# US 12,005,125 B2 · Nanoparticles for use in photodynamic therapies and methods of making, evaluating and using the same

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- Number: US 12,005,125 B2
- Document ID: US12005125B2
- Status: Granted
- Kind: B2
- Application number: 17/228,332
- Filed: 2021-04-12
- Published: 2021-10-14
- Granted: 2024-06-11
- Earliest claimed: 2020-04-10
- Assignees: Mi2 Holdings LLC
- Applicants: Mi2 Holdings LLC
- Inventors: Andrew Hopkins; Thomas Hopkins
- Web page: https://patentgrep.com/patent/US12005125B2

## CPC

- A61K 47/6935: {the polymer being obtained otherwise than by reactions involving carbon to carbon unsaturated bonds, e.g. polyesters, polyamides or polyglycerol}
- 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 47/62: the modifying agent being a protein, peptide or polyamino acid
- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- B82Y 30/00: Nanotechnology for materials or surface science, e.g. nanocomposites
- B82Y 40/00: Manufacture or treatment of nanostructures
- 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)
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES

## Abstract

A nanocomposition for use in treating cardiac, oncologic, bariatric, or dermatologic indications, conditions and diseases condition using phthalocyanine dye, such as IR700. A nanocomposition having IR700, an 8PEG nanoparticle and a RGD, or iRGD targeting agent. Administering a product comprising IR700 to a patient, whereby the IR700 is delivered to the target tissue, and found in only target tissue; and administering light to activate the IR700, thereby producing an ROS.

## Claims

### Claim 1

A composition comprising:
a plurality of nanoparticles, the nanoparticles comprising an 8-arm PEG core;
wherein the 8-arm PEG core is substituted with at least a photosensitizer (PS) and a targeting agent (TA) that are directly linked to the 8-arm PEG core;
wherein at least three arms of the 8-arm PEG core are unsubstituted;
wherein the 8-arm PEG core contains 1-2 PS per 8-arm PEG core; and
wherein the 8-arm PEG core has a weight of at least about 40 kDa.

### Claim 2 (depends on 1)

The composition of claim 1 wherein the photosensitizer (PS) is IR700.

### Claim 3 (depends on 1)

The composition of claim 1 wherein the targeting agent is an RGD peptide.

### Claim 4 (depends on 1)

The composition of claim 1 wherein the targeting agent is iRGD.

### Claim 5 (depends on 1)

The composition of claim 1 wherein the photosensitizer is IR 700; and
wherein the targeting agent is iRGD.

### Claim 6 (depends on 1)

The composition of claim 1
wherein the photosensitizer is a phthalocyanine dye; and
wherein the targeting agent is a targeting peptide.

### Claim 7 (depends on 1)

The composition of claim 1 wherein the direct link is a covalent link.

### Claim 8 (depends on 1)

The composition of claim 1 further comprising at least an additive directly linked to the 8-arm PEG core and the additive is selected from the group consisting of therapeutic agents, diagnostic agents, theranostic agents, and combinations thereof.

### Claim 9 (depends on 1)

The composition of claim 1 wherein the nanoparticles have a hydrodynamic diameter of 25 nm or less.

### Claim 10

A method of Photodynamic treatment of a medical cardiac, oncologic, bariatric, or dermatologic condition in a subject in need thereof, the method comprising:
Administering a composition to the subject, the composition comprising:
a plurality of nanoparticles, the nanoparticles comprising an 8-arm PEG core;
wherein the 8-arm PEG core is substituted with at least a photosensitizer (PS) and a targeting agent (TA) that are directly linked to the 8-arm PEG core;
wherein at least three arms of the 8-arm PEG core are unsubstituted;
wherein the 8-arm PEG core contains 1-2 PS; and
wherein the 8-arm PEG core has a weight of at least about 40 kDa;
Allowing a period of time for the composition to accumulate in a target tissue; and
Administering light to activate the PS in the composition; and,
Providing sufficient light dosage to kill the target tissue.

### Claim 11 (depends on 10)

The Photodynamic treatment method of claim 10 wherein the composition is administered via intravenous injection.

### Claim 12 (depends on 10)

The Photodynamic treatment method of claim 10 wherein the light dosage is less that 1KJ/cm2, and wherein the light source is selected from an LED, a continuous laser, a pulsed laser, or combinations thereof.

### Claim 13 (depends on 10)

The Photodynamic treatment method of claim 10 wherein the light dosage is between 100 and 400 J/cm2.

### Claim 14 (depends on 10)

The Photodynamic treatment method of claim 10 wherein the light is delivered internally to the target tissue via an optical cable.

### Claim 15 (depends on 11)

The Photodynamic treatment method of claim 11 wherein the light is delivered externally through the subject's skin.

### Claim 16 (depends on 10)

The Photodynamic treatment method of claim 10 wherein the photosensitizer (PS) is a phthalocyanine dye.

### Claim 17 (depends on 10)

The Photodynamic treatment method of claim 10 wherein the photosensitizer (PS) is IR700.

### Claim 18 (depends on 1)

The composition of claim 1 wherein the photosensitizer (PS) is a phthalocyanine dye.

### Claim 19 (depends on 1)

The composition of claim 1, wherein the ratio of TA to PS is 1 to 1 or 2 to 1.
