Sydney, Sep 25, 2006 AEST (ABN Newswire) - Apollo Life Sciences (ASX: AOP) announces it has achieved a major breakthrough by successfully lowering blood glucose levels in diabetic rats with oral insulin, using its proprietary oral delivery technology, Oradel TM . This makes needle-free insulin for diabetes treatment now possible.
Currently, people with diabetes can require up to 1,500 insulin injections a year to manage their condition. Diabetes affects almost 1 million Australians, and 100,000 people develop the disease annually.
Results from a series of preclinical studies indicate that Apollo's oral delivery technology, Oradel TM, successfully delivers generic insulin to diabetic rats, significantly lowering blood glucose levels for a sustained period of time with a single dose. Oral feeding of diabetic rats with Oradel TM insulin resulted in reduction in blood glucose levels in responder animals of up to 80%, which persisted for longer than 6 hours. In these studies, the oral insulin formulation was administered once daily to diabetic rats, and blood glucose levels were measured at one- or two-hour intervals over an extended period. This animal model is considered robust for testing the efficacy of diabetes treatments.
Apollo's Science Director, Dr Greg Russell-Jones said, "These studies provide evidence for Oradel TM's ability to protect insulin in the stomach environment and deliver it systemically at levels that lower glucose in the blood."
The ability to provide a sustained reduction in blood glucose levels offers the potential for once or twice daily tablets. This technology also has the advantage of using unmodified insulin, which is less costly than the more recently developed long-acting injectable insulins.
The development can be considered a breakthrough because the stomach's digestive acids usually destroy insulin before it can be absorbed by the body. Apollo's formula overcomes this problem with a protective coating.
"These preclinical results indicate successful oral delivery and subsequent activity of insulin. We are now preparing for clinical trial of oral insulin." said Dr Russell-Jones.
A human Phase 1b study in volunteers with diabetes will be conducted through the International Diabetes Institute. Professor Paul Zimmet AO, Director of the Institute, and who recently joined Apollo's independent scientific advisory board, said: "The data are very promising and impressive. With insulin therapy, the Holy Grail remains the possibility of an oral form of delivery. There has been huge investment around the world, with very little success to date. The data I've seen so far makes this one of the most forward-looking and best prospects of an oral insulin coming to fruition."
The global market for diabetes medications is valued at $18 billion per annum.
Dr Russell-Jones said there is growing demand for better diabetes treatments, such as oral insulin. "Demand will grow if upward trends continue in population ageing and obesity, which are both major risk factors for Type 2 diabetes. Type 2 diabetes accounts for 90% of all cases. The westernisation of countries such as India and China is also expected to lead to significant increases in rates of lifestyle-related illnesses, such as Type 2 diabetes," he said.
About Apollo's oral delivery technology
Apollo's oral delivery technology, Oradel TM , entraps insulin within a nanolattice to protect it in the stomach and uses targeting agents to promote absorption of insulin from the intestine.
Oral delivery of proteins is a breakthrough because the stomach's digestive acids usually destroy proteins before they can be taken up by the body, and the stomach lining typically prevents material passing into the bloodstream.
Oradel TM technology enables controlled release of the active molecule and, thus, a large pharmaceutical window. Pre-clinical studies indicate it transports large protein molecules, up to 130kDa in weight in lattices of around 200 nm in size. Each cell in the stomach wall transports the nanolattice at a different rate, allowing for a controlled release of the drug into the circulation. Once the nanolattice is released into circulation, the structure collapses and the drug is released. Preclinical studies on the oral delivery technology using large proteins have been conducted in more than 120 animals, demonstrating effective delivery of bioactive molecules. The oral insulin studies confirm these findings. This technology is the subject of provisional patents and trademarks.
About Apollo's pre-clinical efficacy studies
The series of experiments involved 20 treatment and control groups, involving two species. Insulin, which is a naturally occurring hormone, reduces blood glucose levels. An oral delivery system needs to be able to protect insulin from degradation in the stomach and deliver it into the body's system in bioactive form.
Studies in eight groups, each of four rats, involving two control groups, demonstrated that intraperitoneal delivery of insulin encapsulated within the Oradel(TM) nanolattice structure does not compromise the bioactivity of insulin. Normal rats were injected in the intraperitoneal cavity with nanolattice containing 0.1, 0.2 or 0.4mg of insulin and compared to similar doses of insulin alone. The data demonstrated that there was no reduction in glucose modifying activity upon incorporation into nanolattice structures. Results were highly statistically significant - p values ranged from .004 to .006.
In the studies to test the effects of oral insulin on blood glucose levels, female Wistar rats were made diabetic via the injection of 50 mg/kg streptozotocin (Sigma - 50130-5G) and considered diabetic once blood glucose levels rose to more than two times normal. Each study typically involved one control and three treatment groups with varied treatment formulations, and four rats per group. Animals in treatment groups received an oral insulin formulation by oral gavage and blood glucose levels for all groups were monitored over time, beginning with the time of administration, and every two hours thereafter, using an Accu-Chek glucose monitor.
The studies used internationally accepted models. Further pre-clinical studies are being conducted in preparation for clinical trials.
Contact
Dr Greg Russell-Jones
Apollo Life Sciences
Science Director
+612 9310 1800
For media enquiries:
Emily Perry
Wilkinson Media
+612 2 8001 8888 / 0431 896 145
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