# US 9,433,673 B2 · Silicon dioxide nanoparticles and the use thereof for vaccination

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- Number: US 9,433,673 B2
- Document ID: US9433673B2
- Status: Granted
- Kind: B2
- Application number: 14/611,891
- Filed: 2015-02-02
- Published: 2015-08-13
- Granted: 2016-09-06
- Earliest claimed: 2008-07-15
- Assignees: Merck Patent GmbH
- Applicants: Merck Patent GmbH
- Inventors: Markus Weigandt; Andrea Hanefeld; Armin Kuebelbeck; Gregor Larbig
- Web page: https://patentgrep.com/patent/US9433673B2

## CPC

- A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants
- 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 9/10: Dispersions; Emulsions
- A61K 9/143: {with inorganic compounds}
- A61K 9/5115: {Inorganic compounds}
- A61K 39/0005: {Vertebrate antigens (from snakes A61K39/38)}
- A61K 47/52: the modifying agent being an inorganic compound, e.g. an inorganic ion that is complexed with the active ingredient
- A61K 47/54: the modifying agent being an organic compound
- A61K 47/643: {Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]}
- A61K 47/6923: {the form being an inorganic particle, e.g. ceramic particles, silica particles, ferrite or synsorb}
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/04: Antibacterial agents
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/04: Immunostimulants
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- A61K 2039/55505: {Inorganic adjuvants}
- A61K 2039/62: {characterised by the link between antigen and carrier}
- Y10T 428/2982: Particulate matter [e.g., sphere, flake, etc.]
- 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
- Y10T: TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION

## Abstract

The invention relates to ultrasmall, monodisperse nanoparticles comprising silicon dioxide to the surface of which at least one antigen is attached. The nanoparticles can be used for the immunoprophylaxis or immunotherapy of cancer. The invention also relates to a method for the targeting of antigens at antigen-presenting cells and for the activation of the immune system, where the efficiency of targeting and/or immunoactivation are set via the particle characteristics. The invention also relates to a method for the active and passive immunization of a mammal.

## Claims

### Claim 1

A method for the activation of the immune system of a patient in need thereof and providing an adjuvant immune response, comprising parenterally administering to a patient in need thereof, monodisperse nanoparticles of silicon dioxide, where the nanoparticles have a diameter of 5 to 50 nm and are free of additional adjuvants.

### Claim 2 (depends on 1)

The method of claim 1, wherein the patient is suffering from an infectious disease, septic shock, a tumor, cancer, an autoimmune disease, an allergic or a chronic or acute inflammation process.

### Claim 3 (depends on 1)

The method of claim 1, wherein the nanoparticles have a size between 20 and 30 nm.

### Claim 4 (depends on 1)

The method of claim 1, for activating the complement system of the immune system in a patient in need thereof.

### Claim 5 (depends on 1)

The method of claim 1, wherein the nanoparticles are passively targeted at antigen-presenting cells.

### Claim 6 (depends on 1)

The method of claim 1, additionally comprising administering an antigen, and thereby targeting the antigen at antigen-presenting cells.

### Claim 7 (depends on 6)

The method of claim 6, wherein the antigen is targeted at dendritic cells in lymph nodes.

### Claim 8 (depends on 6)

The method of claim 6, wherein the antigen is attached to a surface functionality on the nanoparticles.

### Claim 9 (depends on 6)

The method of claim 6, wherein the antigen is a cancer antigen.

### Claim 10 (depends on 6)

The method of claim 6, wherein the antigen is survivin.

### Claim 11

A method for the induction of a T-cell response, antibody response and/or dendritic cell maturation in a mammal, comprising administering an effective amount of a monodispersion of nanoparticles having a diameter of 5 to 50 nm suitable for parenteral administration and a solvent to said mammal,
wherein the nanoparticles comprise
a) a silicon dioxide matrix, and
b) a surface functionality to which an antigen to be targeted is attached,
with the proviso that neither said surface functionality nor said antigen is a major histocompatibility (MHC) molecule, and
wherein the proliferation of T-cells and/or dendritic cells and/or the formation of neutralizing antibodies is induced.

### Claim 12 (depends on 11)

A method for the passive immunization of a mammal, comprising isolating T-cells proliferated by and/or antibodies formed by the method of claim 11, and administering said T-cells and/or antibodies to a mammal.