# US 11,077,190 B2 · Nanoparticle delivery system for targeted anti-obesity treatment

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- Number: US 11,077,190 B2
- Document ID: US11077190B2
- Status: Granted
- Kind: B2
- Application number: 16/543,161
- Filed: 2019-08-16
- Published: 2019-12-12
- Granted: 2021-08-03
- Earliest claimed: 2014-01-06
- Assignees: University of Wyoming
- Applicants: University of Wyoming
- Inventors: Baskaran Thyagarajan; Padmamalini Baskaran
- Web page: https://patentgrep.com/patent/US11077190B2

## CPC

- A61K 41/00: Medicinal preparations obtained by treating materials with wave energy or particle radiation {; Therapies using these preparations}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/5031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)}
- A61K 9/5094: {Microcapsules containing magnetic carrier material, e.g. ferrite for drug targeting}
- A61K 9/5153: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61K 31/165: having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K 31/23: of acids having a carboxyl group bound to a chain of seven or more carbon atoms
- A61K 31/231: having one or two double bonds
- A61K 31/357: having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
- A61K 31/7034: attached to a carbocyclic compound, e.g. phloridzin
- A61K 41/0052: {Thermotherapy; Hyperthermia; Magnetic induction; Induction heating therapy}
- A61K 47/6941: {the form being a granulate or an agglomerate}
- 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 47/02: Inorganic compounds
- Y10S 977/773: Nanoparticle, i.e. structure having three dimensions of 100 nm or less
- Y10S 977/906: 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)
- Y10S: TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS

## Abstract

A magnetic nanoparticle including a TRPV1 agonist, as well as methods of preparation and use, are described herein. A magnetically responsive pharmaceutical can include a core region having a magnetic nanoparticle (MNPs) and a TRPV1 protein agonist. Further, an exterior coating comprising a polymer can be formed around the core region. The magnetically responsive pharmaceutical can be administered to a recipient and directed to a target region using an external magnetic field.

## Claims

### Claim 1

A method for making a magnetically responsive pharmaceutical, comprising:
precipitating ferromagnetic metal salts in the presence of ammonium hydroxide to obtain magnetic nanoparticles (MNPs);
depositing a TRPV1 protein agonist around the MNPs; and
coating the MNPs and the TRPV1 protein agonist with a biodegradable polymer.

### Claim 2 (depends on 1)

The method of claim 1, wherein the ferromagnetic metal salts are selected from the group consisting of iron, cobalt, nickel, and combinations thereof.

### Claim 3 (depends on 2)

The method of claim 2, wherein the ferromagnetic metal salts are selected from the group consisting of iron (II) sulfate, iron (II) nitrate, iron (II) chloride, iron (II) perchlorate, iron (III) sulfate, iron (III) nitrate, iron (III) chloride, iron (III) perchlorate, and combinations thereof.

### Claim 4 (depends on 1)

The method of claim 1, wherein the TRPV1 agonist is selected from the group consisting of dihydrocapsiate, capsaicin, civamide, vanillin, endovanilloids, resiniferatoxin, N-Vanillylnonanamide, capsiate, Capsaicin β-D-Glucopyranoside, and combinations thereof.

### Claim 5 (depends on 4)

The method of claim 4, wherein the TRPV1 agonist is capsaicin.

### Claim 6 (depends on 1)

The method of claim 1, wherein the biodegradable polymer is selected from the group consisting of poly(lactic-co-glycolic acid) (PLGA), Polylactic acid (PLA), Polyglycolic acid (PGA), poly-D-lactic acid (PDLA), PLGA-dimethacrylate, fluorescent PLGA polymers, Poly(ethyl acrylate-co-methyl methacrylate-co-trimethylammonioethyl methacrylate chloride) 1:2:0.2, Poly(ethyl acrylate-co-methyl methacrylate-co-trimethylammonioethyl methacrylate chloride) 1:2:0.1, Ethyl cellulose, cellulose derivatives, and combinations thereof.

### Claim 7 (depends on 6)

The method of claim 6, wherein the biodegradable polymer is poly(lactic-co-glycolic acid) (PLGA).

### Claim 8 (depends on 1)

The method of claim 1, wherein the MNPs comprises metal ions, and wherein a molar ratio of biodegradable polymer to metal ions is between about 1:40 and about 1:300.

### Claim 9 (depends on 1)

The method of claim 1, wherein the TRPV1 protein agonist forms an intermediate layer over the MNPs.

### Claim 10 (depends on 1)

The method of claim 1, wherein the MNPs comprise Fe3+ and Fe2+ ions in a molar ratio of between about 3:1 and about 1:1 Fe3+ to Fe2+ ions.

### Claim 11 (depends on 1)

The method of claim 1, wherein the MNPs are between about 5 nm and about 30 nm in diameter.

### Claim 12 (depends on 1)

The method of claim 1, wherein the MNPs are precipitated by heating a mixture of the ferromagnetic metal salts, the TRPV1 agonist, and ammonium hydroxide to a temperature above 60 degrees Celsius followed by cooling to a temperature at or below room temperature.

### Claim 13 (depends on 1)

The method of claim 1, wherein an initial concentration of TRPV1 protein agonist deposited around the MNPs is between about 100 micromolar and about 1 millimolar.

### Claim 14 (depends on 13)

The method of claim 13, wherein a final concentration of TRPV1 protein agonist deposited around the MNPs is between about 1 micromolar and about 100 micromolar.

### Claim 15

A method for making a magnetically responsive pharmaceutical, comprising:
precipitating ferromagnetic metal salts in the presence of ammonium hydroxide to obtain magnetic nanoparticles (MNPs);
magnetically filtering and washing the MNPs;
depositing a TRPV1 protein agonist around the MNPs to form an intermediate layer over the MNPs; and
depositing a biodegradable polymer over the intermediate layer.

### Claim 16 (depends on 15)

The method of claim 15, wherein the ferromagnetic metal salts are selected from the group consisting of iron, cobalt, nickel, and combinations thereof.

### Claim 17 (depends on 16)

The method of claim 16, wherein the ferromagnetic metal salts are selected from the group consisting of iron (II) sulfate, iron (II) nitrate, iron (II) chloride, iron (II) perchlorate, iron (III) sulfate, iron (III) nitrate, iron (III) chloride, iron (III) perchlorate, and combinations thereof.

### Claim 18 (depends on 15)

The method of claim 15, wherein the TRPV1 agonist is selected from the group consisting of dihydrocapsiate, capsaicin, civamide, vanillin, endovanilloids, resiniferatoxin, N-Vanillylnonanamide, capsiate, Capsaicin β-D-Glucopyranoside, and combinations thereof.

### Claim 19 (depends on 18)

The method of claim 18, wherein the TRPV1 agonist is capsaicin.

### Claim 20 (depends on 18)

The method of claim 18, wherein the biodegradable polymer is selected from the group consisting of poly(lactic-co-glycolic acid) (PLGA), Polylactic acid (PLA), Polyglycolic acid (PGA), poly-D-lactic acid (PDLA), PLGA-dimethacrylate, fluorescent PLGA polymers, Poly(ethyl acrylate-co-methyl methacrylate-co-trimethylammonioethyl methacrylate chloride) 1:2:0.2, Poly(ethyl acrylate-co-methyl methacrylate-co-trimethylammonioethyl methacrylate chloride) 1:2:0.1, Ethyl cellulose, cellulose derivatives, and combinations thereof.