|
|
Oral Delivery | | | | | | Technology | | Apollo's Oradel™ technology has considerable potential to deliver biopharmaceuticals that have traditionally been administered by injections. By combining the ability to protect the therapeutic protein from the harsh stomach environment and to actively promote transport of the drug into the bloodstream, the Oradel™ technology may usher in a new era of convenient, needle-free biopharmaceutical drug administration. Oral delivery systems convey drugs in a way that many patients prefer over other delivery forms including injection, inhalation, implants, transdermal and buccal. It is particularly preferred over injections when a drug needs to be repeatedly administered over a period of months or years, as for diabetes or multiple sclerosis. Apollo's proprietary oral delivery platform technology (Oradel™) allows the uptake of a protein, such as insulin, from the gut into the bloodstream in an active form through the use of small molecule transporters, and protects the proteins from stomach enzymes. Apollo has filed provisional patents on the new oral delivery formulation, following promising in vitro results and pre-clinical experiments with a range of proteins up to antibody size and antibodies. Newer generation biopharmaceutical drugs based on proteins, previously considered unsuitable for oral delivery, have been identified as potential candidates for Oradel™. Apollo will also use its own proteins produced from human cells to develop convenient and more effective treatments for diseases ranging from rheumatoid arthritis and hepatitis C to multiple sclerosis and cancer. Apollo has initiated pre-clinical efficacy studies on oral delivery of peptides and proteins. "Proof of concept" for Oradel™ has been demonstrated at preliminary scale-up levels in pre-clinical studies. The initial application of oral delivery technology is insulin tablets for diabetes, which will be the first of Apollo's oral drugs to enter clinical trials. A Scientific Advisory Board for diabetes has been appointed, chaired by Professor Paul Zimmet, a leading international diabetes expert and Foundation Director of the International Diabetes Institute. Associate Professor Jonathan Shaw and Dr Matt Cohen from the International Diabetes Institute are also members of the Advisory Panel.
I am delighted to be involved in Apollo's research on oral delivery of proteins, with potential application for insulin. Diabetes is growing at an alarming rate worldwide and will probably be the largest epidemic Australia has ever experienced. The potential to deliver insulin orally has always been a high priority in diabetes research - it has been considered the 'holy grail' of diabetes treatment. Professor Paul Zimmet |
Top | | Benefits of Apollo’s oral formulation | | Apollo's oral delivery platform represents a significant improvement in treatment from the patient's point of view. Apollo's Oradel™ technology offers increased convenience, increased patient compliance, and reduced overall health costs. There is significant potential to develop this targeted platform in major global markets. A key commercial application is the technology's potential to deliver biopharmaceuticals such as interferon, growth hormones or TNF blockers (typically dispensed by needles) in oral or tablet form. Most biopharmaceuticals, which represent a rapidly growing proportion of new therapeutics, must currently be injected, because they are not well suited for the oral route. When taken orally, these large, water-soluble molecules are either digested in the stomach or passed down the intestine unabsorbed and end up in the bowel. Apollo's technological advances have made it possible for such proteins to enter the bloodstream from the stomach, and have exciting potential to revolutionise the biopharmaceutical industry. Oradel™ will make it easier and less painful to take prescribed medications for many chronic autoimmune and inflammatory diseases, cancer and cardiac conditions. Oradel™ can apply to generic medications such as insulin, as well as to Apollo's human-expressed proteins including interferon, erythropoietin, G-CSF and TNF blockers.
Top | | Competitive advantage of Apollo’s oral delivery technology | | Many patients would prefer the pain-free convenience of oral drugs compared to more invasive methods of medication. However, with very few exceptions, effective quantities cannot be delivered in an oral form for recently developed protein and antibody-based biopharmaceuticals. Most oral delivery technologies for therapeutic large water-soluble proteins have failed to overcome two major obstacles to effective oral delivery: - Degradation of the protein by the harsh stomach environment
- Poor absorption of the protein through the gut wall into the bloodstream
By overcoming these hurdles, Apollo's Oradel™ represents a major advancement in protein delivery.
| | Degradation | | The high acid content and enzymes of the digestive tract can degrade most peptide and protein pharmaceuticals before they are absorbed into the bloodstream. The Oradel™ technology stabilises the drug molecule within a structure that protects the biopharmaceuticals protein from being broken down by the stomach's enzymes. Degradation will be further reduced by formulating the Oradel™ pharmaceuticals in solid dosage forms such as tablets and capsules that dissolve in the small intestine, not the stomach. By contrast, most oral delivery devices have focused on protecting the drug within the gastro-intestinal tract.
| | Poor Absorption | | Many large molecules are highly charged, water-soluble compounds that are poorly absorbed through biological membranes such as those lining the intestine. The Oradel™ technology overcomes this issue by actively promoting the transport of biologic drugs across the gut-lining barrier. Oradel™ consists of specific targeting agents, which bind to specific naturally occurring transporters embedded in the intestinal wall. Binding to these transporters promotes the uptake of the Oradel™-pharmaceutical unit so that the unit crosses the intestinal wall and enters the circulation. Once in the circulation the Oradel™ structures break down, allowing the biologic drug to enter the circulation.
|
Top | |
|