# US 9,040,079 B2 · Pegylated compounds for age-related macular degeneration

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- Number: US 9,040,079 B2
- Document ID: US9040079B2
- Status: Granted
- Kind: B2
- Application number: 12/743,489
- Filed: 2008-11-19
- Published: 2010-09-30
- Granted: 2015-05-26
- Earliest claimed: 2007-11-19
- Assignees: Biolitec Pharma Marketing Ltd
- Applicants: Volker Albrecht; Stefan Spaniol; Dietrich Scheglmann
- Inventors: Volker Albrecht; Stefan Spaniol; Dietrich Scheglmann
- Web page: https://patentgrep.com/patent/US9040079B2

## CPC

- A61K 49/0084: {liposome, i.e. bilayered vesicular structure}
- A61K 9/0051: {Ocular inserts or implants}
- A61K 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911})
- A61K 41/0071: {PDT with porphyrins having exactly 20 ring atoms, i.e. based on the non-expanded tetrapyrrolic ring system, e.g. bacteriochlorin, chlorin-e6, or phthalocyanines}
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- 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

A special photosensitizer formulation and Photodynamic Therapy method for treating choroidal neovascularization (CNV) associated with age-related macular degeneration (AMD) is provided. CNV is a major cause for vision loss in elderly patients. A special drug delivery formulation is used to encapsulate the hydrophobic photosensitizer, preferably a pegylated liposome. This improves the solubility and therapeutic index of the photosensitizers. In one preferred embodiment, a pegylated photoactive agent remains confined in the intravascular compartment of neovasculature for a longer duration. Thus efficient elimination of neovascular proliferation and minimal damage to extravascular tissue and normal vessels is ensured. In this method, a hydrophobic photosensitizer, that is able to photochemically destroy neovessels, is injected into the patient. CNV irradiation with a non-thermal laser follows after a predefined time interval. The excited photosensitizer photocoagulates newly formed blood vessels thereby improving the vision and preventing further loss of vision.

## Claims

### Claim 1

A chemical formulation for the delivery of a hydrophobic drug to a choroidal neovascular region, comprising:
a carrier for solubilizing a hydrophobic drug; and
a therapeutically effective amount of hydrophobic photosensitize; wherein said carrier is a liposomal bilayer comprising synthetic phospholipids that are a mixture of dipalmitoyl phosphatidyl choline (DPPC), dipalmitoyl phosphatidyl glycerol (DPPG), and pegylated distearoyl phosphatidyl ethanol amine (PEG-DSPE) present in a weight ratio of DPPC:DPPG:PEG-DSPE of 9:1:1 and said drug is present in said liposomal bilayer; and wherein said hydrophobic photosensitizer is temoporfin.

### Claim 2

A method for effecting closure of choroidal neovasculature related to age related macular degeneration (AMD) in patients using photodynamic therapy (PDT) comprising the steps of:
administering a therapeutically effective amount of pegylated liposome comprising synthetic phospholipids that are a mixture of dipalmitoyl phosphatidyl choline (DPPC), dipalmitoyl phosphatidyl glycerol (DPPG), and pegylated distearoyl phosphatidyl ethanol amine (PEG-DSPE) present in a weight ratio of DPPC:DPPG:PEG-DSPE of 9:1:1 and, which has a predetermined amount of a hydrophobic photosensitizer in its bilayer;
allowing sufficient time to release and localize said photosensitizer in chorodial neovasculature; and
irradiating the photosensitizer with non-thermal laser radiation, so as to occlude the choroidal neovasculature; and wherein said photosensitizer is temoporfin administered at a drug dosage ranging between about 0.25 to 1.0 mg/kg body weight.

### Claim 3 (depends on 2)

The method according to claim 2, wherein said photosensitizer is administered intravenously.

### Claim 4 (depends on 2)

The method according to claim 2, wherein said photosensitizer remains confined within the choroidal neovasculature for at least 700 sec.

### Claim 5 (depends on 2)

The method according to claim 2, wherein said non-thermal laser irradiation is applied at a power density between about 12.5 J/cm2 to 100 J/cm2.