# US 12,178,913 B2 · Particles comprising a therapeutic or diagnostic agent and suspensions and methods of use thereof

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- Number: US 12,178,913 B2
- Document ID: US12178913B2
- Status: Granted
- Kind: B2
- Application number: 18/136,012
- Filed: 2023-04-18
- Published: 2023-11-09
- Granted: 2024-12-31
- Earliest claimed: 2016-11-22
- Assignees: Elektrofi, Inc.
- Applicants: Elektrofi, Inc.
- Inventors: Chase Coffman; Lyndon Charles; Paul Brown; Daniel Benjamin Dadon; Lisa Liu; Cory Robinson
- Web page: https://patentgrep.com/patent/US12178913B2

## CPC

- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 9/1682: {Processes}
- A61K 9/5089: {Processes}
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- B05B 5/025: Discharge apparatus, e.g. electrostatic spray guns
- 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)
- B05B: SPRAYING APPARATUS; ATOMISING APPARATUS; NOZZLES (spray-mixers with nozzles B01F25/72; processes for applying liquids or other fluent materials to surfaces by spraying B05D)

## Abstract

The invention provides particles, compositions including the particles, and methods of making the particles using electrospray. In certain embodiments, the particles allow for high concentrations of a therapeutic or diagnostic agent to be delivered at low viscosity. Particles may also exhibit beneficial properties with respect to stability.

## Claims

### Claim 1

A composition comprising particles comprising (a) a protein and (b) a carbohydrate, a salt, or a combination thereof, wherein at least a portion of the carbohydrate, salt, or combination thereof is localized at the particle surface and, wherein the protein in the particles has 0.5 to 1.0 activity per unit.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the particles are in a suspension in a non-aqueous or aqueous liquid.

### Claim 3 (depends on 2)

The composition of claim 2, wherein the suspension has a viscosity from 0.27 to 200 cP.

### Claim 4 (depends on 2)

The composition of claim 2, wherein the suspension comprises from 5 to 90% particles by volume.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the particles comprise the protein at a concentration from 0.0001 to 1000 mg/ml.

### Claim 6 (depends on 2)

The composition of claim 2, wherein the particles are in suspension in the non-aqueous liquid, which is an organic solvent or an ionic liquid.

### Claim 7 (depends on 2)

The composition of claim 2, wherein the particles are in suspension in the aqueous liquid, which is selected from the group consisting of water, 0.9% saline, lactated Ringer's solution, dextrose 5%, and a buffer.

### Claim 8 (depends on 6)

The composition of claim 6, wherein the non-aqueous liquid is the organic solvent, which is selected from the group consisting of benzyl alcohol, benzyl benzoate, castor oil, coconut oil, corn oil, cottonseed oil, fish oil, grape seed oil, hazelnut oil, hydrogenated palm seed oil, olive oil, peanut oil, peppermint oil, safflower oil, sesame oil, soybean oil, sunflower oil, vegetable oil, walnut oil, polyethylene glycol, glycofurol, acetone, diglyme, dimethylacetamide, dimethyl isosorbide, dimethyl sulfoxide, ethanol, ethyl acetate, ethyl ether, ethyl lactate, isopropyl acetate, methyl acetate, methyl isobutyl ketone, methyl tert-butyl ether, N-methyl pyrrolidone, perfluorodecalin, 2-pyrrolidone, trigylcerides, tetrahydrofurfuryl alcohol, triglycerides of the fractionated plant fatty acids C8 and C10, propylene glycol diesters of saturated plant fatty acids C8 and C10, ethyl oleate, ethyl caprate, dibutyl adipate, fatty acid esters, hexanoic acid, octanoic acid, triacetin, diethyl glycol monoether, gamma-butyrolactone, eugenol, clove bud oil, citral, limonene, and any combination thereof.

### Claim 9 (depends on 6)

The composition of claim 6, wherein the non-aqueous liquid is the organic solvent, which is selected from the group consisting of ethyl oleate and fatty acid esters.

### Claim 10 (depends on 6)

The composition of claim 6, wherein the non-aqueous liquid is the ionic liquid, which comprises pyridinium, pyridazinium, pyrimidinium, pyrazinium, imidazolium, pyrazolium, thiazolium, oxazolium, triazolium, ammonium, sulfonium, halides, sulfates, sulfonates, carbonates, phosphates, bicarbonates, nitrates, acetates, PF6-, BF4-, triflate, nonaflate, bis(trifyl)amide, trifluoroacetate, heptafluorobutanoate, haloaluminate, or any combination thereof.

### Claim 11 (depends on 1)

The composition of claim 1, wherein the particles have diameters from 0.1 to 1000 μm.

### Claim 12 (depends on 1)

The composition of claim 1, wherein the particles have a polydispersity index from 0.05 to 0.9.

### Claim 13 (depends on 1)

The composition of claim 1, wherein the carbohydrate is present and is dextran, trehalose, sucrose, agarose, mannitol, lactose, sorbitol, or maltose.

### Claim 14 (depends on 1)

The composition of claim 1, wherein the salt is present and is sodium chloride, calcium chloride, potassium chloride, sodium hydroxide, stannous chloride, magnesium sulfate, sodium glucoheptonate, sodium pertechnetate, or guanidine hydrochloride.

### Claim 15 (depends on 1)

The composition of claim 1, wherein the protein is an antibody.

### Claim 16 (depends on 15)

The composition of claim 15, wherein the antibody is human lgG or a monoclonal antibody.

### Claim 17 (depends on 1)

The composition of claim 1, wherein the protein is bovine serum albumin.

### Claim 18

A method of administering a first therapeutic or diagnostic agent to a mammal, the method comprising administering an effective amount of a suspension or a dry formulation comprising particles to the mammal, wherein the suspension comprises a non-aqueous or aqueous liquid and the particles comprising (a) a protein and (b) a carbohydrate, a salt, or a combination thereof, wherein at least a portion of the carbohydrate, salt, or combination thereof is localized at the particle surface and, wherein the protein in the particles has 0.5 to 1.0 activity per unit.