Oral Delivery of Biologics
Thursday, February 6 2014
8:00 am – 10:00 am
Location: MassBio, 300 Technology Square, 8th Floor, Cambridge, MA
Peptide and protein-based drugs are typically administered parenterally and display poor oral bioavailability due to enzymatic degradation and poor penetration through the intestinal membranes. Significant progress has been achieved in the past few decades regarding macromolecular drug absorption from the GI tract, including the barriers that restrict related absorption. Various strategies have been pursued to overcome such barriers and to develop safe and effective oral delivery systems for biologics. This Forum will review the latest advances in the field achieved by two of the industry’s leading practitioners of the art.
“Oral Delivery of Peptides - Modular Drug Delivery” by Dr. Thomas Tice, Senior Director, Evonik Corp.
Modular Drug Delivery (MDD) is a proprietary technology designed to increase the oral bioavailability of peptides and other biopharmaceuticals. It is a microparticle-based technology using existing, orally acceptable materials and prepared using common manufacturing processes. Various functional components (modular components) can be placed into MDD microparticles to target each peptide to its most permeable area of the gastrointestinal tract, hold the formulation in place during peptide release, protect the peptide from proteases and enhance permeability. The incorporation of these functional components into MDD and in vivo data will be presented.
“Oral peptide delivery-Emerging technologies and continuing challenges” by Dr. Anand Subramony, Principal Fellow & Head, Novel Drug Delivery Technologies & Therapeutics, Novartis Institutes for BioMedical Research, Technical R&D
Delivering macromolecules via the oral route is very challenging given the poor permeability and/or stability of peptides in the GI tract. However needle phobia is a continuing problem of administration of macromolecules since parenteral delivery is the standard of care. There is a large potential benefit to health outcomes through improved patient compliance if we are successful to deliver macromolecules via the oral route. Peptide based therapeutics are emerging in the “synthetic biologics” space for a wide range of indications, making the need for an oral delivery option for peptides more pressing.
Numerous approaches have been explored over the past 20 years to facilitate oral delivery of peptides and proteins. These approaches include use of permeation enhancers,, nanoparticles, conjugation to peptide uptake sequences , or chemical modification with lipids or PEG to enhance permeability. Unique configurational aspects of dosage forms via enteric coating and keeping the excipient and active together may also play in role in improving the bioavailability.
Formulation screening tools and case studies of early pre-clinical research of oral delivery of representative peptides using emerging delivery technologies will be presented.
This Forum is presented by the Formulation and Drug Delivery Forum Working Group.
Anand Subramony PhD, Principal Fellow & Head, Novel Drug Delivery Technologies & Therapeutics, Novartis Institutes for BioMedical Research, Technical R&D
Anand Subramony is a principal fellow and head of the Novel Delivery Technologies & Therapeutics program at Novartis. In his role he focusses on innovation and identifies emerging drug delivery technologies for unmet medical needs and aligns them with internal pipeline compounds for feasibility studies to generate proof of concept data. His portfolio of activities includes leading a cross functional team of scientists, clinicians and formulators to develop novel therapies across different disease indications and using various routes of administration. Some of his key areas of focus involves oral delivery of peptides, evaluation of nanotechnology based formulations for drug targeting to tissues/tumors, novel devices for high volume biologics delivery, technologies for solubility improvement of poorly water soluble drugs, and overcoming BBB via novel formulation and device approaches.
Before his current role Anand lead the Materials Research group at Alza Corporation/Johnson & Johnson where he focused on drug delivery technologies across various trans-mucosal interface (including iontophoresis, microporaton technologies and drug delivery to the back of the eye) and was also the Director of Center of Excellence for Materials Science & Drug delivery devices at Dr. Reddy’s Laboratories. Prior to these roles, Anand worked at the University of Washington, Seattle and Applied Materials in Santa Clara, CA in various capacities.
Anand holds an MS in Materials Sc. & Engineering from IIT Bombay and Ph.D. from Purdue University, West Lafayette, IN.
Thomas R. Tice, PhD, Senior Director, Technical Global Marketing, Evonik Corporation
Dr. Tice is internationally recognized for research in drug delivery of biologics and small molecules, and has lectured on the topic throughout the world. His specialties include microencapsulation, implants, controlled release and medical applications of bioabsorbable polymers. In particular he is known for his accomplishments involving injectable, extended-release microparticles made with bioabsorbable lactide/glycolide polymers designed to release pharmaceuticals. He led the team that developed the first commercial, injectable microparticle product, which was a one-month LHRH formulation indicated for the treatment of prostate cancer (Decapeptyl® SR) and is still on the market today. Dr. Tice earned his PhD in Biophysics from Syracuse University, New York. He holds 34 US patents with numerous foreign equivalents and has more than 180 publications, presentations and invited lectures to his credit. He currently serves on the Boards of McWhorter School of Pharmacy at Samford University and serves on the United States Pharmacopeia General Chapters-Dosage Forms Expert Committee.