeling. In order to scientifically prove the claimed utilization of the plant, the effects of the extracts were investigated using burn wound model in mice including in vivo antioxidant and antimicrobial activity. Healing was assessed by the rate of wound contraction, period of epithelization and hydroxyproline content. The antimicrobial activity of extract was also studied against bacterial and fungal strain using agar dilution method. In vivo antioxidant activity was performed to understand the mechanism of wound healing potency. The result showed that C. cajan leaf extract has significant wound healing activity as evident from the rate of wound contraction and epithelization. Hydroxyproline content was correlative with the healing pattern observed. C. cajan leaf extract treatment promote up-regulation of pro-inflammatory cytokines TNF-α during early phase of wound healing, inhibit ROS accumulation and exhibit moderate antimicrobial activity. We propose induction of cytokine production as one of the mechanism for acceleration of wound healing by C. cajan leaf extract which may be due to flavonoids and stilbenes.

Biography:

Uma Devi P has completed her Ph. D. in Pharmacology from Jamia Hamdard University, New Delhi. She has worked as Research Scientist at Ranbaxy Laboratories Limited, Gurgaon. Currently, she is working as Assistant Professor in the Department of Pharmacology, Amrita School of Pharmacy, Kochi. She has published papers in reputed international journals.

Abstract:

Candida is an important cause of bloodstream infections (BSIs), causing significant mortality and morbidity. The true burden of candidemia in India is not clear. Thus, this study was conducted to evaluate the clinical characteristics, species distribution, antifungal susceptibility and outcome of candidemia at our hospital. A total of 165 episodes of Candida BSI were identified between January 2012 and April 2014, with 115 episodes occurring in adult patients. Most of the episodes occurred in males (69.6%). Nearly 82.6% patients were between 41 to 80 years and majority of the patients were in the intensive care unit (65.2%) at the time of diagnosis. Majority of the candidemia episodes were found in the general medicine department (23.5%) followed by gastrointestinal surgery (13.9%) and medical oncology & hematology (13%). Risk factors identified were prior hospitalization within one year (83.5%), antibiotic therapy within the last one month (64.3%), indwelling urinary catheter (63.5%), central venous catheter use (59.1%), diabetes mellitus (53%), severe sepsis (45.2%), mechanical ventilation (43.5%) and surgery (36.5%). C. tropicalis (30.4%) was the leading cause of infection followed by C. parapsilosis (28.7%) and C. albicans (13%). Other non-albicans species isolated included C. haemulonii (7.8%), C. glabrata (7%), C. famata (4.3%) and C. krusei (1.7%). Antifungal susceptibility to fluconazole was 87.9% (C. parapsilosis), 100% (C. tropicalis) and 93.3% (C. albicans). Mortality was noted in 51 patients (44.3%). To conclude, rapid changes in the rate of infection, potential risk factors, and emergence of non-albicans Candida demand continued surveillance of this serious BSI.

  • 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
Speaker
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.

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.

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.

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).

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 I”. 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.

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).

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.

  • Pharmaceutics and Novel Drug Delivery Systems
    Pharma Analytical Techniques and Instrumentation
    Nanotechnology

Session Introduction

Rajendra Sharma

Swami Rama Himalayan University, India

Title: Newer drug delivery system: Pros & cons
Biography:

Rajendra Sharma is a Medical Doctor who hails from Uttarakhand. He is a keen research worker and having his interest to learn further about newer development in pharmaceutical sciences. He has worked with pharmaceutical organization in different settings like clinical research, pharmacovigilance and product development before joining Himalayan Institute of Medical Sciences, Swami Rama Himalayan University, Jolly Grant, Dehradun. He is currently a tutor in Department of pharmacology, Himalayan Institute of Medical Sciences, Dehradun

Abstract:

Drug delivery is the method or process of administering an Active Pharmaceutical Ingredient [API] to achieve a therapeutic effect in humans and animals. Due to drawbacks associated with conventional therapies, i.e., fluctuation in plasma concentration, decrease concentration of drug at site of action, increase cost of therapy and decrease patient compliance, New Drug Delivery Systems [NDDS] to optimize therapy with established drug are required. Drug delivery technologies are patent protected formulation technologies that modifiy drug release profile, pharmacokinetic parameters for improving product efficacy and safety as well as patient convenience and compliance. Various drug delivery techniques include oral, ophthalmic, transdermal, pulmonary, intravaginal/ intravesical, implant, prodrug, gene therapy, targeted drug delivey systems, etc. NDDS are therefore help increase therapeutic efficacy, patient compliance and decrease adverse drug reaction as well. However, NDDS has its own limitation and drawbacks, i.e., NDDS are costly. Talking about particulate carrier system, i.e., nanoparticle, liposomes, etc., particulate nano-carriers have been praised for their advantageous drug delivery properties in the lung, such as avoidance of macrophage clearance mechanisms and long residence times, however instilled non-biodegradable polystyrene nano-spheres with small diameters and thus large surface areas have been shown to induce pulmonary inflammation. Similarly, in polymeric prodrug system, prodrug are used which get bio-transformed in the drug within the body hence the use of prodrug as drug depends upon the body’s ability to release the drug in the body [inter individual variations in drug response]. It may be concluded that drug delivery therapeutic system is defined as drug containing preparation or device that release one/more drug at predetermined rate over a fixed period of time either systemically or at specified site (target organ) and with the vast database of different studies the science of site specific or targeted delivery of these drugs will become wiser and manifestation of these strategies in clinical practice seems possible in near future.

Biography:

Sushama Talegaonkar has completed her PhD from Sagar University. She is working as Assistant Professor in Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, since September 2000. She has about 15 years experience in teaching and research. She has filed 8 Indian patents and published more than 150 research papers in high impact factor international journals and has been serving as an Editorial Board Member of some reputed journals.

Abstract:

Among various classes of drugs bisphosphonates (alendronate and risedronate) offers the most potent types of molecules to treat osteoporosis. The major obstacle that limits the successful use of orally administered risedronate includes low permeability and more importantly, insufficient and fluctuating bioavailability. This poor bioavailability (<1%) of risedronate results in the supplementation of high doses that may perhaps lead to severe side effects like osteonecrosis of the jaws, fever, vein irritation, general aches and pains and kidney dysfunction. Therefore, in the present study, bioceramic (hydroxyapatite) based Poly(D,L-Lactide-Co- Glycolide) (PLGA) and Polyethylene Glycol (PEG) nanoparticles of risedronate, was prepared by dialysis method for bioavailability enhancement. The structure of prepared diblock copolymers were characterized by FT-IR and NMR spectrometry. The formation of surface-modified PLGA nanoparticle prepared with various ratios of risedronate as well as hydroxyapatite and mPEG was confirmed by 1H NMR and FT-IR spectrometry. Pharmacokinetic study was also performed in male Wistar rats in order to evaluate the efficiency of prepared nanoparticles on existing marketed preparation (rosofos tablet). The size and % entrapment of the prepared nanoparticle was found to be 79.3±2.3 nm and 93±3.1%. Transmission Electron Microscopy (TEM) revealed that mPEG-PLGA-RISHA nanoparticles possess smooth and uniform surface. Pharmacokinetic study showed a significant enhancement in bioavailability (2 fold) when compared to marketed preparation. The results strongly implicated that mPEG-PLGA-RIS-HA has a therapeutic benefits over risedronate sodium monotherapy for the treatment of osteoporosis in a rat model. This research is likely to be helpful in the design of functional nanoparticles for the site-specific drug delivery in the treatment of bone diseases.