The safety and efficacy of protein and peptide therapeutics are limited by in vitro and in vivo instability, immunogenicity and short circulating half-lives. CHI's Inaugural Formulation Strategies for Improved Delivery of Biologics conference will discuss new formulation approaches designed to overcome biologics delivery issues through as chemical modifications, new formulations and delivery technologies and advanced analytical tools to characterize protein interactions with excipients. These strategies have the potential to facilitate the development of next generation peptide and protein therapeutics which are safe, efficacious and promote patient compliance.
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SUNDAY, MAY 4
9:00 am – 4:00 pm Pre-Conference Registration
10:00 am – 1:00 pm Short Course 1: Challenges and Opportunities in Protein and Peptide Drug Delivery*
2:00 – 5:00 pm Short Course 2: Converting Emerging Delivery Technologies into Successful Patient-Friendly Therapies*
*Separate registration required.
MONDAY, MAY 5
7:00 am Registration and Morning Coffee
8:30 Chairperson’s Opening Remarks
Christopher A. Rhodes, Ph.D., President, Christopher A. Rhodes & Associates LLC
8:40 KEYNOTE PRESENTATION: The Growing Role of BioTherapeutics Delivery: Opportunities and Challenges
Julia Rashba-Step, Ph.D., Senior Director, Novel Delivery Technologies, Pfizer, Inc.
There is a rapidly changing environment with the constantly growing role of Biotherapeutics. The presentation will cover thoughts on the future trends on BioTherapeutics and importance of drug delivery in commercial, clinical differentiation and also the need for enabling technologies. Also it will also cover strategic plans for current and future delivery reflective of needs of Pfizer’s BioTherapeutics portfolio.
9:10 Strategies and Consideration for Developing Parenteral Protein Device Combination Products
Sujit K. Basu, Ph.D., Senior Director, Global Technical Operations, Shire
This talk will discuss various considerations and strategies for developing innovative injectable delivery technologies. Examples will be drawn from our intrathecal delivery programs to discuss role of new approaches such as protein device combinations in successfully delivering injectable biotherapeutics.
9:40 Site-Specific Antibody Modification to the Conserved Nucleotide Binding Site (NBS): Effects on Formulation and Delivery of Advanced Therapeutics
Nathan J. Alves, Ph.D., Post-Doctoral Research Fellow, Indiana University School of Medicine, Indiana
Next generation pharmaceutical antibodies that utilize complex conjugation strategies to endow antibodies with various unnatural functional groups brings new challenges, as well as opportunities, to advance drug delivery formulations with hopes of improving therapeutic efficacy. This talk will discuss some critical aspects to consider when producing antibody conjugates and will draw specifically upon an example of site-specific antibody conjugation through UV crosslinking of functional ligands to the highly conserved antibody NBS.
10:10 Grand Opening Coffee Break in the Exhibit Hall with Poster Viewing
11:10 Preventing Aggregation of Therapeutic Peptides
Morten J. Maltesen, Ph.D., Project Manager, Biopharma Application Development, Novozymes Biopharma
The inherent instability of peptides imposes significant challenges on the process and formulation development of peptide based drugs. Overcoming these challenges and developing stable peptide formulations is a major task. One novel approach is to use recombinant human serum albumin (rAlb) as a formulation excipient to stabilize peptides in solution. In this study, we will show the stabilizing properties of rAlb on selected peptide therapeutics from the market.
11:40 Microfluidics-Assisted Engineering of Protein Formulations
Sabiruddin Mirza, Ph.D., Sr. Research Associate, School of Engineering and Applied Sciences, Harvard University
Protein-based therapies hold an enormous potential for treating many terminal diseases. Nevertheless, the lack of universal technological approaches that enable development of protein formulations with the targeted attributes significantly impedes clinical translation of these advanced therapies. This presentation will overview the use of droplet based microfluidic technology for developing protein formulations with pre-programmed functional characteristics, including size and internal morphology, encapsulation efficiency, and protein release profile.
12:10 pm Luncheon Presentation (Opportunity Available) or Enjoy Lunch on Your Own
12:55 Session Break
2:00 Chairperson’s Remarks
Frank Tagliaferri, Ph.D., Vice President, R&D, 4P Therapeutics
2:05 Lyophilized siRNA Nanosome Formulation
Tarun Mandal, Ph.D., McCaffrey/Norwood Endowed Professor of Pharmacy & Director, Center for Nanomedicine & Drug Delivery, College of Pharmacy, Xavier University of Louisiana
Sequence specific gene silencing based on RNA interference (RNAi) holds great promise for molecular-targeted treatment of various diseases. However, delivery of siRNA presents a special challenge due to its rapid in vivo degradation, large molecular weight, and polyanionic charge. In this study, cationic lipid (DOTAP)-based non-toxic formulations were developed for the treatment of HCV.
2:35 Highly-Automated Procedures for the Assessment of Protein Formulations
Russell G. Burge, Ph.D., Application Scientist, Freeslate, Inc.
A highly automated process was devised to prepare and analyze samples for the formulation development of proteins. Automation increased efficiency of the activities compared to current methods and procedures. Forty eight protein formulations were generated together with placebos. Automated procedures were employed for appearance (color, turbidity, and particles),viscosity, and pH testing. Spectrophotometry, chromatography and light scattering were performed using semi automated procedures. Performance of the formulations was evaluated after subjecting the vials to stress conditions.
3:05 Protected Peptide Nanoparticles: Experiments and Brownian Dynamics Simulations of the Energetics of Assembly
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Robert K. Prud’homme, Ph.D., Professor and Director Program in Engineering Biology, Department of Chemical & Biological Engineering, Princeton University
Soluble peptides, susceptible to degradation and clearance in therapeutic applications, have been formulated into protected nanoparticles for the first time through the process of kinetically-controlled, block-copolymer-directed rapid precipitation using Flash NanoPrecipitation. Complimentary Brownian dynamics simulations qualitatively model the nanoparticle formation process. Additionally, the influence of the polymer-peptide interaction energy on the efficiency of nanoparticle protection by polymer surface coverage is elucidated in both experiments and simulations. Approaches to encapsulate, and protect more soluble polypeptide constructs using conjugation strategies will be presented.
3:35 Prefilled Syringe Technologies for Improving Drug Stability and Reliable Plunger Performance for Auto-Injectors Applications
Kevin Constable, Director, Technology Development, Global Pharmaceutical Solutions, Terumo Medical Corporation
4:05 Refreshment Break in the Exhibit Hall with Poster Viewing
4:45 Problem Solving Breakout Discussions
This interactive session provides conference delegates and speakers an opportunity to choose a specific roundtable discussion group to join. Each group has a moderator to ensure focused discussions around key issues within the topic. This format allows participants to network, meet potential collaborators share examples from their work, vet ideas with peers, and be part of a group problem-solving endeavor.
Topic 1: Screening and Optimization of Biological Formulations
Moderator: Russell Burge, Ph.D., Application Scientist, Freeslate, Inc.
• What are the most effective and efficient studies and methods for formulation screening?
• How representative are screening results from 96-well formats of those in the final container-closure, such as PFS or vials?
• How and when should a container closure be selected for formulation studies of a drug product?
Topic 2: Challenges in Topical and Transdermal Drug Delivery
Moderator: Ajay K. Banga, Ph.D., Professor and Department Chair, Pharmaceutical Sciences, Endowed Chair in Transdermal Delivery Systems, College of Pharmacy, Mercer University
• Human skin as an in vitro surrogate model for bioequivalence comparison of topicals
• Challenges in passive patch development: Residual drug, crystallization, and cold flow
• Challenges in getting proteins and vaccines across the skin – limitations of iontophoresis and microneedles
Topic 3: Commercial Biological Products without Cold Chain Management?
Moderator: Weiguo Dai, Ph.D., Scientific Director, Fellow, Drug Product Development, Johnson & Johnson
• What is the biggest benefit for “room temperature controlled” biologics? Saving money in cold chain management vs. patient convenience?
• Challenges and current approaches in developing “room temperature controlled” biologics
Topic 4: Understanding Toxicity of Polymer-Based Nanocarriers for Drug Delivery
Moderator: Pirouz Daftarian, Ph.D., Assistant Research Professor, Department of Biochemistry and Molecular Biology, University of Miami Miller School of Medicine
• What are the proper pre-clinical toxicity tests / biomarkers / analytes that ensure a proactive approach for dissecting the toxicity of polymer-based nanocarriers?
• What is the acute and chronic spectrum that guarantees undesired reactions?
Topic 5: Challenges in Treatment of Brain Diseases
Moderator: Reinhard Gabathuler, Ph.D., Chief Scientist, biOasis Technologies, Inc.
• How do we overcome blood brain barrier and what technologies are available for drug delivery to brain?
• Intrathecal injection versus i.v injection: Which one is better and when?
• Delivery across blood brain barrier- Challenges posed by small molecules and biologics
• Is intracellular delivery of a drug addressed in its design and therapeutical efficacy?
Topic 6: Prefilled Syringe Technologies: Improving Drug Stability and Auto-Injector Performance
Moderator: Kevin Constable, Director, Technology Development, Global Pharmaceutical Solutions, Terumo Medical Corporation
• Minimizing degradation
• Control of dissolved oxygen
• Functional performance in Auto-Injector
5:45 Welcome Reception in the Exhibit Hall with Poster Viewing
6:45 End of Day
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