# US 2024/0197909 A1 · Nanoparticles as carrier-system for adjuvants/antigens

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- Number: US 2024/0197909 A1
- Document ID: US20240197909A1
- Status: Published application
- Kind: A1
- Application number: 17/998,318
- Filed: 2021-05-12
- Published: 2024-06-20
- Earliest claimed: 2020-05-12
- Assignees: Life Science Inkubator GmbH; Deutsches Krebsforschungszentrum Stiftung des Offentlichen Rechts
- Applicants: LIFE SCIENCE INKUBATOR GMBH & Co. KG; Deutsches Krebsforschungszentrum Stiftung Des öFfentlichen Rechts
- Inventors: Armin KÜBELBECK; Angelika RIEMER; Sebastian KRUSE; Eva FEIDT; Agnieszka GRABOWSKA; Ellen JUNGLAS
- Web page: https://patentgrep.com/patent/US20240197909A1

## CPC

- A61K 39/385: Haptens or antigens, bound to carriers
- A61K 39/12: Viral antigens
- A61K 39/145: Orthomyxoviridae, e.g. influenza virus
- A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants
- A61K 47/6923: {the form being an inorganic particle, e.g. ceramic particles, silica particles, ferrite or synsorb}
- A61K 47/6929: {the form being a nanoparticle, e.g. an immuno-nanoparticle}
- A61K 47/6931: {the material constituting the nanoparticle being a polymer}
- A61P 31/20: for DNA viruses
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- C07K 14/025: Papovaviridae, e.g. papillomavirus, polyomavirus, SV40, BK virus, JC virus
- A61K 2039/55555: {Liposomes; Vesicles, e.g. nanoparticles; Spheres, e.g. nanospheres; Polymers}
- A61K 2039/55561: {CpG containing adjuvants; Oligonucleotide containing adjuvants}
- A61K 2039/572: {cytotoxic response}
- A61K 2039/585: {wherein the target is cancer}
- C12N 2710/20034: Use of virus or viral component as vaccine, e.g. live-attenuated or inactivated virus, VLP, viral protein
- 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
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The disclosure relates to immunological compositions (immunostimulants) based on nanoparticles as carrier for adjuvants, optionally in combination with antigens or epitopes, in particular for the use of the compositions for immunoprophylaxis or immunotherapy.

## Claims

### Claim 1

Composition comprising nanoparticles which are loaded with pharmaceutically acceptable compounds comprising polyinosinic:polycytidylic acid, poly(I:C) or any derivatives thereof, having silicon dioxide and functional groups on the surface, wherein
the functional groups are capable to carry and/or stabilize both negative and positive charges of the pharmaceutically acceptable compounds,
the zeta potential of the composition has a value of at least ±15 mV,
the nanoparticles have a particle size below 150 nm.

### Claim 2 (depends on 1)

Composition according to claim 1, wherein the nanoparticles are loaded with pharmaceutically acceptable compounds comprising polyinosinic:polycytidylic acid, (poly(I:C)) or any derivatives thereof and an antigen or epitope.

### Claim 3 (depends on 1)

Composition according to claim 1, wherein derivatives of poly(I:C) are poly(I:C) LMW (Low Molecular Weight Poly(I:C) with an average size from 0.2 kb to 1 kb), poly(I:C) HMW (High Molecular Weight Poly(I:C) with an average size from 1.5 kb to 8 kb), polyI:polyC12U.

### Claim 4 (depends on 1)

Composition according to claim 1, wherein the nanoparticles have a surface loading density up to 0.5, in relation to the total number of the pharmaceutically acceptable compounds with regard to the surface of the nanoparticle in nm2 [molecules/nm2].

### Claim 5 (depends on 1)

Composition according to claim 1, wherein the Polydispersity Index (PDI) of the composition is between 0 and 0.32.

### Claim 6 (depends on 1)

Composition according to claim 1, wherein the zeta potential of the composition has a value of at least ±30 mV.

### Claim 7 (depends on 1)

Composition according to claim 1, wherein the net charge of the loaded nanoparticles in total is different to zero.

### Claim 8 (depends on 1)

Composition according to claim 1, wherein the functional groups are connected to a linker L which is linked to the surface of the nanoparticles by way of a covalent or adsorptive bond.

### Claim 9 (depends on 8)

Composition according to claim 8, wherein the linker compound L comprises at least one carboxyl (—COOH) or carboxylate (—COO−) group as functional group.

### Claim 10 (depends on 8)

Composition according to claim 8, wherein the linker compound L comprises at least one guanidino-group (—NHC(═NH)NH2 or —NHC(═NH2+)NH2) or amino-group (—NH2 or —NH3+) group as a functional group.

### Claim 11 (depends on 8)

Composition according to claim 8, wherein the linker L comprises at least one further functional group L′, which is selected from the group —SH, —COOH, —NH2, -guanidino-group (—NHC(═NH))NH2), —PO3H2, —PO2CH3H, —SO3H, —OH, —NR3+X−.

### Claim 12 (depends on 1)

Composition according to claim 1, wherein the pharmaceutically acceptable compounds are conjugated to the nanoparticle by adsorptive attachment.

### Claim 13 (depends on 1)

Composition according to claim 1 for use as immunostimulant.

### Claim 14 (depends on 1)

Composition according to claim 1 for the use of the prevention and/or treatment of bovine respiratory disease (BRD).

### Claim 15 (depends on 1)

Compositions according to claim 1 for perioperative immune stimulation in humans.