# US 9,750,694 B2 · Transpulmonary liposome for controlling drug arrival

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- Number: US 9,750,694 B2
- Document ID: US9750694B2
- Status: Granted
- Kind: B2
- Application number: 14/108,826
- Filed: 2013-12-17
- Published: 2014-04-17
- Granted: 2017-09-05
- Earliest claimed: 2007-03-30
- Assignees: Hirofumi Takeuchi; Otsuka Pharmaceutical Co., Ltd.
- Applicants: Hirofumi Takeuchi; Otsuka Pharmaceutical Co., Ltd.
- Inventors: Hirofumi Takeuchi; Koji Nakano; Hidekazu Toyobuku
- Web page: https://patentgrep.com/patent/US9750694B2

## CPC

- A61K 9/1277: Preparation processes; Proliposomes
- A61K 9/007: {Pulmonary tract; Aromatherapy}
- 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 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911})
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/36: Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K 48/0075: {characterised by an aspect of the delivery route, e.g. oral, subcutaneous}
- A61P 11/00: Drugs for disorders of the respiratory system
- C12N 15/88: using microencapsulation, e.g. using {amphiphile} liposome vesicle
- A61K 48/00: Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
- C12N 2810/10: Vectors comprising a non-peptidic targeting moiety
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

An object of the present invention is to provide a liposome which is excellent in intrapulmonary delivery controllability of drugs or genes and is suited for pulmonary administration. By modifying the surface of a liposome using a terminal hydrophobized polyvinyl alcohol and/or chitosan, retention of drugs or genes encapsulated in the liposome on the surface of lung tissue and transfer of drugs or genes into lung tissue can be properly modulated, and thus in vivo behavior can be controlled.

## Claims

### Claim 1

A method for treating a disease of lung tissue, comprising the step of administering to a lung of a patient suffering from the disease of lung tissue and needing fast-transfer of a drug or a gene into the lung tissue a therapeutically effective amount of a liposome preparation for pulmonary administration in which a drug or a gene is encapsulated in a liposome having a liposome membrane surface modified with a chitosan, thereby transferring the drug or the gene to the inside of a lung tissue,
wherein the liposome contains the chitosan in a proportion of 5 to 250 parts by weight, per 100 parts by weight of a total amount of all constituent components of the liposomal membrane; and
wherein the chitosan has a molecular weight from 100,000 to 150,000 daltons and a degree of deacetylation of 80% to 100%.

### Claim 2 (depends on 1)

The method for treating a disease of lung tissue according to claim 1, wherein the liposome contains a phospholipid as a constituent component of a liposomal membrane.

### Claim 3 (depends on 1)

The method for treating a disease of lung tissue according to claim 1,
wherein the liposome for pulmonary administration contains phosphatidylcholine, cholesterol and a dialkyl phosphate ester as constituent components of the liposomal membrane.

### Claim 4 (depends on 1)

The method for treating a disease of lung tissue according to claim 1, wherein the gene is at least one nucleic acid selected from the group consisting of siRNA, mRNA, rRNA, micro RNA, ribozymes, antisense oligonucleotide, decoy oligonucleotide, plasmid DNA, peptide nucleic acid, tri plex forming oligonucleotide, aptamer, and isolated DNA.

### Claim 5 (depends on 1)

The method for treating a disease of lung tissue according to claim 1, wherein the lung administrated the liposome is that of the patient needing fast-transfer of the gene into the lung tissue.