Delivery methods to improve the safety and efficacy of existing drugs, extend their clinical applications, and enable delivery of novel products were the focus of Arrowhead Conferences’ “ Drug Delivery Summit”, held earlier this month. Presenting companies discussed topics including the inherent challenges of RNAi delivery, delivery of ocular therapeutics to treat serious eye disease, and current issues in aerosol delivery development.
Aegis Therapeutics’ delivery platforms, based on its Intravail® transmucosal absorption agents, were developed at the University of Alabama Medical School. Edward Maggio, Ph.D., Aegis’ CEO, discussed progress with the Intravail platform and its applications for peptide-based drugs at the meeting.
Intravail technology comprises chemically synthesized transmucosal absorption enhancement agents that allow noninvasive systemic delivery of peptide, protein, nucleotide-related, and other small and large molecule drugs. These drugs may previously have been deliverable by injection only.
According to Dr. Maggio, Aegis has established the feasibility of intranasal administration using Intravail technology for a variety of therapeutic molecules, including parathyroid hormone, beta interferon, calcitonin, and a new anti-obesity peptide.
Aegis is currently focused on peptide drug delivery, explained Dr. Maggio, who added that the therapeutic use of physiologically active peptides has been limited compared to small molecules and other chemically synthesized compounds.
“Peptides and proteins remain susceptible to destruction in the GI tract and, with few exceptions, require administration via injection in order to achieve therapeutic levels,” Dr. Maggio said. Aegis’ technology uses alkylsaccharides to reduce peptide and protein aggregation during manufacturing processes and in final formulations, thereby, enhancing stability and reducing undesirable immunogenicity, he added.
“When you can increase the bioavailability of a peptide drug, you can increase its applications,” Dr. Maggio noted. As an example, he cited his company’s work with intranasal calcitonin. “Calcitonin has only 3% on average bioavailability when delivered intranasally in current formulations used to treat osteoporosis. And while many important applications that require higher blood levels for efficacy have been described in the medical literature, the current calcitonin nasal spray is inadequate.
“Our technology provides a 12-fold increase in calcitonin blood levels via intranasal delivery, therefore, enhancing the potential for other clinical uses for calcitonin, for example as an analgesic for opioid-resistant metastatic bone cancer pain.”