# US 2016/0250332 A1 · Upconverting nanoparticles

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- Number: US 2016/0250332 A1
- Document ID: US20160250332A1
- Status: Published application
- Kind: A1
- Application number: 14/632,752
- Filed: 2015-02-26
- Published: 2016-09-01
- Earliest claimed: 2015-02-26
- Inventors: Amol Punjabi
- Web page: https://patentgrep.com/patent/US20160250332A1

## CPC

- A61N 5/062: {Photodynamic therapy, i.e. excitation of an agent}
- A61K 41/0061: {5-aminolevulinic acid-based PDT: 5-ALA-PDT involving porphyrins or precursors of protoporphyrins generated in vivo from 5-ALA}
- A61K 41/008: {Two-Photon or Multi-Photon PDT, e.g. with upconverting dyes or photosensitisers}
- A61K 47/6923: {the form being an inorganic particle, e.g. ceramic particles, silica particles, ferrite or synsorb}
- A61K 47/6929: {the form being a nanoparticle, e.g. an immuno-nanoparticle}
- C09K 11/025: {non-luminescent particle coatings or suspension media}
- C09K 11/7773: {with alkali or alkaline earth metal}
- A61N 2005/0659: {infrared}
- A61N 2005/0662: {Visible light}
- A61N: ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY (measurement of bioelectric currents A61B; surgical instruments, devices or methods for transferring non-mechanical forms of energy to or from the body A61B18/00; anaesthetic apparatus in general A61M; incandescent lamps H01K; infrared radiators for heating H05B)
- 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)
- C09K: MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE

## Abstract

Provided herein are lanthanide-containing upconverting nanoparticles, methods of their preparation, compositions, and methods of using the same. The polymers and compositions provided herein may be used, for example, in photodynamic therapy.

## Claims

### Claim 1

A nanoparticle comprising a rare earth metal fluoride composition according to the formula M1M2F4 comprising lanthanide ions, wherein M1 is the alkali metal, M2 is the rare earth, and wherein the composition comprises:
ytterbium in an amount from about 70 mol % to about 99 mol % of the rare earth present in the composition;
erbium in an amount from about 0.1 mol % to about 10 mol % of the rare earth present in the composition; and
yttrium in an amount from about 0 mol % to about 30 mol % of the rare earth present in the composition.

### Claim 2 (depends on 1)

The nanoparticle of claim 1 wherein the alkali metal is sodium.

### Claim 3 (depends on 2)

The nanoparticle of claim 2 comprising:
ytterbium in an amount of about 98 mol % of the rare earth present in the composition; and
erbium in an amount of about 2 mol % of the rare earth present in the composition.

### Claim 4 (depends on 2)

The nanoparticle of claim 2 comprising:
ytterbium in an amount of about 70 to 90 mol % of the rare earth present in the composition;
erbium in an amount of about 1 to 5 mol % of the rare earth present in the composition; and
yttrium in an amount from about 10 to 30 mol % of the rare earth present in the composition.

### Claim 5 (depends on 2)

The nanoparticle of claim 2 comprising:
ytterbium in an amount of about 80 mol % of the rare earth present in the composition;
erbium in an amount of about 2 mol % of the rare earth present in the composition; and
yttrium in an amount of about 18 mol % of the rare earth present in the composition.

### Claim 6 (depends on 2, 5)

An aqueous composition comprising the nanoparticle of claim 5. The nanoparticle of claim 2 further comprising a coating comprising calcium fluoride.

### Claim 8 (depends on 1)

The nanoparticle of claim 1 further comprising a photosensitizer, or precursor thereof.

### Claim 9 (depends on 8)

The nanoparticle of claim 8, wherein the photosensitizer or precursor thereof is covalently attached to the nanoparticle.

### Claim 10 (depends on 8)

The nanoparticle of claim 8, wherein the photosensitizer or precursor thereof is 5-aminolevulinic acid.

### Claim 11 (depends on 2)

The nanoparticle of claim 2 comprising:
ytterbium in an amount of about 80 mol % of the rare earth present in the composition;
erbium in an amount of about 2 mol % of the rare earth present in the composition; and
yttrium in an amount of about 18 mol % of the rare earth present in the composition;
a coating comprising calcium fluoride;
polyacrylic acid; and
5-aminolevulinic acid conjugated via a hydrazine linkage to the polyacrylic acid.

### Claim 12 (depends on 2)

A method of treating a tumor in a subject in need of such treatment comprising:
administering to the subject an effective amount of the nanoparticle of claim 2;
administering to the subject an effective amount of a photosensitizer or precursor thereof; and
subsequently administering to the subject an effective amount of infra-red radiation.

### Claim 13 (depends on 12)

The method of claim 12, wherein the nanoparticle comprises the photosensitizer or precursor thereof.

### Claim 14 (depends on 12)

The method of claim 12, wherein the photosensitizer or precursor thereof is covalently attached to the nanoparticle.

### Claim 15 (depends on 12)

The method of claim 12, wherein the photosensitizer or precursor thereof is 5-aminolevulinic acid.

### Claim 16 (depends on 11)

A method of treating a tumor in a subject in need of such treatment comprising:
administering to the subject an effective amount of the nanoparticle of claim 11; and
subsequently administering to the subject an effective amount of infra-red radiation.

### Claim 17

A method of preparing an upconverting nanoparticle comprising reacting in a reaction mixture rare earth trifluoroacetates and sodium trifluoroacetate under conditions sufficient to form a sodium rare earth trifluoroacetate, wherein the rare earth trifluoroacetates are selected from the group consisting of:
ytterbium trifluoroacetate in an amount from about 70 mol % to about 99 mol % of the rare earth trifluoroacetates present in the reaction mixture;
erbium trifluoroacetate in an amount from about 0.1 mol % to about 10 mol % of the rare earth trifluoroacetates present in the reaction mixture; and
yttrium trifluoroacetate in an amount from about 0.1 mol % to about 10 mol % of the rare earth trifluoroacetates present in the reaction mixture.

### Claim 18 (depends on 17)

A method according to claim 17 wherein the rare earth trifluoroacetates consist of:
ytterbium trifluoroacetate in an amount of about 80 mol % of the rare earth trifluoroacetates present in the reaction mixture;
erbium trifluoroacetate in an amount of about 2 mol % of the rare earth trifluoroacetates present in the reaction mixture; and
yttrium trifluoroacetate in an amount of about 18 mol % of the rare earth trifluoroacetates present in the reaction mixture.

### Claim 19 (depends on 17)

A nanoparticle prepared according to the method of claim 17.

### Claim 20 (depends on 18)

A nanoparticle prepared according to the method of claim 18.