PARTICLES FOR ORAL DELIVERY OF PEPTIDES AND PROTEINS

Title:

PARTICLES FOR ORAL DELIVERY OF PEPTIDES AND PROTEINS

Document Type and Number:

WIPO Patent Application WO2000041740

Kind Code:

A3

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 mu 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.

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Inventors:

GROVE CARL F
DEHLINGER PETER J
FRIEND DAVID R
MARTIN FRANCIS J
FERRARI MAURO

Application Number:

PCT/US2000/000362

Publication Date:

September 28, 2000

Filing Date:

January 07, 2000

Export Citation:

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Assignee:

UNIV CALIFORNIA (US)
IMEDD (US)

International Classes:

C12N15/09; A61K9/14; A61K9/16; A61K9/26; A61K9/48; A61K9/52; A61K31/7088; A61K38/00; A61K38/21; A61K38/22; A61K38/26; A61K38/28; A61K39/395; A61K47/10; A61K47/14; A61K47/22; A61K47/34; A61K47/36; A61K47/38; A61K47/40; A61K47/42; A61K47/44; A61K47/48; A61P35/00; A61P43/00; G03F7/00; (IPC1-7): A61K9/14

Foreign References:

US5968554A

1999-10-19

Other References: