# US 10,945,966 B2 · PEGylated lipid nanoparticle with bioactive lipophilic compound

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- Number: US 10,945,966 B2
- Document ID: US10945966B2
- Status: Granted
- Kind: B2
- Application number: 16/681,908
- Filed: 2019-11-13
- Published: 2020-05-28
- Granted: 2021-03-16
- Earliest claimed: 2015-08-11
- Assignees: Eyesiu Medicines B.V.
- Applicants: Eyesiu Medicines B.V.
- Inventors: Pieter Jaap Gaillard; Jacob Rip
- Web page: https://patentgrep.com/patent/US10945966B2

## CPC

- A61K 9/5123: {Organic compounds, e.g. fats, sugars}
- 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 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/164: of a carboxylic acid with an aminoalcohol, e.g. ceramides
- A61K 31/436: the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
- A61K 38/13: Cyclosporins
- A61K 47/6929: {the form being a nanoparticle, e.g. an immuno-nanoparticle}
- A61K 47/6935: {the polymer being obtained otherwise than by reactions involving carbon to carbon unsaturated bonds, e.g. polyesters, polyamides or polyglycerol}
- A61K 49/0041: {Xanthene dyes, used in vivo, e.g. administered to a mice, e.g. rhodamines, rose Bengal (in vivo G01N)}
- A61K 49/0093: {Nanoparticle, nanocapsule, nanobubble, nanosphere, nanobead, i.e. having a size or diameter smaller than 1 micrometer, e.g. polymeric nanoparticle}
- A61P 27/02: Ophthalmic agents
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- 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
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES

## Abstract

The invention relates to nanoparticles for the systemic or topical delivery of lipophilic diagnostic or therapeutic agents to a subject in need thereof. The nanoparticles of the invention comprise a water soluble polymer and at least one of a biocompatible lipid and a lipophilic agent. The invention further relates to ophthalmic treatment using the nanoparticles of the invention. In addition, the invention pertains to compositions and formulations comprising the nanoparticle of the invention. Such formulation may be an eye drop formulation.

## Claims

### Claim 1

A nanoparticle comprising:
a) two or more phospholipids; and,
b) at least one acylethanolamide,
wherein the nanoparticle has a surface comprising a water soluble polymer wherein the water soluble polymer is conjugated to one of the two or more phospholipids.

### Claim 2 (depends on 1)

The nanoparticle according to claim 1, wherein the one or more phospholipids are neutral phospholipids.

### Claim 3 (depends on 1)

The nanoparticle according to claim 1, wherein the water soluble polymer is at least one of:
i) a polyalkylether;
ii) a homopolymer that is a PEG substitute or a PEG alternative;
iii) a heteropolymer of small alkoxy monomers.

### Claim 4 (depends on 3)

The nanoparticle according to claim 3, wherein the water soluble polymer has a molecular weight of at least about 120 Daltons and a polymerization number of at least 6.

### Claim 5 (depends on 1)

The nanoparticle according to claim 1, wherein the size of the nanoparticle is between 5-300 nm.

### Claim 6 (depends on 1)

A composition comprising a nanoparticle according to claim 1 and an excipient or carrier that is suitable for human or veterinary use.

### Claim 7 (depends on 6)

The composition according to claim 6, wherein the composition has a turbidity that is not higher than FTU as determined according to the ISO 7027:1999 standard.

### Claim 8 (depends on 6)

The composition according to claim 6, wherein the composition further comprises a substrate for a drug efflux pump.