# US 11,896,713 B2 · Strategies to enhance lung cancer treatment

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- Number: US 11,896,713 B2
- Document ID: US11896713B2
- Status: Granted
- Kind: B2
- Application number: 17/508,535
- Filed: 2021-10-22
- Published: 2022-04-28
- Granted: 2024-02-13
- Earliest claimed: 2020-10-22
- Assignees: Rutgers, The State University of New Jersey
- Applicants: Rutgers, The State University of New Jersey
- Inventors: Tamara Minko; Olga B. Garbuzenko
- Web page: https://patentgrep.com/patent/US11896713B2

## CPC

- A61K 9/1272: comprising non-phosphatidyl surfactants as bilayer-forming substances, e.g. cationic lipids or non-phosphatidyl liposomes coated or grafted with polymers (lipids as modifying agents {A61K47/543})
- A61K 9/0078: {for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions}
- A61K 9/127: Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A61K 9/5123: {Organic compounds, e.g. fats, sugars}
- A61K 31/277: having a ring, e.g. verapamil
- A61K 31/282: Platinum compounds
- A61K 31/337: having four-membered rings, e.g. taxol
- A61K 31/365: Lactones
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61K 31/553: having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
- A61K 31/704: attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)}
- A61K 33/243: Platinum; Compounds thereof
- 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)
- A61P 35/00: Antineoplastic agents
- 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

## Abstract

A nanocarrier containing a combination of bioactive agents is provided. The nanocarrier allows for targeted delivery of the agents to cancer cells with minimized side effect.

## Claims

### Claim 1

A nanocarrier system formulated for in vivo delivery of an anticancer agent by inhalation, comprising:
(a) a lipid nanoparticle comprising a lipid matrix consisting essentially of at least one lipid that is solid at room temperature and at least one lipid that is liquid at room temperature;
(b) an anticancer agent incorporated in imperfections in the lipid matrix;
(c) a first group of polyethylene glycols (PEGs) extending from the surface of the nanoparticle, wherein the PEGs each have an inner terminus bonded to an anchor lipid in the nanoparticle and an outer terminus;
(d) a ligand bonded to the outer terminus of the first group of PEGs, wherein the ligand is specific to receptors overexpressed in cancer cells; and
(e) one or more siRNAs distributed on the surface of the nanoparticle;
wherein the lipid nanoparticle is not a liposome.

### Claim 2 (depends on 1)

The nanocarrier system of claim 1, wherein the lipid nanoparticle comprises two or more lipids selected from the group consisting of triglycerides, partial glycerides, fatty acids, and steroids and waxes.

### Claim 3 (depends on 1)

The nanocarrier system of claim 1, wherein the anticancer agent is selected from the group consisting of cisplatin, carboplatin, paclitaxel, doxorubicin, erlotinib, gefitinib, afatinib, dacomitinib, osimertinib imatinib, PD 153035, picropodophyllin, PP2, staurosporine, and Tyrphostin AG 490.

### Claim 4 (depends on 1)

The nanocarrier system of claim 1, wherein the first group of PEGs has a molecular weight ranging from about 1000 to about 3000 daltons.

### Claim 5 (depends on 1)

The nanocarrier system of claim 1, wherein the anchor lipid is selected from the group consisting of 1,2-Distearoyl-sn-glycero-3-phosphoethanolamine (DSPE), N-[1-(2,3-Dioleoyloxy)propyl]-N,N,N-trimethylammonium methyl-sulfate (DOTAP), and dioleoylphosphatidylethanolamine (DOPE).

### Claim 6 (depends on 1)

The nanocarrier system of claim 1, wherein the ligand is Gln-His-Trp-Ser-Tyr-DLys(D-Cys)-Leu-Arg-Pro.

### Claim 7 (depends on 1)

The nanocarrier system of claim 1, further comprising a second group of PEGs extending from the surface of the nanoparticle, wherein the second group of PEGs are not bonded to the ligand.

### Claim 8 (depends on 1)

The nanocarrier system of claim 1, wherein the nanoparticle has an average diameter ranging from about 100 to about 300 nm.

### Claim 9 (depends on 1)

The nanocarrier system of claim 1, wherein the anticancer agent is cisplatin or carboplatin.

### Claim 10 (depends on 1)

The nanocarrier system of claim 1, wherein the siRNAs target one or more of EGFR1, EGFR2, EGFR3, and EGFR4.

### Claim 11 (depends on 1)

A kit comprising the nanocarrier system of claim 1.

### Claim 12 (depends on 11)

The kit of claim 11, which is a nebulizer.

### Claim 13 (depends on 1)

A method of treating cancer comprising administering the nanocarrier system of claim 1 by inhalation.

### Claim 14 (depends on 13)

The method of claim 13, wherein the cancer is small cell lung cancer.

### Claim 15 (depends on 13)

The method of claim 13, wherein the cancer is non-small cell lung cancer.

### Claim 16 (depends on 13)

The method of claim 13, further comprising administering to the subject an additional therapy selected from the group consisting of chemotherapy, radiotherapy, gene therapy, surgery, hormonal therapy, anti-angiogenic therapy and immunotherapy.

### Claim 17 (depends on 13)

The method of claim 13, wherein the cancer is resistant to the treatment of a prior tyrosine kinase inhibitor.