18^th Annual Congress on Pharmaceutics & Drug Delivery Systems June 27-28, 2019 Holiday Inn Amsterdam – Arena Towers. Amsterdam, Netherlands

Biography:

Hiba Natsheh is currently a Post-doctoral fellow in Prof. Elka Touitou lab at The Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem. Prof. Touitou lab is worldwide recognized for designing novel approaches for enhanced dermal and transmucosal drug delivery.

Abstract:

In a previous work, we have shown the ability of Phospholipid Magnesome to improve nasal drug delivery to brain. Here, we focus on the role of this carrier to enhance the antinociceptive effect of two central acting analgesic drugs, tramadol and oxytocin. More than a two-fold increase in tramadol brain concentration relative to controls was detected in 10 minutes (the first tested time point) following the drug nasal administration in Phospholipid Magnesome. In an in vivo experiment using the acetic acid induced pain mice model, we observed a rapid and improved antinociceptive effect of nasal treatment with these drugs, each incorporated in the new carrier. The treatments reduced significantly the number of writhes achieving a maximum possible effect (MPE%) of 67 and 62% for tramadol and oxytocin systems, respectively. On the other hand, a weak antinociceptive effect was noticed for the nasal control systems: water solution, a non-vesicular system and liposome. In conclusion, our data showed that administrating the two analgesic drugs nasally from Phospholipid Magnesome enhances their delivery to brain and improves pain treatment efficacy in animal model. Using the new carrier may help to design nasal products for noninvasive and efficient pain treatment with a rapid onset of action.

Biography:

KVRNS Ramesh has completed his Post-graduation in Pharmaceutical Sciences and obtained his Doctoral degree in Pharmaceutics specialization from Andhra University, India. His broad area of interest is in the development of controlled release dosage forms and investigations on the stabilization of fast dissolving dosage forms. He has 30 years of teaching and research experience. He has published about 35 research papers in national and international journals. He has delivered lectures in different seminars and conferences organized in the area of Pharmaceutics and Drug Product Development. He has worked in Addis Ababa University under the United Nations Development Project. He is presently Associate Dean and Professor at RAK College of Pharmaceutical Sciences, RAK Medical & Health Sciences University, United Arab Emirates.

Abstract:

New technologies and processes are being developed for existing and new drug molecules to prepare sustained release (SR) and controlled release (CR) dosage forms. Multi-unit forms such as pellets offer significant advantages such as better control over drug release and less chances of dose dumping. In the present work, pellets of furosemide (as a model drug) are prepared by extrusion and spheronization. It belongs to BCS class IV drugs having poor solubility. Since furosemide exhibits low solubility in gastric fluids, to initiate a prompt release from the pellets, a novel approach of incorporating the inclusion complex of furosemide in sulfobutyl ether cyclodextrin in the pellets was employed. Inclusion complex is prepared by kneading method. The utility of almond gum as a binding agent in extrusion and spheronization was investigated. Compared to pellets prepared by employing microcrystalline cellulose, the pellets made by using almond gum were found to be more uniform in size and exhibited a more controlled release spread over 12 hours. The influence of various processing parameters such as speed of extrusion, rpm of spheronizer and time of operation was studied. The characteristics of pellets such as size, size distribution, and shape and drug release are influenced by formulation and processing variations. The drug release data showed a good fit into both Higuchi and Korsmeyer - Peppas equations. The differential scanning calorimetry and infrared spectroscopy (IR) studies revealed that there are no interactions between furosemide and almond gum. The x-ray diffraction studies indicated that the drug furosemide existed in amorphous state in the inclusion complex. The scanning electron microscope (SEM) images of pellets showed that the pellets have spherical shape and their size depended on amount of almond gum employed. The details of experiments performed and results of the investigations will be presented.

Biography:

Leena H Saeed is a Clinical Pharmacist, was graduated from King Saud University in 2009 with First Honor degree. She has obtained her Master’s degree in Clinical Pharmacy in 2013 from King Saud University. Currently, she is working as Clinical Pharmacist covering Neurology and Neurosurgery at King Fahad Medical City, Riyadh, Saudi Arabia. She is interested in Pharmacoeconomics - the use of drug formulations for cost minimization and also in Pharamcogenetics.

Abstract:

Background: In each hospital, there is a good number of patients who are candidates for the switch-over from intravenous (IV) to oral therapy. The main hindrance that restricts intravenous to oral conversion is the idea that oral medications do not reach the same bioavailability as that of intravenous medications and that the same item must be used both intravenously and orally. Although several drugs commonly used in hospitalized patients are equally bioavailable intravenously and orally, patients usually are not shifted to the oral medication when stable and taking oral medications or eating an oral diet. There are many advantages involved in earlier conversion from the intravenous to the oral therapy, including but not conclusive to less nursing time for medication administration, lower cost, less intravenous catheters needed can lead to increased patient satisfaction and safety.

Objective: The objective of the present study is establishment of a pharmacist-led IV to oral switch over protocol in the national neuroscience institute (NNI) at King Fahad Medical City (KFMC), in an attempt to reduce the annual medication cost.

Materials & Methods: The study was conducted in the NNI of KFMC in Riyadh Saudi Arabia. The study was prospective. We identified five targeted medications that are commonly prescribed in NNI (NHDU, NW1, Stroke) inpatient wards with almost identical oral and intravenous bioavailability Forty five (45) patients were recruited. Their files were reviewed by the pharmacist and recommendation to switch was communicated to physician either verbally or documented in the patient file. The total cost of the medications was compared between oral and intravenous forms according to the length of stay in the ward. Inclusion and exclusion criteria are mentioned Difference between oral and IV medication cost were compared using Mann-Whitney U test. All data entry and statistical analyses were performed using SPSS 22.0 software.

Results: This study has been in place for six months. Seventy one (71) recommendations were made. Of these recommendations, 11 (15.5%) were rejected and 60 (84.5%) were accepted and implemented, resulting in a cost savings of 10,652 SAR (P=0.001). When annualized, the expected savings is 21,304 SAR or nearly the monthly salary of two full-time pharmacists.

Conclusion: This study demonstrates successful implementation of a pharmacist-led switch-over strategy. Duration of IV treatment reduced dramatically and the annual savings significantly improved. This program has been well accepted by physicians and pharmacists. It appears to be having a positive impact on physician awareness of using oral medications when appropriate. This study may be used as a template for the introduction of further pharmacist-led early IV to oral switch-over initiatives.

Biography:

Dr Madi is a Postdoctoral Research Fellow and PI with a demonstrated history of working in the higher education sector. Dr Madi is currently undertaking an Industrial Research Fellowship with APC Ltd (Science Foundation Ireland Award). Skilled in Pharmaceutics and Pharmaceutical Technologies. Dr Madi holds a Master of Science (MSc.) in Pharmaceutical Analysis and Doctor of Philosophy (PhD) focused on Oral Drug Delivery. Dr Madi works under the direction of Professor Anne-Marie Healy of Trinity College Dublin, Dublin, Ireland since February 2016.

Abstract:

Spray drying (SD) is often used as a continuous processing technique to isolate, purify and to enhance the biopharmaceutical properties and processability of many active pharmaceutical ingredients (APIs). One of the main applications of SD is to manufacture amorphous solid dispersion (ASD) formulations of poorly water-soluble crystalline drugs. The amorphous state, with a higher energy than the equivalent crystalline form, typically confers significantly higher solubility on the API, resulting in enhanced dissolution and bioavailability characteristics, which can reflect in a higher therapeutic efficacy of the drug product. One of the limitations of SD is that it usually produces fine spherical solid particles that exhibit poor powder flow characteristics, which requires further processing before they can be presented in a final dosage form such as a tablet. Materials selection and processing conditions are critical parameters for the success of the SD technique in  the manufacture of ASDs. Furthermore, addition of excipients and further downstream processing will influence the performance of manufactured ASDs. In our research, the SD technique was employed as a continuous processing technique to manufacture ASD formulations of model poorly water-soluble drugs; namely: Indomethacin and Glibenclamide. The effect of polymeric carrier selection, solvent mixtures used, and different SD processing conditions were all investigated. ASDs of the candidate API were successfully manufactured and different process critical parameters were monitored and identified. This study provides deeper insights on the effect of different SD process related parameters, as well as material selection, on the nature and performance of the manufactured formulations.

Biography:

Prof. Radostina Alexandrova has graduated with honors in Biochemistry and Microbiology, Sofia University “St. Kl. Ohridski” (SU) in 1991; MSc and PhD in Virology; Postdoctoral training in Slovakia, Hungary, Denmark, Iceland; lecturer in SU and PhD School of Bulgarian Academy of Sciences (BAS). She is a team-leader in the Department of Pathology, IEMPAM-BAS. She has published more than 150 papers in reputed journals and conference proceedings.

Abstract:

The aim of our study was to evaluate the influence of newly synthesized  complexes of Zn(II), Co(II) and Ni(II) with kojic acid on viability and proliferation of cultured human (HeLa cervical carcinoma), rat (sarcoma LSR-SF-SR) and avian (liver cancer LSCC-SF-Mc29) cancer cells. Short-term experiments (24-72 h, with monolayer cell cultures) by thiazolyl blue tetrazolium bromide (MTT) test, neutral red uptake assay (NR), crystal violet staining (CV), double staining with acridine orange and propidium iodide, AnnexinV/FITC method as well as long-term experiments (14 days, with 3D cancer cell colonies) by 3D-colony forming method were carried out to investigate the cytotoxic activity of the compounds. The results obtained revealed that the compounds examined decreased viability and inhibited 2D and 3D growth of the treated cells in a time- and concentration-dependent manner. Co(II) complex with kojic acid (CoKoj) was found to be the most promising cytotoxic agent in human HeLa and rat LSR-SF-SR cells whereas ZnKoj showed the highest effectivity in chicken LSCC-SF-Mc29 cells. NiKoj exhibited the lowest cytotoxicity. Cytopathological changes and apoptosis were observed in the cells cultivated in the presence of the compounds tested.

Biography:

Jesús Rodriguez Lastra is Doctor in Medicine Physiologist at Habana University. He is Professor of Physiology at Habana University and Carabobo University, Valencia, Venezuela. He is also Professor Collaborator at University Autonomic de Madrid.

Abstract:

Introduction: There is evidence that electromagnetic stimulation can result in a greater reduction of the surface area with more complete healing of stage II to IV ulcers.

Methodology: We studied 36 patients, 21 women and 15 men, who presented ulcers in the lower limbs. Nine men and 15 women had diabetes mellitus. The thickness of the skin of the leg was measured with ultrasonography and the temperature with thermographic camera.

Results: A CAPENERGY C200 Tecartherapy device was used. A total of 10 sessions were applied at a frequency of one/week with a power of 60% and a frequency of 1.2 MHz for 30 minutes. The edema, observed in 34 patients in the region of the lower extremity, disappeared in 26 of the 36 patients (Wilcoxon p=0.003). This result was confirmed by the 0.4 mm decrease in subcutaneous cell thickness (Friedman's test p=0.000). The temperature before and after was increased by an average of 1.4°C (Wilcoxon p=0.000).

Discussion: The use of radiofrequency in the treatment of ulcers in diabetic and non-diabetic patients is beneficial. An important characteristic is that it is not invasive, it is not painful, it is well tolerated and the results are evident, the injury improves and the quality of life.

Conclusion: The greater speed in healing can be explained by the anti-inflammatory effect due to the changes in the coagulation and anticoagulation systems, the improvement of the microcirculation, together with better response of the immune system.

Biography:

Zavialova Kseniia Vladimirovna is a Research Scientist at the Department of Radiophysics at Tomsk State University. She has obtained her Master's degree in Radiophysics and defended PhD in the field of Physical and Mathematical Sciences in 2015. Since 2016, she has been researching and developing methods of radio wave tomography of biological objects.

Abstract:

Biography:

Patricia Sibylle Hegger has completed her PhD on “Hyaluronan Based ECM-Mimetics with Tunable Charge Densities - Physico-Chemical Properties and Biological Implications” from Max-Planck-Institute for medical research in 2017. Before starting her career in industry she took over an interim-groupleader position at the Max-Planck-Institute for Medical Research continuing her studies on hyaluronic acid. She is now a Lab-Head in the Biopharmacy group of the TIDES Drug Product department of Sanofi-Aventis Deutschland GmbH, a global pharmaceutical company.

Abstract:

The uptake of subcutaneous (s.c.) administered formulations into the systemic circulation is a function of numerous quite diverse processes like active pharmaceutical ingredient (API) dissolution from the formulation and disintegration to monomers (“liberation”), local metabolism and the permeation through the interstitium and endothelium into the blood vessels (“absorption”). The determination of these parameters prior to launch of the drug is the field of biopharmacy, with its three pillars: in silico, in vitro and in vivo assessment combined with in vivo - in vitro correlation. For s.c. administered formulations however there is only a limited number of systematically applied biopharmaceutical in vitro - in silico tools for characterization of those processes. For example the first in vitro methods for biopharmaceutical evaluation was published in 2015, whereas comparable methods for orally administered small molecules are established since the 1960s. Taken into account, that around 70% of the marketed drugs today are s.c. applied, this is a highly evolving field with the potential of improvement for (I) molecule selection, (II) formulation selection and optimization and (III) understanding as well as prediction of in vivo findings in animals and humans.

Biography:

Peter H Karpinski has recently retired from Novartis Pharmaceuticals, USA, is a Consultant, Expert Witness, and Trainer in the areas of polymorphism, form/salt selection, and characterization of APIs; and crystallization and precipitation processes. At Novartis, he was the Leader of Particle Engineering and Salt & Polymorphism networks. He has over 40 years of international experience in research on crystallization and precipitation processes. He taught Chemical Engineering at Polish and US universities. He has published several textbooks and over 50 refereed papers, presented dozens of invited papers at national and international symposia, and hold a number of patents.

Abstract:

In order to control drug substance (DS) properties one has to select an optimal form (specific polymorph or hydrate of free form, salt, or co-crystal) and be able to consistently manufacture it with the same particle size (PS), particle size distribution (PSD), and crystal surface attributes. The use of automated and robotic systems in salt/co-crystal and polymorph screening, and in early crystallization development experimentation, facilitates DS form selection. Ultimate properties of DS are largely determined by the way the batch precipitation or crystallization processes are conducted, and to obtain crystalline material of desired properties consistently, these processes must be carefully controlled. This can be accomplished via in-situ seeding that simplifies the design and control of batch precipitation/crystallization and gives the results comparable with the conventional seeding approach. Continuous precipitation/crystallization removes the risk of batch-to-batch variability and ensures an optimal control of PS, PSD, and particle surface attributes.

Biography:

Lamis Refaat has completed her BSc degree in Pharmaceutical Sciences from the Faculty of Pharmacy, Ain Shams University and MSc degree in Chemistry from the American University in Cairo in 2019. Her research interests include targeted drug delivery and nanotechnology applications in cancer research.

Abstract:

Carboplatin’s success in the treatment of major types of cancer has been attributed to its ease of administration and its high therapeutic index. However, despite its superior toxicity profile, myelosuppression remains to be its dose-limiting side effect. Liposomes have been researched extensively as carrier systems for therapeutic agents; their high biocompatibility, their ability to escape the immune system and most importantly their ability to incorporate both hydrophobic and hydrophilic drugs led to numerous liposomal formulations being designed for cancer therapy. Magnetic nanoparticles have been gaining attention as their properties enable them to be used in various therapeutic and diagnostic applications, in addition to gene and drug delivery. We report the successful preparation of magnetic liposomal formulation with particle size less than 200 nm, coated with Polyethylene Glycol, encapsulating superparamagnetic magnetite nanoparticles and carboplatin in its aqueous lumen. Two types of liposomes were prepared through thin film hydration technique; magnetite liposome and carboplatin-magnetite liposome with mean particle sizes of 183.3±2.651 nm and 192.5±3.427 nm respectively. Both formulations showed uniform particle size distribution and sterical stability as evident from their polydispersity index and Zeta-potential values. Encapsulation efficiency of magnetite in magnetite liposomal formulation was 61.37%, this value decreased significantly upon incorporation of carboplatin with magnetite in the second formulation. Carboplatin’s EE% was found to be 13.87%, its release profile from the liposome showed a controlled release over the course of 72 hours. The prepared formulations have been successfully magnetically controlled and currently the magnetic gradient and input current strength are being manipulated in order to determine the optimum velocity of particles in the desired media. Additionally, in vitro tests performed on melanoma and mammary cell lines showed significant superior cytotoxicity profile of carboplatin-magnetite liposome over free carboplatin solution.

Biography:

Bilge Debelec Butuner has completed her PhD in 2012 from Ege University, Turkey and Post-doctoral studies in Faculty of Pharmacy at Ege University. She has been working in the same department as Assistant Professor since 2016 with the focus on cancer therapeutics, drug delivery, cancer immunology and immunotherapy.

Abstract:

Sirtuin 1 (SIRT1) is a histone deacetylase (HDAC) from sirtuin family. High expression of SIRT1 induces activation of DNA repairing factors eventually leading either tumor suppression or tumor development in cellular context dependent manner. Most of the chemotherapeutics induce apoptosis by creating DNA damage in tumor cells. However, SIRT1-activated repair of the chemotherapeutic-induced DNA damage results in decreased apoptosis and finally chemotherapy resistance. Therefore, inhibition of SIRT1 is a promising strategy both in anticancer therapy and preventing chemotherapy resistance. In this study, SIRT1 siRNA carrying liposomal formulations have been formulated by using N-[1-(2,3-dioleyloxy)propyl]-N,N,N-trimethylammonium chloride (DOTMA) as cationic lipid by freeze drying method. Their effect on SIRT1 silencing has been determined as 2.5-4 folds both on mRNA and protein levels on prostate cancer cells (LNCaP, Du145, and PC3) with different p53 expression pattern. Efficiency of the formulations to enhance the activity of doxorubicin, which is a chemotherapeutic performing its activity by creating DNA damage has been studied and found to increase the activity of doxorubicin on cell death although they have no effect on cell viability when they applied onto cells alone. Besides, enhanced DNA damage recognition after SIRT1 silencing by the formulations has been determined as the underlying cause of increased cell death. Further, no negative effect of the formulations on cell viability of normal prostate cells has been evaluated as a promising result for selectivity on cancer cells. As a conclusion, a series of siRNA carrying liposomal formulations for SIRT1 inhibition is able to enhance the chemotherapy efficiency in combinatorial use with DNA-damaging chemotherapeutics on prostate cancer cell lines.

Biography:

Ehab R Bendas is Professor of Pharmaceutics, Pharmaceutical Technology and Pharmacy Practice at the Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt. He obtained his Master’s degree and PhD in Pharmaceutics from Faculty of Pharmacy, Cairo University. He was a Post-doctoral Research Fellow at Oregon State University, USA. His research interests are focused on Nanotechnology, Drug Delivery and Pharmacokinetics.

Abstract:

In latest years, excipient development has become an essential part of research in pharmaceutical drug delivery because it impacts the formulation development and drug delivery process. Repeated dose medication usually maximizes adverse effects, while sustained release systems did not offer a fast onset of action. The aim of this study is to formulate Etodolac to enable pulsatile and sustained drug release patterns, which was chronologically more suitable as an anti-inflammatory drug. Eudragit RSPO, Eudragit RLPO, and Hydroxypropyl Methylcellulose (HPMC K15M) were added in the sustained release layer and tried in different ratios. Croscarmellose sodium or sodium starch glycolate were used as superdisintegrants for the fast release layer offering the loading dose for rapid onset of drug action. Bilayer tablets were successively coated with Opadry II, HPMC K4M and HPMC E5 (1:40), and Surelease. All formulations complied with the Pharmacopeial standards for post-compression parameters. The coated bilayer tablet showed pulsatile and sustained release effects in rats. The licking time and swelling degree were tested and results demonstrated significant difference (P<0.05) between the sustained anti-inflammatory action of formulation C1 compared to other groups. Therefore the new chronological design could provide a consistent drug release over 24 h with good protection against associated symptoms of gastric release.

Biography:

Meenakshi Barua has completed her graduation in Environmental Science from Delhi University (2007) and Master’s in Biotechnology from KIIT University, Bhubaneshwar (2010). She had been in Environmental and Industrial Biotechnology Division at The Energy and Resources Institute (TERI), Lodhi Road, New Delhi from period 12^th January 2010 - 12^th July 2010 for dissertation. She has qualified GATE, (Biotechnology) in 2011. Further she had enrolled herself in PhD (Biotechnology) at B.K. Birla College of Arts, Science and Commerce, University of Mumbai. Recently, she has submitted her synopsis and thesis is under process for submission. She worked as a visiting Faculty in her present college also. She had presented papers (oral and posters) in national and international conferences. She has published several papers in reputed journals during her PhD. She had participated in the state level science model exhibition sponsored by Delhi (state) Govt. in 2004.

Abstract:

The present study investigated Cassia alata L. flower plant fraction on human urinary bladder carcinoma (T24) cell lines via in-vitro SRB assay for anticancer property. Fresh flowers of Cassia alata (C. alata) plant were collected from suburban area of Maharashtra, India for preparation of plant extract. Soxhlet extraction method was used for plant extract preparation. Bioactive fraction was separated via column chromatography method. Separated fraction was used against T24 carcinoma cell line and Vero cell line (mammalian non-cancerous cells) in four different concentration viz. 10, 20, 40, 80 µg ml. Effect was compared with Adriamycin (standard anticancer drug and used as appositive control) and Emodin, a plant standard. Separated plant fraction demonstrated a dose-dependent reduction in the overall activity of T24 carcinoma cell line. C. alata flower separated fraction exhibited cytotoxic effect on T24 carcinoma cell line with IC₅₀ value 45.3 μg/ml and effective GI₅₀ value 18.8 μg/ml. Graph obtained from SRB cytotoxicity assay showed that separated plant fraction reduced the growth in T24 cell lines by lower than 50% with initial 10 µg/ml concentration. In Vero cell line separated plant fraction and plant standard not showed any cytotoxic effect even when applied in higher concentration i.e. 80 µg/ml. In contrast, standard anticancer drug showed pronounced cytotoxic effect even in lower concentration i.e. 10 µg/ml. Phase contrast micrographs of T24 cell line treated with separated fraction showed significant decrease in viable cell numbers at 24 hrs of treatment. In conclusion, present study showed that separated fraction from C. alata flower has potential anticancer activity and showed significant result against urinary bladder carcinoma cell line.

Biography:

Fariba Hajifathaliha is a PhD student at School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran (SBMU). She works on cell microencapsulation. She recently published an article entitled “Comparison of Different Cationic Polymers Efficacy in Fabrication of Alginate Multilayer Microcapsules” in Asian Journal of Pharmaceutical Sciences. She also attended in different congress as poster presenter.

Abstract:

Poly l-lysine (PLL) has been introduced as a strengthening covering layer for alginate microcapsules which are the most convenient way for cell encapsulation. Some disadvantages of PLL such as high price, low biocompatibility have made scientist to find better alternatives to it. Linear poly ethylene imine (LPEI), due to its highly similar structure to PLL, could be considered as a proper cost-effective alternative. In this study LPEI and PLL as covering layers of cell-loaded microcapsules (cALA/cAPA) were compared. In addition to the physico-mechanical properties, the encapsulation efficiency, cell survival post encapsulation, cell viability and cellular metabolic activity within the microcapsules were evaluated using trypan blue, live/dead cell staining and MTT test, respectively. Physico-mechanical evaluation of the microcapsules revealed that the cell microencapsulation process did not affect shape, size and mechanical stability of them. Although the encapsulation efficiency for cALA and cAPA was not different (P>0.05), cell survival post encapsulation was higher in cALA than cAPA (P<0.05) which could be the reason for the higher cell viability and also cellular metabolic activity within these microcapsules in comparison to cAPA. Here, based on these results ALA could be introduced as preferable alternative to APA for cell encapsulation.