# US 2023/0053600 A1 · Porous silicon nanoparticle-based drug delivery system inducing reactive oxygen species and self-activation thereof, and method for preparing same

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- Number: US 2023/0053600 A1
- Document ID: US20230053600A1
- Status: Published application
- Kind: A1
- Application number: 17/739,616
- Filed: 2022-05-09
- Published: 2023-02-23
- Earliest claimed: 2021-08-02
- Assignees: University-Industry Cooperation Group of Kyung Hee University
- Applicants: University-Industry Cooperation Group of Kyung Hee University
- Inventors: Do Kyoung Kim; Rae Hyung Kang
- Web page: https://patentgrep.com/patent/US20230053600A1

## CPC

- A61K 47/6929: {the form being a nanoparticle, e.g. an immuno-nanoparticle}
- A61K 41/0057: {Photodynamic therapy with a photosensitizer, i.e. agent able to produce reactive oxygen species upon exposure to light or radiation, e.g. UV or visible light; photocleavage of nucleic acids with an agent}
- 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 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61K 47/6923: {the form being an inorganic particle, e.g. ceramic particles, silica particles, ferrite or synsorb}
- B82Y 5/00: Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
- 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)
- B82Y: SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES

## Abstract

Proposed is a porous silicon nanoparticle with isothiocyanate moiety conjugated to the surface. The porous silicon nanoparticle with isothiocyanate moiety conjugated to the surface has low side effects due to high biocompatibility, and can generate reactive oxygen species in cells without an external initiator, which can promote decomposition and release of supported drugs.

## Claims

### Claim 1

A drug delivery system comprising:
a porous silicon nanoparticles; and
an isothiocyanate moiety conjugated to the surface of the porous silicon nanoparticle.

### Claim 2 (depends on 1)

The drug delivery system of claim 1, wherein the drug delivery system further comprises a drug or prodrug supported on the porous silicon nanoparticles.

### Claim 3 (depends on 2)

The drug delivery system of claim 2, wherein the prodrug is converted into a drug by reactive oxygen species.

### Claim 4 (depends on 1)

The drug delivery system of claim 1, wherein the drug delivery system further comprises a tumor homing peptide conjugated to the surface of the porous silicon nanoparticles.

### Claim 5 (depends on 4)

The drug delivery system of claim 4, wherein the tumor homing peptide is at least one peptide selected from the group consisting of an RGR-containing peptide, a CGKRK-containing peptide, and a CREKA-containing peptide.

### Claim 6 (depends on 1)

The drug delivery system of claim 1, wherein the drug delivery system is represented by the following Formula 1:
In Formula 1, pSiNP is a porous silicon nanoparticle, and the R1 is an alkyl group having 1 to 8 carbon atoms.

### Claim 7 (depends on 4)

The drug delivery system of claim 4, wherein the drug delivery system is represented by the following Formula 2:
In Formula 2, pSiNP is a porous silicon nanoparticle,
the R1 is an alkyl group having 1 to 8 carbon atoms,
the THP is a tumor homing peptide,
the L is a linker, and X is 0 or 1.

### Claim 8

A pharmaceutical composition for treating cancer, the composition comprising a porous silicon nanoparticle and a drug delivery system comprising an isothiocyanate moiety conjugated to the surface of the porous silicon nanoparticle as an active ingredient.

### Claim 9

A method for manufacturing a drug delivery system, the method comprising:
preparing porous silicon nanoparticles; and
conjugating an isothiocyanate moiety to the surface of the porous silicon nanoparticle.

### Claim 10 (depends on 9)

The method of claim 9, wherein the method further comprises supporting a drug or prodrug on the porous silicon nanoparticles.

### Claim 11 (depends on 9)

The method of claim 9, wherein the method further comprises conjugating a tumor homing peptide to the surface of the porous silicon nanoparticles.