# US 11,998,562 B2 · Ophthalmological formulations for the prevention of a coronavirus infection

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- Number: US 11,998,562 B2
- Document ID: US11998562B2
- Status: Granted
- Kind: B2
- Application number: 17/583,781
- Filed: 2022-01-25
- Published: 2022-07-28
- Granted: 2024-06-04
- Earliest claimed: 2021-01-25
- Assignees: University of South Florida
- Applicants: University of South Florida
- Inventors: Vijaykumar Sutariya; Srinivas Tipparaju; Kevin Sneed; Manas Biswal; Ramesh Ayyala; Radouil Tzekov
- Web page: https://patentgrep.com/patent/US11998562B2

## CPC

- A61K 31/706: containing six-membered rings with nitrogen as a ring hetero atom
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)}
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- 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)

## Abstract

The present disclosure provides for an ophthalmological composition comprising remdesivir and an ophthalmologically suitable carrier, and the use thereof for treating and preventing a coronavirus infection and treating conjunctivitis.

## Claims

### Claim 1

An ophthalmological composition comprising a nanoparticle and ophthalmologically suitable carrier, wherein the nanoparticle comprises remdesivir, or a pharmaceutically acceptable salt thereof, in a concentration of about 15 wt %, and wherein the nanoparticle has an average diameter of from 200 to 250 nm, further wherein the nanoparticle comprises poly(lactic acid-co-glycolic-acid) carboxylic acid (PLGA-COOH).

### Claim 2 (depends on 1)

The ophthalmological composition of claim 1, wherein the composition is in the form of eye drops.

### Claim 3 (depends on 1)

The ophthalmological composition of claim 1, further comprising an angiotensin converting enzyme inhibitor (ACEI).

### Claim 4 (depends on 1)

The ophthalmological composition of claim 1, further comprising an angiotensin receptor blocker (ARB).

### Claim 5 (depends on 4)

The ophthalmological composition of claim 4, wherein the ARB comprises losartan, telmisartan, or any combination thereof.

### Claim 6 (depends on 1)

The ophthalmological composition of claim 1, further comprising a corticosteroid.

### Claim 7 (depends on 6)

The ophthalmological composition of claim 6, wherein the corticosteroid comprises dexamethasone.

### Claim 8 (depends on 1)

The ophthalmological composition of claim 1, wherein the ophthalmologically suitable carrier comprises a biodegradable polymer, a lipid, or any combination thereof.

### Claim 9 (depends on 8)

The ophthalmological composition of claim 8, wherein remdesivir is encapsulated or dispersed within the biodegradable polymer, a lipid, or any combination thereof.

### Claim 10 (depends on 8)

The ophthalmological composition of claim 8, wherein the biodegradable polymer comprises a poly(hydroxy acid); poly(lactic acid); poly(glycolic acid); poly(lactic acid-co-glycolic acid); poly(lactic-co-glycolic acid); a polyanhydride; a polyorthoester; a polyamide; a polycarbonate; a polyalkylene; polyethylene; polypropylene; a polyalkylene glycol; poly(ethylene glycol); methoxypoly(ethylene glycol); a polyalkylene oxide; poly(ethylene oxide); a polyalkylene terephthalate; poly(ethylene terephthalate); a polyvinyl alcohol; a polyvinyl ether; a polyvinyl ester; a polyvinyl halide; poly(vinyl chloride); polyvinylpyrrolidone; a polysiloxane; a poly(vinyl acetate); a polyurethane; a co-polymer of a polyurethane; a derivativized cellulose; alkyl cellulose; a hydroxyalkyl cellulose; a cellulose ether; a cellulose ester; a nitro cellulose; methyl cellulose; ethyl cellulose; hydroxypropyl cellulose; hydroxy-propyl methyl cellulose; hydroxybutyl methyl cellulose; cellulose acetate; cellulose propionate; cellulose acetate butyrate; cellulose acetate phthalate; carboxylethyl cellulose; cellulose triacetate; cellulose sulfate sodium salt; a polymer of acrylic acid; methacrylic acid; a copolymer of methacrylic acid; a derivative of methacrylic acid; poly(methyl methacrylate); poly(ethyl methacrylate); poly(butylmethacrylate); poly(isobutyl methacrylate); poly(hexylmethacrylate); poly(isodecyl methacrylate); poly(lauryl methacrylate); poly(phenyl methacrylate); poly(methyl acrylate); poly(isopropyl acrylate); poly(isobutyl acrylate); poly(octadecyl acrylate); poly(butyric acid); poly(valeric acid); poly(lactide-co-caprolactone); a copolymer of poly(lactide-co-caprolactone); a blend of poly(lactide-co-caprolactone); polygalactia poly-(isobutyl cyanoacrylate); poly(2-hydroxyethyl-L-glutamine); poly(caprolactone); or any combination, or copolymers thereof.

### Claim 11 (depends on 8)

The ophthalmological composition of claim 8, wherein the lipid comprises fatty acids, glycerolipids, glycerophospholipids, sphingolipids, saccharolipids, polyketides, sterol lipids, prenol lipids, or any combination thereof.

### Claim 12 (depends on 1)

A method of reducing the likelihood of a coronavirus infection from an eye in a subject comprising administering to the subject a therapeutically effective amount of an ophthalmological composition of claim 1 to the subject's eye.

### Claim 13 (depends on 12)

The method of claim 12, wherein coronavirus infection is caused by an avian coronavirus (IBV), porcine coronavirus HKU15 (PorCoV HKU15), Porcine epidemic diarrhea virus (PEDV), HCoV-229E, HcoV-OC43, HcoV-HKU1, HcoV-NL63, SARS-CoV, SARS-CoV-2, or MERS-CoV.

### Claim 14 (depends on 12)

The method of claim 12, further comprising administering a corticosteroid.

### Claim 15 (depends on 14)

The method of claim 14, wherein the corticosteroid is dexamethasone.

### Claim 16 (depends on 1)

A method of reducing the likelihood of conjunctivitis caused by a coronavirus infection in an eye of a subject in need thereof comprising administering to the subject's eye a therapeutically effective amount of an ophthalmological composition of claim 1.

### Claim 17 (depends on 16)

The method of claim 16, wherein the coronavirus infection is caused by an avian coronavirus (IBV), porcine coronavirus HKU15 (PorCoV HKU15), Porcine epidemic diarrhea virus (PEDV), HCoV-229E, HCoV-OC43, HCoV-HKU1, HCoV-NL63, SARS-CoV, SARS-CoV-2, or MERS-CoV.

### Claim 18 (depends on 1)

A method of inhibiting a coronavirus spike protein interaction with angiotensin converting enzyme II (ACE2) in the eye of a subject, the method comprising administering to a part of the eye of the subject an effective amount of an ophthalmological composition of claim 1.
