# US 12,178,908 B2 · Tolerogenic liposomes and methods of use thereof

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- Number: US 12,178,908 B2
- Document ID: US12178908B2
- Status: Granted
- Kind: B2
- Application number: 16/975,789
- Filed: 2019-02-26
- Published: 2020-12-31
- Granted: 2024-12-31
- Earliest claimed: 2018-02-26
- Assignees: AnTolRx, Inc.
- Applicants: AnTolRx, Inc.
- Inventors: Aditi Jhaveri; Vincent P. Stanton, Jr.
- Web page: https://patentgrep.com/patent/US12178908B2

## CPC

- 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 9/1272: 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 9/0031: {Rectum, anus}
- A61K 9/0034: {Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants}
- A61K 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays}
- A61K 9/007: {Pulmonary tract; Aromatherapy}
- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K 9/127: Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A61K 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911})
- A61K 31/711: Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61K 39/0008: {Antigens related to auto-immune diseases; Preparations to induce self-tolerance}
- A61K 39/001193: {Prostate associated antigens e.g. Prostate stem cell antigen [PSCA]; Prostate carcinoma tumor antigen [PCTA]; PAP or PSGR}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 2039/5256: {expressing foreign proteins}
- A61K 2039/53: {DNA (RNA) vaccination}
- A61K 2039/55555: {Liposomes; Vesicles, e.g. nanoparticles; Spheres, e.g. nanospheres; Polymers}
- A61K 2039/577: {tolerising response}
- 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)

## Abstract

The invention provides compositions (e.g., liposomes) for treating diseases and conditions associated with pathologic immune responses and methods for formulating and administering such compositions.

## Claims

### Claim 1

A composition comprising a population of liposomes having an average diameter from 50 to 250 nanometers (nm), wherein the population of liposomes comprises:
(i) a lipid mixture comprising (a) at least 50% of egg phosphatidylcholine or 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC); (b) between 26 mole percentage and 34 mole percentage cholesterol; and (c) a saturated poly(ethylene glycol) (PEG) derivatized lipid;
(ii) an average from 200-15,000 molecules of 2-(1H-Indol-3-ylcarbonyl)-4-thiazolecarboxylic acid methyl ester (ITE), or salt thereof, per liposome.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the lipid mixture comprises egg phosphatidylcholine and cholesterol, wherein the egg phosphatidylcholine accounts for at least 50% of the lipid mixture and the cholesterol accounts for 30-32 mole percentage of the mixture.

### Claim 3 (depends on 1)

The composition of claim 1 wherein the lipid mixture comprises 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) and cholesterol, wherein the DOPC accounts for at least 50% of the lipid mixture and the cholesterol accounts for 30-32 mole percentage of the mixture.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the saturated PEG derivatized lipid is PEG2000-DSPE.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the population of liposomes further comprises an antigen at a mass ratio of antigen-to-ITE from 1:10 to 100:1.

### Claim 6 (depends on 5)

The composition of claim 5, wherein the antigen is a peptide antigen comprising an amino acid sequence selected from the group consisting of SEQ ID NOs: 1-81.

### Claim 7 (depends on 5)

The composition of claim 5, wherein the antigen is associated with an autoimmune disorder.

### Claim 8 (depends on 5)

The composition of claim 5, wherein the antigen comprises a therapeutic agent, wherein the therapeutic agent is:
(i) a therapeutic protein or peptide;
(ii) a virus or capsid protein or peptide; and/or
(iii) a polynucleotide encoding (i) and/or (ii).

### Claim 9 (depends on 1)

The composition of claim 1, wherein the population of liposomes has an average zeta potential from −10 to −50 mv.