# US 9,517,201 B2 · Nanocarrier and nanogel compositions

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- Number: US 9,517,201 B2
- Document ID: US9517201B2
- Status: Granted
- Kind: B2
- Application number: 12/936,392
- Filed: 2009-04-06
- Published: 2011-05-19
- Granted: 2016-12-13
- Earliest claimed: 2008-04-04
- Assignees: Rutgers, The State University of New Jersey
- Applicants: Patrick J. Sinko; Stanley Stein; Hilliard Kutscher; Manjeet Deshmukh; Anupa Menjoge; Yashveer Singh; Simi Gunaseelan
- Inventors: Patrick J. Sinko; Stanley Stein; Hilliard Kutscher; Manjeet Deshmukh; Anupa Menjoge; Yashveer Singh; Simi Gunaseelan
- Web page: https://patentgrep.com/patent/US9517201B2

## CPC

- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 9/10: Dispersions; Emulsions
- A61K 9/1641: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers}
- A61K 31/704: attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- 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 49/003: {Thiazine dyes}
- A61K 49/0043: {Fluorescein, used in vivo}
- A61K 49/0054: {Macromolecular compounds, i.e. oligomers, polymers, dendrimers}
- A61P 35/00: Antineoplastic agents
- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- A61K 9/51: Nanocapsules; {Nanoparticles; (nanotubes A61K9/0092; polymeric micelles A61K9/1075; polymersomes A61K9/1273; pure drug nanoparticles A61K9/14; drug nanoparticles with adsorbed surface modifiers A61K9/141; conjugates, e.g. between drug and non-active nanoparticles, A61K47/50; preparations for in vivo diagnosis A61K49/00; with radioactive substances A61K51/00)}
- A61K 47/51: the non-active ingredient being a modifying agent
- A61K 47/56: the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K 47/6925: {the form being a microcapsule, nanocapsule, microbubble or nanobubble}
- Y10T 428/2982: Particulate matter [e.g., sphere, flake, etc.]
- 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
- Y10T: TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION

## Abstract

Novel classes of multi-arm polyalkylene oxide-based materials including PEG nanocarriers, nanogel particles, and aggregated nanogel particles are disclosed. These classes of compositions may be associated with therapeutic agents and targeting moieties, or visibility enhancing agents, and may have a modified surface structure. In some embodiments the PEG-based materials can be made to provide relatively high drug loads with improved solubility and targeted delivery.

## Claims

### Claim 1

A nanocarrier, comprising two doxorubicin molecules (Dox) coupled to at least one end of a linear polyalkylene oxide or a four-arm polyalkylene oxide by the linker Glu(Leu-Gly)2 SEQ ID No: 1, wherein two or four Dox are coupled to said linear polyalkylene oxide and eight Dox are coupled to said four-arm polyalkylene oxide.

### Claim 2 (depends on 1)

The nanocarrier of claim 1, wherein four Dox are coupled to said linear polyalkylene oxide and eight Dox are coupled to said four-arm polyalkylene oxide.

### Claim 3 (depends on 1)

The nanocarrier of claim 1, wherein the aqueous solubility is at least about 100 mg/ml.

### Claim 4 (depends on 1)

The nanocarrier of claim 1, wherein the four-arm polyalkylene oxide is four-arm polyethylene glycol.

### Claim 5 (depends on 1)

The nanocarrier of claim 1, further comprising a targeting moiety.

### Claim 6 (depends on 5)

The nanocarrier of claim 5, wherein the targeting moiety is peptide.

### Claim 7 (depends on 5)

The nanocarrier of claim 5, wherein the targeting moiety is selected from the group consisting of an RGD peptide, a DV3 peptide, a LYP peptide, a membrane binding domain of IGFBP3, fMLF, mannose, transferrin ligand, and a monoclonal antibody.