# US 12,758,556 B2 · Compositions and methods for the delivery of therapeutics

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- Number: US 12,758,556 B2
- Document ID: US12758556B2
- Status: Granted
- Kind: B2
- Application number: 17/655,112
- Filed: 2022-03-16
- Published: 2022-07-07
- Granted: 2026-10-13
- Earliest claimed: 2014-10-09
- Assignees: Board of Regents of the University of Nebraska
- Applicants: Board of Regents of the University of Nebraska
- Inventors: Howard E. Gendelman; Xin-Ming Liu; Benson Edagwa
- Web page: https://patentgrep.com/patent/US12758556B2

## CPC

- A61K 31/52: Purines, e.g. adenine
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/5146: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides}
- A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
- A61K 47/542: {Carboxylic acids, e.g. a fatty acid or an amino acid}
- A61K 47/551: {one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic 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)
- A61K 47/6901: {Conjugates being cells, cell fragments, viruses, ghosts, red blood cells or viral vectors}
- A61K 47/6907: {the form being a microemulsion, nanoemulsion or micelle}
- A61K 47/6921: {the form being a particulate, a powder, an adsorbate, a bead or a sphere}
- A61K 47/6929: {the form being a nanoparticle, e.g. an immuno-nanoparticle}
- C07D 411/04: directly linked by a ring-member-to-ring-member bond
- C07D 473/16: two nitrogen atoms
- 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)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention provides compositions and methods for the delivery of antivirals to a cell or subject.

## Claims

### Claim 1

A nanoparticle comprising an amphiphilic block copolymer comprising at least one block of poly(oxyethylene) and at least one block of poly(oxypropylene) coating a crystal of a compound having the formula:
wherein R is a C4-C22 unsaturated or saturated aliphatic or alkyl chain.

### Claim 2 (depends on 1)

The nanoparticle of claim 1, wherein the diameter of the nanoparticle is about 100 nm to 1 μm.

### Claim 3 (depends on 1)

The nanoparticle of claim 1, wherein said amphiphilic block copolymer is poloxamer 407.

### Claim 4 (depends on 1)

The nanoparticle of claim 1, wherein said nanoparticle further comprises an amphiphilic block copolymer linked to at least one targeting ligand.

### Claim 5 (depends on 1)

The nanoparticle of claim 1, wherein said amphiphilic block copolymer is linked to at least one targeting ligand.

### Claim 6 (depends on 4)

The nanoparticle of claim 4, wherein said targeting ligand is a macrophage targeting ligand.

### Claim 7 (depends on 6)

The nanoparticle of claim 6, wherein said macrophage targeting ligand is folate.

### Claim 8 (depends on 1)

The nanoparticle of claim 1, wherein said nanoparticle comprises poloxamer 407 linked to folate.

### Claim 9 (depends on 1)

The nanoparticle of claim 1, wherein said R is —(CH2)12CH3.

### Claim 10

A nanoparticle comprising a compound having the formula:
wherein R is a C4-C22 unsaturated or saturated aliphatic or alkyl chain.

### Claim 11 (depends on 10)

The nanoparticle of claim 10, further comprising at least one surfactant.

### Claim 12 (depends on 11)

The nanoparticle of claim 11, wherein the at least one surfactant is an amphiphilic block copolymer, polysorbate, phospholipid, derivative thereof, or combination thereof.

### Claim 13 (depends on 11)

The nanoparticle of claim 11, wherein the at least one surfactant is an amphiphilic block copolymer.

### Claim 14 (depends on 10)

The nanoparticle of claim 10, wherein R is —(CH2)12CH3.

### Claim 15 (depends on 1)

A pharmaceutical composition comprising at least one nanoparticle of claim 1 and at least one pharmaceutically acceptable carrier.

### Claim 16 (depends on 15)

The pharmaceutical composition of claim 15, wherein said pharmaceutical composition further comprises an additional anti-HIV compound.

### Claim 17 (depends on 10)

A pharmaceutical composition comprising at least one nanoparticle of claim 10 and at least one pharmaceutically acceptable carrier.

### Claim 18 (depends on 1)

A method for treating and/or reducing the incidence of an HIV infection in a subject in need thereof, said method comprising administering to said subject a nanoparticle of claim 1.

### Claim 19 (depends on 18)

The method of claim 18, further comprising the administration of an additional anti-HIV compound.

### Claim 20 (depends on 10)

A method for treating or reducing the incidence of an HIV infection in a subject in need thereof, said method comprising administering to said subject a nanoparticle of claim 10.