Mauro Ferrari - Dublin OH Peter J. Dehlinger - Palo Alto CA Francis J. Martin - San Francisco CA Carl F. Grove - Portola Valley CA David R. Friend - Menlo Park CA
Assignee:
The Regents of the University of California - Oakland CA
Microfabricated, asymmetrical, reservoir-containing particles for use in the oral delivery of biopolymer therapeutic agents such as peptides, proteins and oligonucleotides are disclosed. The particles are encapsulated in enteric-coated capsules or tablets to provide passage through the stomach and release of a suspension of the particles in the intestinal lumen. The particles have a selected shape, and uniform dimensions preferably in the 100 m to 1 mm range. The reservoirs open to the face of the particle and are filled with a therapeutic agent and selected excipients. The excipients are selected to delay the dissolution/release of the agent from the particle reservoirs for 5-60 minutes after the particle is released in the intestinal lumen. Alternatively, the pore is plugged with an erodable material. The face of the particle is grafted with a layer of muco-adhesive ligands designed to quickly bind the particle to the intestinal mucosa for several minutes to several hours after release of the particles from the enteric-coated carrier.
William Tacon - Westerville OH, US Anthony Boiarski - Hilliard OH, US Carl Grove - Upper Arlington OH, US Richard Brody - Worthington OH, US
International Classification:
A61K048/00 A61L009/04 A61K009/14 A61K039/395
US Classification:
514/002000, 424/046000, 514/044000, 424/130100
Abstract:
Microparticles for use in the pulmonary delivery of a therapeutic material, comprising a polymer matrix, which is prefabricated to have a particular geometric shape including that of a disc cube, rectangle or snowflake. Additionally, these microparticles may include a winged structure to enhance the aerodynamic characteristics of said microparticle. Microfabrication methods for making these microparticles are provided.
Marilyn Morgan, Linda Schelling, Dana Dowell, Rick Maville, Marletta Jones, Reita Pair, Gail Palmer, Bernadette Leather, Karen Engel, Robert Croft, Lynn Morgan