Scientific Program

Day 1 :

Keynote Forum

Juergen Lademann

Director Center of Experimental and Applied Cutaneous Physiology, Germany

Keynote: Topical drug delivery with nanoparticles: Science fiction or reality?

Time : 09:15 - 09:55

Biography:

Jurgen Lademann graduated from the Moscow Lomonosov State University in 1980. 1991 he received the Assistant Professorship from the University of Jena, Germany. From 1993 to 1995 he headed the Medical Center of Sensor Technology at the University of the Armed Forces Germany. In 1996 Jurgen Lademann joined the Charite Universitatsmedizin Berlin and was appointed Director of the Center of Experimental and Applied Cutaneous Physiology. In 2001 the Charite appointed him full professor of Dermatology. He is the Vice President of the IFSCC and the editor of the Journal Skin Pharmacology and Physiology. He authored more than 600 peer-reviewed articles.

Abstract:

The demands on nanoparticles for use in dermatology and cosmetics are very different. While nanoparticles widely applied in sunscreens, like TiO2 and ZnO, shall remain on the skin surface or in the upper cell layers of the stratum corneum, nanoparticles intended for drug delivery shall penetrate through the skin barrier to the target structures in the living cells.

At the Charité - Universitätsmedizin Berlin various laser scanning microscopy methods are used to investigate the penetration and storage of nanoparticles in the skin, hair follicles being in the focus of attention. Human hair follicles are ideal target structures for drug delivery. Hosting both the stem and dendritic cells, they are surrounded by a dense network of blood vessels. Investigating nanoparticles of different size and materials, it was found that particles of approximately 600nm diameter penetrate most efficiently into the hair follicles and can be stored there for ca. 10 days. Their retention time in the hair follicles exceeds that in the stratum corneum by almost one order of magnitude

Biography:

Michael O'Rourke has over 30 years drug delivery experience across ophthalmology, periodontal and pulmonary markets in sales, marketing, product launch, strategy development and global commercialization. In 2009 he founded Scotia Vision, a specialized ophthalmic consulting company with extensive expertise in global ocular drug delivery commercial and product development strategies. Career experience includes senior positions with several global leading organizations and start-ups, including 3M, Alza, Chiron Vision, Bausch + Lomb, GrayBug and Re-Vana Therapeutics. His unique global ocular drug delivery experience includes launching the world’s first intra ocular drug delivery technology in Europe, Vitrasert, and the world’s second, Retisert, in the USA. He’s managed 28 brands, led 13 product launches, structured/negotiated 12 strategic business deals and has been a team member in 18 device/drug approvals. Michael is from Glasgow Scotland but is now based in Tampa Florida. He was recently elected into the Global Scot "Hall of Fame”, for supporting and advising Scottish start ups and existing organisations in the Life Sciences and other sectors including music with the Royal Scottish National Orchestra.

Abstract:

The global ophthalmic pharmaceutical industry is estimated to reach $29 billion by 2022 with a growing elderly population and the increasing incidence of diabetic eye disease, due in part to increasing obesity rates in both adults and children. The number of people visually impaired in the world is approx. 295 million, with at least 39 million blind and 256 million having low vision. 65% of people visually impaired and 82% of all blind are 50 years and older. There is urgent need to develop new therapeutics and ocular drug delivery systems, providing controlled release for 4-6 months or longer for the treatment of chronic and blinding eye diseases. These will increase patient' s and doctor' s convenience by reducing the dosing frequency including the ability to minimize frequent intra vitreal injections for chronic conditions of the retina. Currently there are only 4 sustained release ocular drug delivery systems ever approved worldwide, treating blinding eye diseases. There is a significant need for both new delivery systems and therapeutics for both small and large molecules. This presentation will cover the development of systems to date, discuss new technologies under current development, the challenges to overcome and how they can ultimately successfully commercialized.

Keynote Forum

Istvan Toth

Professor, The University of Queensland, St. Lucia, Queensland, Australia

Keynote: Lipophilic vaccine delivery systems

Time :

Biography:

Professor Istvan TOTH is Chair in Biological Chemistry & Professor of Pharmacy, The University of Queensland (UQ), Brisbane, Australia; Affiliated Professorial Research Fellow and Group Leader, Institute of Molecular Biosciences, UQ. He graduated with a degree in Chemical Engineering from the Technical University, Budapest, Hungary in 1969 and was awarded his PhD in 1972 for research in Alkaloid Chemistry. In 1994 he was awarded a DSc for his work on drug delivery. Prof. Toth moved from the School of Pharmacy at the University of London to the University of Queensland in 1998, and leads a productive medicinal chemistry research group (presently 30 members). He is an elected RACI Fellow, Fellow of the Queensland Academy of Arts and Sciences and Fellow (External) of the Hungarian Academy of Sciences. In 2009 he was awarded the Adrian Albert award for sustained and outstanding research in medicinal biochemistry. He has over 400 peer-reviewed publications (>500 citations/year since 2012), 44 patents, and a strong record in research commercialization.His research has attracted over $84 million in competitive grants, research contracts and investment funds in the past 10 years, including an NHMRC Program grant, which is now in its fourth successive 5-year term and a recent NHMRC Project Grant.

Abstract:

Infection with group A streptococci (Streptococcus pyogenes, GAS), one of the common and widespread human pathogens, can result in a broad range of diseases, with the potential of acute and post-infectious rheumatic fever and rheumatic heart disease. Immunity to GAS relies on the production of opsonic antibodies specific to the hypervariable N-terminal and conserved C-terminal regions of the coiled-coil α-helical M protein, the major virulent factor in GAS. The development of an effective vaccine for GAS has been challenged by the induced autoimmunity of epitopes derived from the C-terminal regions, unsuitable B-cell epitopes that have been shown to react with human heart tissue, and the minimal B-cell epitopes, which believed to be safe, shows little or no immunogenicity unless bound to a delivery platform. For vaccine delivery, self-adjuvanting lipid core peptide (LCP) and polymer coated liposome systems including antigen, carrier and adjuvant within the same molecular entity has been developed. The systems allow the attachment of multiple copies of antigens.

  • Sessions on: Novel Drug Delivery System | Targeted Drug Delivery System
Biography:

Dr. Thomas J. Webster’s (H index: 109; Google Scholar) degrees are in chemical engineering from the University of Pittsburgh (B.S., 1995; USA) and in biomedical engineering from RPI (Ph.D., 2000; USA). He has served as a professor at Purdue (2000-2005), Brown (2005-2012), and Northeastern (2012-2021; serving as Chemical Engineering Department Chair from 2012 - 2019) Universities and has formed over a dozen companies who have numerous FDA approved medical products currently improving human health.  He has graduated over 200 Ph.D. students and has over 800 publications. Dr. Webster has numerous awards including: 2020, World Top 2% Scientist by Citations (PLOS); 2020, SCOPUS Highly Cited Research (Top 1% Materials Science and Mixed Fields); 2021, Clarivate Top 0.1% Most Influential Researchers (Pharmacology and Toxicology), and is a fellow of over 8 academic societies.

Abstract:

Introduction: Over the past 20 years, the use of nanotechnology in medicine has grown from the unknown to now significantly helping to prevent, diagnosis, and treat numerous diseases. This includes the use of nano biodegradable metals (like Mg) and self-assembled materials that carry metals and are biodegradable. Methods: Numerous biodegradable metal nanoparticles as well as nanotextures have been synthesized1.  For example, Mg nanoparticles were pressed into model surfaces and soaked in NaOH to create a nanoscale surface roughness. Similarly, self-assembled materials containing biodegradable metals have been synthesized using standard organic chemistry methods (Figure 1)2. All materials have been studied for their ability to attach to viruses (such as SARS-CoV-2) to keep the virus from replicating. Further, such materials have been used to fight infection, inhibit cancer cell growth, and improve tissue growth using standard in vivo and in vitro methods3, 4. Results: For the self-assembled nanomaterials, one type of self-assembled nanomaterial composed of DNA base pairs has been the focus of our efforts to functionalize with specific peptides suitable for attaching to SARS-CoV-2 and all of its known variants. After binding to SARS-CoV-2, the self-assembled molecule inhibits SARS-CoV-2 binding to and entering mammalian cells keeping it from replicating. Moreover, these unique self-assembled nanomaterials have been functionalized with peptides to attach to and penetrate to kill gram-positive bacteria, gram-negative bacteria, and antibiotic-resistant bacteria. Further, these self-assembled nanomaterials were functionalized with peptides to attach to and kill cancer cells. Lastly, significant effort has been spent to functionalize these self-assembled nanomaterials with peptides to promote bone, cartilage, vascular, skin and other tissue growth. Conclusions: In vitro and in vivo studies will be presented as well as lessons learned trying to commercialize university-based research into real commercial products.

 

Surangi Jayawardena

Assistant professor The University of Alabama in Huntsville USA

Title: Targeted Drug Delivery -Nanoantibiotics for Targeted Antibiotic Delivery for Bacteria
Biography:

Nanoparticle development and imaging for end user applications such as therapeutics and diagnostics. Nanomaterial development for therapeutics encompass antibacterial agent conjugated material which enhance the the efficacy of the antibacterial agent. Diagnostics include nanoparticle based fluorescent imaging of surface lectin receptors on lung human carcinoma cell lines.
Discriminant analysis based pattern recognition to recognize patterns of lectin and carbohydrate binding.

Abstract:

The work demonstrates the use of carbohydrate-conjugated nanomaterial (glyconanomaterial) to target bacterial pathogens. A collection of systematic studies done by several groups has demonstrated that bacteria can be specifically targeted using various oligosaccharides. Through our preliminary investigations we have discovered that oligosaccharide conjugated nanoparticles (glyconanoparticles) could be used to target strain specific bacteria. For example D-maltoheptaose (G7) and trehalose conjugated nanoparticle used to effectively target Escherichia coli and Mycobacterium spp. Antibiotic resistance in pathogenic bacterial strains is a growing global concern. We have demonstrated that these glyconanoparticles have been used as a carrier for antibiotics that would help target bacteria and reduce minimum inhibitory concentration of a conventional antibiotic. Antibiotic streptomycin (Str) is a broad range aminoglycoside typically used in the treatment of tuberculosis. We have bi-functionalized a nanoparticle using carbohydrate-G7 antibiotic-Str to produce glyconanoantibiotics (GNAs). As proof of concept for active targeting GNAs are used against a highly Str resistant E. coli strain. The GNAs demonstrated size dependent increased antibacterial efficacy few log folds improvement over the free the free antibiotic (Str).

Biography:

Panpan Ma has been a PhD student in the Faculty of Health (Université Paris Cité) since 2019 under the supervision of Dr. Yohann Corvis. She focuses on the preparation of anti-cancer and anti-inflammatory nanocrystal suspensions by using a solvent/antisolvent precipitation approach. The original nanocrystals prepared present targeting and sustained release properties, modifying the therapeutic impact of the drug. Her work includes synthesis of nanocrystals, structural characterization, dissolution studies, in vitro and in vivo studies, emphasizing the advantages of innovative drug delivery systems.

Abstract:

Up to 90% of the active pharmaceutical ingredients (API) currently in development present low solubility because approximately 65% and 15% belong to Class II and Class IV of the biopharmaceutical classification system (BCS), respectively. 1 Therefore, in order to develop new drugs towards clinical applications, improving API solubility is a major challenge for the pharmaceutical field. Crystal nanosuspensions, otherwise known as nanocrystals (NCs), consisting of pure API stabilized by a surface-active agent, have emerged as one of the most promising approaches for overcoming bioavailability issues. This allows optimizing the therapeutic efficiency of the NC drugs with better safety and targeting properties, while being administrated through various routes.2,3 The UTCBS lab pioneered the bottom-up approach with minimal amount of Pluronic®F-127 as stabilizer to engineer etoposide (BCS class IV) NCs for anti-cancer treatment, which strengthened the feasibility of drug NCs as effective delivery systems for nanomedicines administered parenterally and with lower side effects than the related marketed product, Toposar®. 4 Interestingly, around 40 NC drug formulations are in market and under clinical trials, but only two marketed antiinflammatory products have been approved by the U.S. Food and Drug Administration (i.e. Naprelan® and Acticoat®, approved in 2006 and 2008, respectively), and another one, the anti-inflammatory drug Paxceed®, is currently on phase III of clinical trial. 5 The present work consists of developing our expertise on anti-cancer therapeutic NCs with other API pharmaceutical classes like anti-inflammatory with curcumin (BCS class IV), a typical natural compound extracted from turmeric, and prednisolone (non-classified BCS class), a synthetic cortisol compound. For that purpose, two different Pluronic®derivatives, namely Pluronic® F-127 and F-68 were evaluated. By optimizing several experimental parameters, the API/stabilizing agent ratio were adjusted to screen out the best formulation of nanocrystal with convenient yield, high stability, sustained release performance and improved therapeutic activity.

Shuhaib.B

Department of Pharmaceutics, Crescent College Of Pharmaceutical Sciences, Kannur, India

Title: Studies On Formulation And Characterization Of Topical Preparations Like Microsponge Gel And Emulgel Containing Mefenamic Acid
Biography:

Abstract:

The objective of the present investigation was formulate & characterize the microsponge of Mefenamic acid, these microsponges were prepared by quassi-emulsion method. Pre formulation studies by FTIR, revealed no interaction between pure drug and the different polymers used. The prepared microsponges were characterized for their production yield, drug content, mean particle size & entrapment efficiency, Effect of formulation variables was also studied. The microsponge containing 0.5 gm of poly vinyl alcohol, 0.6 gm of ethyl cellulose and 5ml ethanol was found to be good compared to the other formulations prepared. The best microsponges (M3, M6, and M9) were in cooperated into gel and emulgel. The topical gel and emulgel formulation were evaluated for their organoleptic characters, viscosity, spreadability, drug content and drug release studies. The results showed microsponge gel of mefenamic acid containing eudragit RS100 microsponge emulgel of mefenamic acid containing ethyl cellulose as best formulations, the in vitro drug release profile of mefenamic acid was found to better from the emulgel formulation compared to gel formulation.

 

  • Sessions on: Nanotechnology in Drug Delivery | Pharmaceutical Development | Formulation Technology

Session Introduction

Ritu Singla

Project Manager II Labcorp Drug Development, Australia

Title: Title: Advanced Applications of Nano Drug Delivery Systems
Biography:

Abstract:

Statement of the Problem: Cancer is a world-wide problem. Better diagnostic technologies can improve cancer detection and outcomes from cancer treatments. Advanced diagnostic technologies such as nano delivery system serve as means of diagnostic tools or to deliver therapeutic agents (chemotherapeutic agents, biological agents, immunotherapeutic agents etc.) site-specific, and target-oriented delivery of precise medicines in a controlled manner. Methodology & Theoretical Orientation: The therapeutic progress of cell-based therapies was assessed by labelling chimeric antigen receptor (CAR) T-cells with novel radioactive labelled superparamagnetic iron oxide nanoparticle and tracked using clinical hybrid imaging modalities. Findings: The cell tracking platform in first-in-human studies provided real-time data on distribution, migration and localization of CAR-T cells. It further provided insight into physiology, efficacy and toxicities of cell based therapy. The dual imaging technology developed is simple, scalable, non-invasive and biocompatible and addressed the lack of effective imaging tools for cell-based therapies. It is not only suitable for early tumour detection but also for ongoing monitoring in oncology. In another study, a sustainable, reagent-less and one-pot ultrasonic methodology has been developed to transform natural biomaterials into micro/nanocrystals with distinct morphologies which then can be used to load anticancer drugs with high loading efficiency) for site specific and targeted delivery in controlled manner. The synthesized particles showed, high thermostability, antioxidant properties and a remarkable antiproliferative effect in human breast cancer cells. Conclusion & Significance: Nanomedicine has revolutionized the way we discover, image and administer drugs in biological systems. The first study validated and demonstrated the potential for cell tracking in immunotherapy. The second study emphasized on green chemistry to convert novel natural biomaterials into nano drug delivery system for precision medicine. 

 

Hakam Alaqabani

Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Jordan

Title: Colloidal Stability and Cytotoxicity of Polydopamine-Conjugated Gold Nanorods against Prostate Cancer Cell Lines

Time : 14:30-15:00

Speaker
Biography:

A committed researcher experience in nanoparticles for drug delivery targeting and performing tissue culture, synthesis of nanoparticles, cytotoxicity, apoptosis, migration, molecular evolution of cancer, and other assays, responsible for the synthesis of nanoparticles in different shapes and conjugation with different ligands, and characterized GNPs of various shapes, then functionalized GNPs with various ligands, assessing chemical and colloidal stability, to create a Nano-platform for cancer treatment as targeting drug delivery system for chemotherapeutic agents. finally evaluating cytotoxicity and anti-invasion properties

Abstract:

Prostate cancer is one of the most common cancers in men. Cell invasion is an important step in the process of cancer metastasis. Herein, gold nanorods (GNRs) and polyethylene glycol (PEG)- coated GNRs were conjugated with polydopamine (PDA). The PDA-nanoconjugates demonstrated excellent colloidal stability upon lyophilization and dispersion in cell culture media with or without the addition of fetal bovine albumin (FBS), compared to unconjugated GNRs. PDA-nanoconjugates exhibited a considerable cytotoxicity against DU-145 and PC3 prostate cancer cell lines over a concentration range of 48 μg/mL–12 μg/mL, while they were biocompatible over a concentration range of 3.0 μg/mL–0.185 μg/mL. Furthermore, PDA-nanoconjugates demonstrated possible anti- invasion activity towards prostate cancer cell lines, particularly DU-145 cell line, by reducing cell migration and cell adhesion properties. The PDA-nanoconjugates could be considered a promising nano-platform toward cancer treatment by reducing the invasion activity; it could also be considered a drug delivery system for chemotherapeutic agents

Speaker
Biography:

Himanshu Verma completed her M.Pharm degree in Pharmaceutical Chemistry from the Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, India. She is currently pursuing a Ph.D. in the same department under the supervision of Dr.Om Silakari. She is a senior research fellow in the ICMR fellowship project and works, by using in silico techniques, on designing heterocycles for addressing the problem of resistant cancer

 

Abstract:

Aldehyde dehydrogenase 1 (ALDH1A1), an oxidoreductase class of enzymes, is overexpressed in various types of cancer cell lines and is the major cause of resistance to the Food and Drug Administration (FDA)‐approved drug, cyclophosphamide (CP). In cancer conditions, CP undergoes a sequence of biotransformations to form an active metabolite, aldophosphamide, which further biotransforms to its putative cytotoxic metabolite, phosphoramide mustard. However, in resistant cancer conditions, aldophosphamide is converted into its inactive metabolite, carboxyphosphamide, via oxidation with ALDH1A1. Herein, to address the issue of ALDH1A1 mediated CP resistance, we report a series of benzo[d]oxazol‐2(3H)‐one and 2‐oxazolo[4,5‐b]pyridin‐2(3H)‐one derivatives as selective ALDH1A1 inhibitors. These inhibitors were designed using a validated 3D‐quantitative structure activity relationship (3D‐ QSAR) model coupled with scaffold hopping. The 3D‐QSAR model was developed using reported indole‐2,3‐diones based ALDH1A1 inhibitors, which provided field points in terms of electrostatic, van der Waals and hydrophobic potentials required for selectively inhibiting ALDH1A1. The most selective indole‐ 2,3‐diones‐based compound, that is, cmp 3, was further considered for scaffold hopping. Two top‐ranked bioisosteres, that is, benzo[d]oxazol‐2(3H)‐one and 2‐oxazolo[4,5‐b]pyridin‐ 2(3H)‐one, were selected for designing new inhibitors by considering the field pattern of 3D‐QSAR. All designed molecules were mapped perfectly on the 3D‐QSAR model and found to be predictive with good inhibitory potency (pIC50 range: 7.5–6.8). Molecular docking was carried out for each designed molecule to identify key interactions that are required for ALDH1A1 inhibition and to authenticate the 3D‐QSAR result. The top five inhibitor‐ALDH1A1 complexes were also submitted for molecular dynamics simulations to access their stability. In vitro enzyme assays of 21 compounds suggested that these compounds are selective toward ALDH1A1 over the other two isoforms, that is, ALDH2 and ALDH3A1. All the compounds were found to be at least three and two times more selective toward ALDH1A1 over ALDH2 and ALDH3A1, respectively. All the compounds showed an IC50  value in the range of 0.02–0.80 μM, which indicates the potential for these to be developed as adjuvant therapy for CP resistance.

 

Tamrat Balcha

Department of Pharmaceutics and Social Pharmacy, School of Pharmacy, College of Health Sciences, Addis Ababa University, Ethiopia

Title: In Vitro Evaluation of Native Taro Boloso-I Starch as a Disintegrant in Tablet Formulations
Biography:

Abstract:

In drug delivery, solid dosage forms, of which tablet is the commonest, are still the leading preferences. An area of research focus in tablet drug delivery is the search for tablet excipients. This study was aimed at evaluating and optimizing native Taro Boloso-I starch as a tablet disintegrant. Methods: The response surface methods with central composite design (CCD-RSM) was used for the analysis and optimization of the concentration of native Taro Boloso-I starch and compression force. Wet granulation method was used for the preparation of paracetamol tablets. The response variables considered were tablet crushing strength, friability and disintegration time. Results and Discussions: Both the native Taro Boloso-I starch concentration and compression force had increasing effect on the tablet breaking force. The friability of the tablets was shown to decrease with increasing levels of the disintegrant concentration. On the other hand, compression force had a decreasing effect on friability in the investigated range. The disintegration time of the tablets was found to decrease with the concentration of the starch. The paracetamol tablets prepared with the optimized levels of native Taro Boloso-I starch and compression force showed tablet breaking force of 116.24 N, friability of 0.153%, disintegration time of 1.36 min, disintegration efficiency ratio of 562.3 N /(%Min) and comparative disintegration efficiency ratio 13.6 with respect to commercial potato starch. Conclusions: The tablets exhibited improved crushing strength, friability, in vitro disintegration time and disintegration efficiency ratio which suggest the novel applicability of the native Taro Boloso-I starch as an efficient pharmaceutical tablet disintegrant.

Vijay Kulkarni

Swalava Enterprises Private Limited, India

Title: Twin Screw Continuous Granulation
Speaker
Biography:

Dr. Vijay Kulkarni (M.Pharm, Ph.D) has experience in pharmaceutical industry working on solid oral dosage forms development especially using hot melt extrusion or Twin screw processing for Solubility enhancement of poorly soluble drugs and for continuous Twin Screw Granulation. He has developed various formulations using this technology and transferred the technology to various pharmaceutical industries. He is also a recipient of Rising Star Award in Formulation Development, presented during FDD 2019 Conclave, Hyderabad.  He has 15 years of research experience in pharmaceutical industry and academic research as formulation development scientist. He was a Post-Doctoral research fellow at University of Mississippi, USA working with Prof. Michael Repka

Abstract:

Statement of the Problem:

Pharmaceutical industry has faced increasing pressure to reduce costs due to the competition raised from generics production [1]. This has induced a shift from batch to continuous manufacturing because of several advantages (reduction in development and processing time, equipment size, manufacturing space, costs, quality control and less scale-up problems, increased control and ability to integrate process analytical tools) and due to this there are several initiatives are undertaken by regulatory agencies and pharmaceutical companies [2]. Continuous granulation using twin screw granulation (TSG) has emerged as an alternative to conventional batch granulation [3 & 4] and this is discussed in this presentation with case studies.

Methodology & Theoretical Orientation:

The continuous granulation sequence starts with 1) feeding the material (API+ excipient/s) through feeder (Gravimetric or Volumetric) in the twin screw processor as a premix blend or feeding the individual materials to continuous blender and then to the Twin screw processor, 2) addition of water or binder solution into the processor through pump, 3) mixing or kneading of the powder blend with water or binder solution by the specific configuration of screw elements, 4) drying and sizing inside the processor or through the integrated dryer and mill as shown in Fig 1. The granules and resultant tablets were evaluated for physical-chemical properties.

 

Speaker
Biography:

Dr. Pavitra has his expertise in pharmaceutical nanotechnology and drug evaluation in improving the women health and wellbeing. His pharmacodynamic and pharmacokinetic evaluation model based on osteoporotic wistar rats for improving osteoporotic related disorders is commendable. He has gained this after years of experience in animal model research, drug evaluation, teaching and administration both in research and educational institutions. He has published more than 20 research papers and received national as well as international awards in drug delivery and nanotechnological based research

Abstract:

Statement of the Problem: Osteoporosis emerged as a chronic disease of skeleton system leading to weaken bones and hip fractures making it a burden to the society. During lifetime, one out of every three women and one out of every six males will experience an osteoporotic fracture. Every minute, eight new fracture cases are reported in the EU. In the European Union, it is projected that over 23 million men and women are at high risk of osteoporotic fractures. According to estimates from 2019, osteoporosis and the 4.3 million fragility fractures it generates cost Europe's health-care systems more than €56 billion every year.  Methodology: A nano complex tagged pamidronate was prepared with hot-micro-emulsification and ultrasonication method. The prepared formulation was characterized for particle size, zeta potential, in-vitro drug release, ex-vivo gut permeation and in-vivo anti osteoporosis activity. Size of nanoformulation was further confirmed by TEM. Bone mineral density of wistar rat femur was determined using micro-computed tomography and bone mechanical strength was determined with universal testing machine. Clinical findings: The oral bioavailability and permeability was enhanced by 37.56 % and 152.71% respectively. Bone mineral density was enhanced in female wistar rat models by 25.81 % compared to marketed formulation. Bone strength was enhanced by 19.22 % Conclusion & Significance: Bisphosphonates are the primary therapeutic agents for treating osteoporosis but very low oral bioavailability limits their use. In this paper, a novel approach was utilized to develop orally applicable nanoformulation with significant oral bioavailability to reduce injection and cost burden to the society. This research will be of great interest in further studies with significant outcomes to treat post-menopausal osteoporosis in women.

 

Gaurav

Ph.D Scholar, Delhi Pharmaceutical Science and Research University, India

Title: In vivo Assessment of Scalp Retention and Penetration of Minoxidil Solutions using Scintigraphy
Speaker
Biography:

Mr. Gaurav is a nanomedicine researcher who focuses on alopecia and its treatment. He has two years of experience 3D printing tablets and is interested in developing novel Alopecia treatment solutions. He has worked in both hospitals and educational institutions, doing research and evaluating drug and delivery systems. His strategy is unique, and his execution is as effective.

 

Abstract:

Background: Efficacy of minoxidil for the treatment of androgenetic alopecia has been demonstrated through several clinical studies, however scalp retention and penetration, which is imperative for application frequency, has not been determined till date.

Methods: The scalp retention and penetration of the three radiolabeled minoxidil (5%) formulations: Formulation A (40% alcohol and 60% water); B (30% alcohol, 10% PG and 60% water) and C (40% alcohol, 10% HPC and 60% water) were prepared. Ex vivo retention, penetration and permeation was conducted using swine ear skin and in vivo scalp retention and penetration of the formulations was evaluated in human participants with male pattern baldness using scintigraphy.

Results: Minoxidil radiolabeling efficiency of 99.1% was observed when 0.2% stannous chloride was used as reducing agent at pH 6 and incubation temperature of 40°C. Results showed that formulation C containing 10% HPC demonstrated highest viscosity (0.8 Pa.s) and significantly higher ex vivo retention (p < 0.05) and permeation (0.75±0.12%, 8h) compared to Formulation A (0.40±0.05%, 8h) and B (0.44±0.05%, 8h). In vivo studies using human scalp showed significantly higher (p < 0.05) scalp retention in FC group (57±2.3%) compared to FA (41±1.9%) and FB (44±3.4%) group. Post 8 h application of formulation, scalp penetration in FC group was nearly 2.8-fold and 2.2-fold higher than group FA and FB, respectively. Further, absence of minoxidil in systemic circulation during study duration indicates safety.

Conclusions: In conclusion, increasing the contact time of formulation with scalp by modifying viscosity might result in reduced frequency of application and improved efficacy.

 

Day 2 :

Biography:

Dr. Lee is Executive Vice President of Pharmaceutical Development Services at Particle Sciences, a Lubrizol Advanced Materials, Inc. company, a pharmaceutical contract development and manufacturing organization (www.particlesciences.com). He provides direction and is involved with product and business development. Before joining Particle Sciences, Rob held senior management positions at Novavax, Inc., Lyotropic Therapeutics, Inc., and Imcor Pharmaceutical Co. He holds BSs in Biology and Chemistry from the University of Washington and a PhD in Physical Bioorganic Chemistry from the University of California, Santa Barbara. Rob has published articles in numerous peer-reviewed journals and five book chapters plus holds over two dozen issued patents or provisional patent applications.

Abstract:

Many active pharmaceutical ingredients are poorly water soluble and may suffer from low oral bioavailability, if formulated in unmodified form.  These compounds are also challenging to formulate for other routes of administration, especially parenteral.  The prevalence of low solubility compounds has led to intensive research and has generated many technologies to address formulation.  For BCS II molecules, there are other drug delivery approaches besides nanoparticulate suspensions (NSs) used for oral administration but many feel the higher value of this technology is for parenteral delivery.  This technology has been used for several marketed products including oral tablets, oral liquid NSs, and parenteral liquid NSs.  There continues to be a strong interest in employing NS formulations, particularly for parenteral dosage forms.  An overview of the history and product development of NSs with an emphasis on sterile products will be presented

I look forward to the meeting.  It looks like my talk may be appropriate for tracks 1, 5, 6, and 9 – probably track 6 may be the best fit.  Please get back to me as soon as possible on what session, date, and time my presentation is scheduled for along with when I need to be there to chair my session (and what session).  Let me know if you need any additional information.  Once I know what date my session is, I’ll make my hotel reservations.

Biography:

Nélio Drumond is a PharmD by training with a PhD in Patient Centric Drug Product Design. He shares several years of experience in the Pharmaceutical Industry, providing scientific leadership to govern the formulation and manufacturing strategies for drug product development programs during clinical stages, including their scalability and validation for commercial use. Currently, Dr. Drumond is responsible for the technical management and leadership of commercial manufacturing activities at different Contract Manufacturing Organizations (CMOs) for an established portfolio of Takeda products within the EMEA region.

Abstract:

Oral drug administration provided as solid oral dosage forms (SODF) remains the major route of drug therapy in primary and secondary care. There is clear evidence for a growing number of clinically relevant swallowing issues (e.g., dysphagia) in the older patient population, especially when considering the multimorbid, frail, and polymedicated patients. Swallowing impairments have a negative impact on SODF administration, which leads to poor adherence and inappropriate alterations (e.g., crushing, splitting). Different strategies have been proposed over the years in order to enhance the swallowing experience with SODF, by using conventional administration techniques or applying swallowing aids and devices. Nevertheless, new formulation designs must be considered by implementing a patient centric approach in order to efficiently improve SODF administration by older patient populations. Together with appropriate SODF size reductions, innovative film coating materials that can be applied to SODF and provide swallowing safety and efficacy with little effort being required by the patients are still needed. Scientific evidence demonstrating the benefits of given SODF coating materials in the concerned patient populations are still very limited. Consequently, the availability for safe, effective, and clinically proven solutions to address the increasing prevalence of swallowing issues in the older patient population are still limited.

Keynote Forum

Syed H Askari

Maculus Therapeutix, USA

Keynote: Medical Devices as Tools for drug delivery: Challenges and opportunities

Time : 10:35 - 11:15

Biography:

Syed Askari, PhD, is the Founder, President and CEO of Maculus Therapeutix, an ENT medical device/drug delivery company. Previously he founded Medicus Biosciences, and launched two wound healing products, SutureSeal and HyFlex.Syed holds more than 25 patents/patents applications. Syed has a PhD in Organic Chemistry from the University of British Columbia and has completed his post doctoral work at UCLA and UCSB under Prof Wudl and Prof Heeger Nobel Laureate (year 2000) labs.

Abstract:

Medical device with drug delivery technology has improved over the last 20 years to address issues with ease of application or implantation, biocompatibility, durability, bioabsorbability and drug dosage control. These developments have been applied to stents and lenses, heart valves and seats, vascular stents and shunts, hemostasis and embolization, post-surgical closure, liquid bandages, and other areas. The devices have also been used as drug delivery vehicles. New technologies must be tailored to the target physiologic environment since materials that function well in one environment may fail in another. Research has brought about a much greater understanding of the importance of the surfaces of medical devices in terms of the reaction to contact with bodily fluids and tissues, and novel materials have been developed that resist attachment to cells, platelets, calcium deposits, etc.  Overall, greater understanding of the specific environment in which a device will be deployed leads to more reliable, durable and functional designs with fewer complications over time. This talk will explore some of the advancements in polymer chemistry and hydrogel-based materials and how these technologies have been applied to medical devices and drug delivery in numerous settings. Significant challenges remain in the medical device and delivery arena, and potential future advancements will be discussed.

  • Sessions on: Advances in Drug Delivery Systems | Pharmaceutical Research | Drug Discovery

Session Introduction

Kuldeep K. Bansal

Pharmaceutical Sciences, Laboratory, Faculty of Science and Engineering, Ã…bo Akademi University, Finland

Title: Novel polymers with functionalities from renewable feedstock for smart drug-delivery
Speaker
Biography:

Dr. Kuldeep Bansal obtained his PhD in pharmacy discipline from the University of Nottingham in 2015 after receiving basic degree in pharmacy from India. As of 2017, he has been working in the lab of Prof. Rosenholm and has been developing novel polymers for drug delivery applications. His previous research mostly involved synthesis of polymers-based nanocarriers for enhancing safety, efficacy, and stability of drugs. His current bibliographic data includes 29 published papers, >700 citations and h-index 14 (Google Scholar 21.7.2022).

 

Abstract:

Polymer-drug conjugates with stimuli-sensitive linkers (smart polymer therapeutics) have demonstrated superior efficacy in targeted drug delivery. However, ongoing research is lacking in the simplicity of design and broad applicability of single polymeric material. Limited functional groups on polymers, tedious synthesis methodology, non-renewable monomer source, reproducibility, etc. are a few hurdles, which still need to be addressed to enhance the applicability of polymers in smart drug delivery. With the objective to circumvent these hurdles, we have recently reported the synthesis of a novel amphiphilic block copolymer (mPEG-b-PJL) using renewable jasmine lactone monomer under mild reaction conditions. The functional groups, such as -COOH, -NH2, -OH and aromatic ring were later introduced to the polymer via facile thiol-ene click reaction. As a proof of concept, doxorubicin (DOX) was conjugated to the hydroxyl terminated polymer [i.e., mPEG5k-b-PJL3k-(OH)24] via a disulfide linkage to generate PJL-DOX. It was expected that PJL-DOX release the higher drug in cancer cells due to the presence of excessive glutathione (a reductive agent). Further, the -COOH functional polymers were also analysed for their capability to increase the aqueous solubility of hydrophobic drugs by fabrication of polymeric micelles.

The PJL-DOX containing 30 wt% of DOX was readily self-assembled into micelles with an average hydrodynamic size of ~150 nm. The in-vitro cytotoxicity of PJL-DOX suggested redox triggered DOX release, while no significant toxicity was observed for polymer alone. In-vivo results suggested intermediate tumour inhibition activity of PJL-DOX compared to free DOX and marketed liposomal DOX formulation. However, the PJL-DOX demonstrate lesser side effects and increased mice survivability.

Further, the -COOH terminated polymer demonstrate high drug loading of weakly basic drugs, indicating that functional groups on polymer have a direct impact on loading in polymeric micelles. These polymers can be explored further to prepare nano-sized drug conjugates for targeted delivery, theranostics and/or combined delivery of bioactives. In addition, tuning of free functional groups can further enable their applications in polymeric micelles with high drug loading, which is otherwise hamper the clinical translation of micelles-based drug delivery system.

 

Yogeshwar Bachhav

AiCuris Anti-infective Cures GmbH, Germany

Title: Complex parenteral formulations

Time : 11:45-12:00

Speaker
Biography:

Dr. Yogeshwar Bachhav is associated with AiCuris Anti-infective Cures GmbH Wuppertal (Germany) for around 9 years. AiCuris (name derived from 'anti-infective cures') is focused exclusively on the discovery, research and development of novel antiviral and antibacterial drugs.

Yogeshwar has around 16 years of experience in Pharmaceutical development (CMC) of poorly soluble/stable  drugs for oral, parenteral and topical route from the start-up and mid-size Pharmaceutical companies in Europe. In his current role at AiCuris, he is responsible for the outsourcing of drug product for preclinical and clinical trials up to phase II. His experience involves both in house and external Pharmaceutical development of poorly soluble/labile APIs for oral parenteral and topical route.

 

Abstract:

The present talk will focus on the CQAs of parenteral formulations including but not limited to    pH, osmolality, drug load, absence of excipients with irritation potential, absence of precipitation upon injection. Other alternative options to develop parenteral formulations of poorly soluble drugs or difficult to formulate drugs such as Cyclodextrins (Captisol, HPBCD),  Liposomes,   Mixed micelles/miceller solutions (use of surfactants),  Intralipid emulsion, Nanosuspension will also be discussed. Author will also present some case studies involving difficulty  in formulating parenteral formulation od complex compounds such as potent/cytotoxic drugs (case studies) e.g. anticancer drugs and Penicillin or cephalosporin type of compounds.

 

Baddipadige Raju

Molecular Modeling Lab, Department of Pharmaceutical Sciences and Drug Research, Punjabi University, India

Title: Multiple machine learning, molecular docking, and ADMET screening approach for identification of selective inhibitors of CYP1B1
Speaker
Biography:

Baddipadige Raju completed his M. S. (Pharm.) degree in Pharmacoinformatics from the National Institute of Pharmaceutical Sciences and Drug Research (NIPER), Mohali, Punjab, India. He is currently pursuing a Ph.D. in Medicinal Chemistry from the Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab, India, under the supervision of Dr. Om Silakari. He is a senior research fellow in the ICMR fellowship project and works, by using in silico techniques, on designing heterocycles for addressing the problem of Drug metabolizing enzymes medicated Anticancer drug resistance.

 

Abstract:

Cytochrome P4501B1 is a ubiquitous family protein that is majorly overexpressed in tumors and is responsible for biotransformation-based inactivation of anti-cancer drugs. This inactivation marks the cause of resistance to chemotherapeutics. In the present study, integrated in-silico approaches were utilized to identify selective CYP1B1 inhibitors. To achieve this objective, we initially developed different machine learning models corresponding to two isoforms of the CYP1 family i. e. CYP1A1 and CYP1B1. Subsequently, small molecule databases including ChemBridge, Maybridge, and natural compound library were screened from the selected models of CYP1B1 and CYP1A1. The obtained CYP1B1 inhibitors were further subjected to molecular docking and ADMET analysis. The selectivity of the obtained hits for CYP1B1 over the other isoforms was also judged with molecular docking analysis. Finally, two hits were found to be the most stable which retained key interactions within the active site of CYP1B1 after the molecular dynamics simulations. Novel compound with CYP-D9 and CYP-14 IDs were found to be the most selective CYP1B1 inhibitors which may address the issue of resistance. Moreover, these compounds can be considered as safe agents for further cell-based and animal model studies.

 

Biography:

Muhammad Muzamil Khan is a PhD research Scholar at Northeastern University, Boston, USA. He is working now on Folate-targeted
Lipid-polymer Hybrid Nanoparticles for the targeted and controlled delivery of cisplatin for effective treatment of ovarian cancer. He is
interested in Co- delivery of siRNA and chemotherapeutic agents for the effective treatment of cancer.

Abstract:

Lipid-Polymer Hybrid Nanoparticles (LPHNP) are novel delivery systems for controlled drug delivery at tumor sites. The superior biocompatible properties of lipid and structural advantages of polymer can be obtained via this system for controlled drug delivery. In the present study, cisplatin- loaded lipid-chitosan hybrid nanoparticles were formulated by the single step ionic gelation method based on ionic interaction of positively charged chitosan and negatively charged lipid. Formulations with various chitosan to lipid ratio were investigated to obtain the optimal particle size, encapsulation efficiency and controlled release pattern. Transmission electron microscope and dynamic light scattering analysis demonstrated a size range of 181-245 nm and a zeta potential range of 20-30 mV. Compatibility among the components and the stability of formulation were demonstrated with FTIR analysis and thermal studies, respectively. The therapeutic efficacy and cellular interaction of cisplatin-loaded LPHNP were investigated using in vitro cell-based assays in A2780/ADR ovarian carcinoma cell line. Additionally, the cisplatin loaded LPHNP exhibited a low toxicity profile in rats. The in-vivo pharmacokinetics study also proved a controlled delivery of cisplatin with enhanced mean residual time and half-life. Our studies suggested that the cisplatin- loaded LPHNP being a promising platform for controlled delivery of cisplatin in cancer therapy.

Gera Narendra

Molecular Modeling Lab, Department of Pharmaceutical Sciences and Drug Research, Punjabi University,Punjab, India

Title: Molecular Docking, Dynamics, and WaterSwap Analysis to Identify Anti aggregating Agents of Insulin and IFN β
Speaker
Biography:

Gera Narendra completed his M. S. (Pharm.) degree in Pharmacoinformatics from the National Institute of Pharmaceutical Sciences and Drug Research (NIPER), Mohali, Punjab, India. He is currently pursuing a Ph.D. in Medicinal Chemistry from the Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab, India, under the supervision of Dr. Om Silakari. He is a senior research fellow in the ICMR fellowship project and works, by using in silico techniques, on designing heterocycles for addressing the problem of Drug metabolizing enzymes medicated Anticancer drug resistance.

 

Abstract:

There are several challenges in the development, and formulation of biologics, particularly concerning their physical stabilities. The self-assembly of peptides like human insulin and interferon beta (IFN-β) has potential to form aggregates in pharmaceutical formulation. Therefore, it is a significant problem in the manufacturing, storage, and delivery of insulin and IFN-β formulations. Amino acids as aggregation suppressing additives have been used to stabilize proteins during manufacturing and storage. Several changes to the B chain’s C-terminus have been proposed in an attempt to improve insulin formulation. The core segments of the A and B chains (SLYQLENY and LVEALYLV) have recently been identified as sheet-forming areas, and their microcrystalline structures have been exploited to construct a high-resolution insulin amyloid fibril model. Here, we have chosen twenty-one amino acids to develop as additives in rendering the insulin and IFN-β aggregations. Thereafter, integrated molecular docking studies of single layer monomers of full-length insulin and IFN-β have been performed to identify structural elements (amino acids) that can act as disaggregating agents. The stability of the best-docked amino acid complexes was judged using molecular dynamics studies. Finally, phenylalanine was identified as a disaggregation agent for insulin, and lysine, tyrosine, phenylalanine, and tryptophan were identified as disaggregation agents for IFN-β from the molecular dynamics study. These findings may open a novel proposal to explore further in vitro studies to increase the stability of the insulin and IFN-β formulation.