# US 12,758,533 B2 · Nanoparticles for delivery of therapeutics to the eye for treatment of glaucoma

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 12,758,533 B2
- Document ID: US12758533B2
- Status: Granted
- Kind: B2
- Application number: 18/577,632
- Filed: 2022-07-11
- Published: 2024-09-19
- Granted: 2026-10-13
- Earliest claimed: 2021-07-09
- Assignees: Northwestern University
- Applicants: Northwestern University
- Inventors: Mark Johnson; Amir Vahabikashi; Trevor Stack; Michael Patrick Vincent; Evan Alexander Scott
- Web page: https://patentgrep.com/patent/US12758533B2

## CPC

- A61K 31/427: not condensed and containing further heterocyclic rings
- A61K 9/0051: {Ocular inserts or implants}
- A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)}
- A61K 9/146: {with organic macromolecular compounds}
- A61P 27/06: Antiglaucoma agents or miotics
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides systems for targeted delivery of therapeutic agents to Schlemm's canal (SC) endothelial cells. Also provided are methods for using the systems to treat glaucoma or reduce intraocular pressure.

## Claims

### Claim 1

A system for targeted delivery of a therapeutic agent to a Schlemm's canal (SC) endothelial cell, the system comprising:
a. a nanocarrier comprising a poly(ethylene glycol)-block-poly(propylene sulfide) (PEG-b-PPS) copolymer;
b. the therapeutic agent loaded in the nanocarrier; and
c. a targeting moiety that targets SC endothelial cells incorporated into the surface of the nanocarrier;
wherein the targeting moiety comprises:
i. a peptide that specifically binds to SC endothelial cells;
ii. a polyethylene glycol (PEG) spacer comprising 48 or more units; and
iii a hydrophobic anchor.

### Claim 2 (depends on 1)

The system of claim 1, wherein the nanocarrier is a micelle.

### Claim 3 (depends on 1)

The system of claim 1, wherein the nanocarrier has a diameter within the range of 5 nm to 60 nm.

### Claim 4 (depends on 1)

The system of claim 1, wherein the nanocarrier has a diameter within the range of 100 nm to 300 nm.

### Claim 5 (depends on 1)

The system of claim 1, wherein the PEG-b-PPS copolymer is a PEG45-b-PPS23 copolymer.

### Claim 6 (depends on 1)

The system of claim 1, wherein the therapeutic agent is a cell softening agent.

### Claim 7 (depends on 6)

The system of claim 6, wherein the therapeutic agent is latrunculin A.

### Claim 8 (depends on 1)

The system of claim 1, wherein the peptide binds to a FLT4/VEGFR3 receptor.

### Claim 9 (depends on 8)

The system of claim 8, wherein the peptide has a sequence of SEQ ID NO: 1 or a sequence having 95% sequence similarity to SEQ ID NO: 1.

### Claim 10 (depends on 1)

The system of claim 1, wherein the molar ratio of the targeting moiety to the PEG-b-PPS copolymer is from 1% to 5%.

### Claim 11 (depends on 10)

The system of claim 10, wherein the molar ratio of the targeting moiety to the PEG-b-PPS copolymer is 5%.

### Claim 12 (depends on 1)

The system of claim 1, wherein the hydrophobic anchor is palmitoleic acid.

### Claim 13 (depends on 1)

A pharmaceutical composition comprising the system of claim 1; and one or more pharmaceutically acceptable carriers.

### Claim 14 (depends on 1)

A method of reducing the intraocular pressure (IOP) in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising the system of claim 1.

### Claim 15 (depends on 14)

The method of claim 14, wherein the therapeutic agent is latrunculin A and the concentration of latrunculin A in the pharmaceutical composition is 0.05 μM-20 μM.

### Claim 16 (depends on 14)

The method of claim 14, wherein the IOP is reduced by at least 35% after 24 hours from the administration.

### Claim 17 (depends on 1)

A method of treating glaucoma in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising the system of claim 1.

### Claim 18 (depends on 17)

The method of claim 17, wherein the therapeutic agent is latrunculin A and the concentration of latrunculin A in the pharmaceutical composition is 0.05 μM-20 μM.