# US 8,772,258 B2 · Single walled carbon nanotube/sirna complexes and methods related thereto

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- Number: US 8,772,258 B2
- Document ID: US8772258B2
- Status: Granted
- Kind: B2
- Application number: 13/175,314
- Filed: 2011-07-01
- Published: 2012-01-05
- Granted: 2014-07-08
- Earliest claimed: 2010-07-02
- Assignees: Ensysce Biosciences Inc.
- Applicants: D. Lynn Kirkpatrick; Michelle K. Weiss
- Inventors: D. Lynn Kirkpatrick; Michelle K. Weiss
- Web page: https://patentgrep.com/patent/US8772258B2

## CPC

- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- 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 9/0092: {Hollow drug-filled fibres, tubes of the core-shell type, coated fibres, coated rods, microtubules or nanotubes}
- A61K 47/6925: {the form being a microcapsule, nanocapsule, microbubble or nanobubble}
- A61P 35/00: Antineoplastic agents
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- C12N 15/111: {General methods applicable to biologically active non-coding nucleic acids}
- C12N 2310/14: interfering nucleic acids [NA]
- C12N 2320/32: Special delivery means, e.g. tissue-specific
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- 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
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES

## Abstract

The present invention includes single-walled carbon nanotube compositions for the delivery of bioactive agents and methods of making such single-walled carbon nanotube compositions.

## Claims

### Claim 1

A method for delivering siRNA to tumorigenic tissue comprising:
administering via intravenous injection to a subject having tumorigenic tissue an effective amount of a pharmaceutical composition comprising
one or more short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes; and
a pharmaceutically acceptable excipient;
administering one or more subsequent doses of the pharmaceutical composition about every 12 to 24 hours based on effect without regard to blood plasma concentration levels of the short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes.

### Claim 2 (depends on 1)

The method of claim 1, wherein the subject is selected from a mammal, a mouse, and a human.

### Claim 3 (depends on 1)

The method of claim 1, wherein the subject is a human having cancer.

### Claim 4 (depends on 1)

The method of claim 1, wherein the effective amount comprises up to about 100 mg of the one or more short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes.

### Claim 5 (depends on 1)

The method of claim 1, wherein the effective amount comprises up to about 30 mg of the one or more short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes.

### Claim 6 (depends on 1)

The method of claim 1, wherein the effective amount comprises from about 15 mg to about 100 mg of the one or more short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes.

### Claim 7 (depends on 1)

The method of claim 1, wherein the effective amount comprises from about 15 mg to about 30 mg of the one or more short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes.

### Claim 8 (depends on 1)

The method of claim 1, wherein a substantial portion of the one or more short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes accumulates in the tumorigenic tissue at sufficient concentrations to inhibit expression of at least one target associated with the one or more short-interfering ribonucleic acid (siRNA)tissue within about 1 hour after administration.

### Claim 9 (depends on 1)

The method of claim 1, wherein substantially none of the one or more short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes are in circulation from about 5 to about 15 minutes after administration of the one or more short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes.

### Claim 10 (depends on 1)

The method of claim 1, wherein the effective amount of one or more short-interfering ribonucleic acid (siRNA) is non-covalently complexed to single-walled carbon nanotubes.

### Claim 11

A method for inhibiting expression of a gene in a subject comprising:
administering to the subject an effective amount of a pharmaceutical composition comprising:
an effective amount of one or more short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes; and
a pharmaceutically acceptable excipient;
and administering one or more subsequent doses of the pharmaceutical composition about every 12 to 24 hours based on effect without regard to blood plasma concentration levels of the short-interfering ribonucleic acid (siRNA) complexed to single-walled carbon nanotubes.

### Claim 12

A method for delivering siRNA to tumorigenic tissue comprising:
administering via intravenous injection to a subject having tumorigenic tissue a pharmaceutical composition comprising:
an effective amount of one or more short-interfering ribonucleic acid (siRNA) complexed to carbon nanotubes; and
a pharmaceutically acceptable excipient.
