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May 15, 2009 (Vol. 29, No. 10)

Delivery Firms Focus on Efficiency & Efficacy

Administering Novel Therapeutics and Improving Drug Safety Serve as the Driving Forces

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    Aegis Therapeutics has established the feasibility of intranasal administration using its Intravail technology for a variety of therapeutic molecules.

    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.”

  • Nanocochleate Technologies

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    Niraj Vasisht, Ph.D., vp, product development at BioDelivery Sciences (BDSI), described BDSI’s delivery platforms including its Bioral™ oral delivery system and its BioErodableMucoAdhesive (BEMA™) technology. 

    The company’s first drug candidate using Bioral technology for oral delivery of the antifungal agent amphotericin B (Bioral Amphotericin B) entered Phase I trials last year. The company reported initial results in February that identified doses that were well tolerated with no meaningful changes in laboratory safety values. Plasma concentrations of amphotericin B were comparable to those seen in prior animal toxicology studies using the same formulation, according to Dr. Vasisht.

    Bioral technology encapsulates a drug in a lipid crystal to allow its oral administration. Alternating layers of lipids spiral around a drug molecule, potentially protecting it from degradation by acid or digestive enzymes in the stomach. 

    According to BDSI, unlike other technologies, Bioral protects the drug without chemically bonding to it, can be used for a wide variety of drugs, and facilitates oral delivery of drugs that currently require intravenous administration.

    The company’s lead product, Onsolis™ (fentanyl buccal soluble film), consists of a small, dissolvable polymer film formulated with the opioid analgesic, fentanyl.

    Applied to the buccal lining of the cheek, Dr. Vasisht said that BEMA technology delivers a dose of the drug quickly, and that Onsolis can manage breakthrough cancer pain in patients already receiving opioid treatment for underlying persistent cancer pain. Biodelivery Systems’ NDA for Onsolis is currently under late-stage review by the FDA.

    A second product utilizing the BEMA drug delivery technology, BEMA Buprenorphine, is also under clinical development for various pain conditions.

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