Particles for oral delivery of peptides and proteins

US6355270B1 · kind B1 · utility

Assignee

• The Regents of the University of California · US

Inventors

• Mauro Ferrari · Beijing, CN
• Peter Dehlinger · Palo Alto, US
• Francis J. Martin · San Francisco, US
• Carl F. Grove · Portola Valley, US
• David Friend · Boston, US

Key dates

• Filing date: Jan 6, 2000
• Grant date: Mar 12, 2002
• Expiry date: Jan 6, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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 &mgr;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.