Oral Delivery of Macromolecules

The licensing-in of a new technology based on the formation of microparticles to explore the feasibility of developing oral delivery of macromolecules has been announced by Debiopharm S.A. (Lausanne, Switzerland).

The microparticles are prepared with blends of biodegradable and polycationic polymers. The macromolecules to be delivered are from three researchers based at the University Henri Poincaré, Nancy (France), who have filed a patent application on the particular carriers developed to improve the oral absorption of large biomolecules such as low molecular weight heparin, peptides, and proteins. The research will be performed at the department of pharmacy of the University Henri Poincare in the laboratory of Professor P. Maincent.

The feasibility study will initially focus on low molecular weight heparin (LMWH), to identify the best parameters in terms of oral bioavailability and prolonged release for the active ingredient. Current research has concentrated mainly on increased duration of antithrombotic activity, improved bioavailabilty and reduced thrombocytopenia after administration of heparin and only rarely on administration routes. However, one of the major disadvantages of heparins consists in their parenteral administration requiring medical assistance to administer the drug and subsequent careful monitoring of patients. In order to overcome this problem, Prof. Maincent and colleagues have developed an oral form of heparin that could be highly accepted by patients.

Various polymeric formulations (micro- and nanoparticles) of unfractionated heparin (UFH) and low molecular weight heparin (LMWH) were developed. Among all formulations tested in vivo, some heparin-loaded micro- and nanoparticles showed satisfactory results after oral administration in rabbits. High absolute bioavailabilities were obtained with microparticles prepared with two different blends of biodegradable and polycationic polymers that included PCL and PLGA and well known granulating aids and coating agents.

According to Dr R.-Y. Mauvernay, founder and CEO of Debiopharm, "Turning injectable formulations of peptides and proteins into oral administrations for patients will reduce healthcare costs and improve patient compliance and comfort. Oral administration is a priority for Debio and we welcome all ideas in this area of research.”




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