# US 5,702,727 A · Compositions and methods for the oral delivery of active agents

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- Number: US 5,702,727 A
- Document ID: US5702727A
- Status: Granted
- Kind: A
- Application number: 08/409,613
- Filed: 1995-03-06
- Granted: 1997-12-30
- Earliest claimed: 1993-02-22
- Assignees: Alza Corporation
- Inventors: Alfred A. Amkraut; Heechung Yang
- Web page: https://patentgrep.com/patent/US5702727A

## CPC

- A61K 9/5138: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 47/6931: {the material constituting the nanoparticle being a polymer}
- A61K 47/6933: {the polymer being obtained by reactions only involving carbon to carbon, e.g. poly(meth)acrylate, polystyrene, polyvinylpyrrolidone or polyvinylalcohol}
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- Y10T 428/2982: Particulate matter [e.g., sphere, flake, etc.]
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
- Y10T: TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION

## Abstract

Compositions and methods for the oral administration of drugs and other active agents are provided. The compositions comprise an active agent carrier particle attached to a binding moiety which binds specifically to a target molecule present on the surface of a mammalian enterocyte. The binding moiety binds to the target molecule with a binding affinity or avidity sufficient to initiate endocytosis or phagocytosis of the particulate active agent carrier so that the carrier will be absorbed by the enterocyte. The active agent will then be released from the carrier to the host's systemic circulation. In this way, degradation of degradation-sensitive drugs, such as polypeptides, in the intestines can be avoided while absorption of proteins and polypeptides from the intestinal tract is increased.

## Claims

### Claim 1

A method for systemically delivering a protein or polypeptide drug to a mammalian host, said method comprising (a) orally administering to the host a composition which comprises the protein or polypeptide drug protectively retained by a carrier particle wherein said carrier particle is attached to a binding moiety which binds specifically to a target molecule present on the surface of a mammalian enterocyte, the target molecule being an endocytosis- or phagocytosis- promoting receptor, and (b) delivering the protein or polypeptide drug through the intestinal mucosa of the host to the blood stream of the host, wherein the carrier particle is absorbed by the mammalian enterocyte prior to release of the protein or polypeptide drug from the particle.

### Claim 2 (depends on 1)

A method as in claim 1, wherein the active agent is a polypeptide drug.

### Claim 3 (depends on 1)

A method as in claim 1, wherein the carrier particle is a nanoparticle.

### Claim 4 (depends on 1)

A method as in claim 1, wherein the binding moiety is an adhesion molecule or a mimic thereof, or a fragment of an adhesion molecule or a mimic thereof.

### Claim 5 (depends on 1)

A method as in claim 1, wherein the binding moiety is selected from the group consisting of an oligopeptide containing the sequence RGD, an invasin molecule or a fragment thereof, EGF or a fragment thereof, and an antibody or a fragment thereof.