# US 2014/0193486 A1 · Sustained releasing composition via local injection for treating eye diseases

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- Number: US 2014/0193486 A1
- Document ID: US20140193486A1
- Status: Published application
- Kind: A1
- Application number: 14/200,439
- Filed: 2014-03-07
- Published: 2014-07-10
- Earliest claimed: 2006-11-16
- Assignees: Tlc Biopharmaceuticals, Inc.; Taiwan Liposome Co., Ltd.
- Applicants: TLC Biopharmaceuticals, Inc.; Taiwan Liposome Company
- Inventors: Jun-Jen LIU; Yun-Long Tseng; Sheue-Fang SHIH; Luke S.S. GUO; Keelung HONG
- Web page: https://patentgrep.com/patent/US20140193486A1

## CPC

- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911})
- A61K 9/1272: comprising non-phosphatidyl surfactants as bilayer-forming substances, e.g. cationic lipids or non-phosphatidyl liposomes coated or grafted with polymers (lipids as modifying agents {A61K47/543})
- A61P 27/02: Ophthalmic agents
- 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 invention provides a sustained release composition for intravitreal injection to the eye of a subject in need thereof. The sustained release composition contains an effective amount of a therapeutic agent in association with a nanosphere. The nanosphere contains a particle that comprises a particle-forming component capable of forming a vesicle, and an agent-carrying component capable of forming a complex with the therapeutic agent via electrostatic charge-charge interaction or hydrophobic-hydrophobic interaction. The particle-forming component has at least one head group moiety selected from a hydrophobic head group moiety, a polar head group moiety and a combination thereof. The agent-carrying component is a chemical entity that contains one or more negatively or positively charged groups.

## Claims

### Claim 1

A method for treating an eye disease, comprising
intravitreally administering a composition comprising
a liposome free of an encapsulated therapeutic agent and the surface of the liposome is derivatized with one or more hydrophilic polymers; and
an anti-VEGF antibody;
wherein the anti-VEGF antibody is covalently attached to the distal end of said hydrophilic polymer.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the hydrophilic polymer is polyethylene glycol (PEG).

### Claim 3 (depends on 2)

The method according to claim 2, wherein the hydrophilic polymer is 1,2-Distearoyl-sn-Glycero-3-Phosphoethanolamine-N-[Maleimide (Polyethylene Glycol)2000] (PEG-DSPE2000-maleimide).

### Claim 4 (depends on 1)

The method according to claim 1, wherein after intravitreally administering the composition, the anti-VEGF antibody remains at the injection site for more than 7 days after the intravitreal injection.

### Claim 5 (depends on 1)

The method according to claim 1, wherein after intravitreally administering the composition, the anti-VEGF antibody remains remains at the injection site for more than 28 days after the intravitreal injection.

### Claim 6 (depends on 1)

The method according to claim 1, wherein the anti-VEGF antibody is a Fab.

### Claim 7 (depends on 1)

The method according to claim 1, wherein the eye disease is confined to the posterior portion of the eye.

### Claim 8 (depends on 1)

The method according to claim 1, wherein the eye disease is in close proximity to the retina.

### Claim 9 (depends on 1)

The method according to claim 1, wherein the eye disease is age-related macular degeneration.

### Claim 10 (depends on 1)

The method according to claim 1, wherein the eye disease is diabetic retinopathy.