# US 2016/0256404 A1 · Drugs and Gene Carrier Particles That Rapidly Move Through Mucous Barriers

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- Number: US 2016/0256404 A1
- Document ID: US20160256404A1
- Status: Published application
- Kind: A1
- Application number: 14/620,333
- Filed: 2015-02-12
- Published: 2016-09-08
- Earliest claimed: 2004-01-28
- Assignees: The Johns Hopkins University
- Applicants: The Johns Hopkins University
- Inventors: Justin Hanes; Michelle R. Dawson; Denis Wirtz; Jie Fu; Eric M. Krauland
- Web page: https://patentgrep.com/patent/US20160256404A1

## CPC

- A61K 9/5153: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61K 9/0073: {Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; (nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M)}
- A61K 9/167: {with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface (with further drug-free outer coating A61K9/5073)}
- A61K 9/5031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)}
- A61K 9/5123: {Organic compounds, e.g. fats, sugars}
- A61K 9/5146: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides}
- A61K 47/543: {Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine}
- A61K 47/6935: {the polymer being obtained otherwise than by reactions involving carbon to carbon unsaturated bonds, e.g. polyesters, polyamides or polyglycerol}
- A61K 47/6937: {the polymer being PLGA, PLA or polyglycolic acid}
- A61K 48/0033: {the non-active part being non-polymeric}
- A61K 48/0041: {the non-active part being polymeric}
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- 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

## Abstract

The invention generally relates to polymeric particles suitable for transporting bioactive agents across mucosal barriers. The invention also relates to methods of making and using those polymeric particles.

## Claims

### Claim 1

A method for treating, preventing, or diagnosing a condition in a patient, comprising administering to the patient a pharmaceutical composition comprising a polymeric particle and a pharmaceutically acceptable carrier, wherein the polymeric particle comprises a pharmaceutically acceptable polymer core, a bioactive agent, and a surface-altering agent disposed on the surface of the polymer core that renders the surface of the polymeric particle mucus resistant and/or enhances the average rate at which the particles or a fraction of the particles moves in mucus.

### Claim 2 (depends on 1)

The method of claim 1, wherein the bioactive agent is encapsulated in the polymer core.

### Claim 3 (depends on 1)

The method of claim 1, wherein the bioactive agent is disposed on the surface of the polymeric particle.

### Claim 4 (depends on 1)

The method of claim 1, wherein the bioactive agent is covalently coupled to the polymer core.

### Claim 5 (depends on 1)

The method of claim 1, wherein the pharmaceutically acceptable polymer is a poly(D,L-lactic-co-glycolic) acid, polyethylenimine, dioleyltrimethylammoniumpropane/dioleyl-sn-glycerolphosphoethanolamine, poly(anhydrides), or a polymer formed from clinically approved monomers.

### Claim 6 (depends on 5)

The method of claim 5, wherein the clinically approved monomers are monomers of sebacic acid, 1,3-bis(carboxyphenoxy)propane, and/or ethylene glycol.

### Claim 7 (depends on 1)

The method of claim 1, wherein the bioactive agent is a therapeutic agent or an imaging agent.

### Claim 8 (depends on 7)

The method of claim 7, wherein the therapeutic agent is a DNA, an RNA, a small molecule, a peptidomimetic, or a protein.

### Claim 9 (depends on 7)

The method of claim 7, wherein the imaging agent is a diagnostic agent.

### Claim 10 (depends on 7)

The method of claim 7, wherein the imaging agent further comprises a detectable label.

### Claim 11 (depends on 1)

The method of claim 1, wherein the polymeric particle further comprises a targeting moiety.

### Claim 12 (depends on 1)

The method of claim 1, wherein the polymeric particle further comprises an adjuvant.

### Claim 13 (depends on 1)

The method of claim 1, wherein the surface-altering agent is a cationic surfactant.

### Claim 14 (depends on 13)

The method of claim 13, wherein the cationic surfactant is dimethyldioctadecylammonium bromide.

### Claim 15 (depends on 1)

The method of claim 1, wherein the surface-altering agent enhances hydrophilicity of the surface of the polymeric particle.

### Claim 16 (depends on 15)

The method of claim 15, wherein the surface-altering agent is polyethylene glycol.

### Claim 17 (depends on 1)

The method of claim 1, wherein the polymeric particle is less than 200 nm in diameter.

### Claim 18 (depends on 1)

The method of claim 1, wherein the polymeric particle passes through a mucosal barrier at a greater rate than a polystyrene particle of a similar size.

### Claim 19 (depends on 1)

The method of claim 1, wherein the bioactive agent is a DNA, and wherein the polymeric particle comprising the DNA transfects a cell more efficiently than does naked DNA.

### Claim at position 20

20-24. (canceled)

### Claim 25 (depends on 1)

The method of claim 1, wherein the polymeric particle in the pharmaceutical composition passes through a mucosal barrier in the patient.
