# US 2019/0314520 A1 · Carrier Nanoparticles And Related Compositions, Methods And Systems

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2019/0314520 A1
- Document ID: US20190314520A1
- Status: Published application
- Kind: A1
- Application number: 16/458,614
- Filed: 2019-07-01
- Published: 2019-10-17
- Earliest claimed: 2008-08-13
- Assignees: California Institute of Technology
- Applicants: California Institute Of Technology
- Inventors: Mark E. Davis; Akinleye Alabi
- Web page: https://patentgrep.com/patent/US20190314520A1

## CPC

- A61K 47/6935: {the polymer being obtained otherwise than by reactions involving carbon to carbon unsaturated bonds, e.g. polyesters, polyamides or polyglycerol}
- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 9/5146: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides}
- A61K 31/337: having four-membered rings, e.g. taxol
- A61K 31/4745: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48)
- A61K 31/704: attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)}
- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61K 47/545: {Heterocyclic compounds (A61K47/558 takes precedence)}
- A61K 47/549: {Sugars, nucleosides, nucleotides or nucleic acids}
- A61K 47/59: obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K 47/595: {Polyamides, e.g. nylon (polyamino acids A61K47/62)}
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61K 47/62: the modifying agent being a protein, peptide or polyamino acid
- A61K 47/644: {Transferrin, e.g. a lactoferrin or ovotransferrin}
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C08G 59/4078: {boron containing compounds}
- C08G 65/337: containing other elements (organic compounds containing halogens only as halides of a carboxyl group C08G65/332)
- C08G 69/40: Polyamides containing oxygen in the form of ether groups (C08G69/12, C08G69/32 take precedence)
- C08G 69/48: Polymers modified by chemical after-treatment
- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- C12N 2310/14: interfering nucleic acids [NA]
- C12N 2310/351: Conjugate
- 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
- C08G: MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

Carrier nanoparticles comprising a polymer containing a polyol coupled to a polymer containing a boronic acid and a linkage cleavable under reducing conditions, configured to present the polymer containing a boronic acid to an environment external to the nanoparticle and related compositions, methods and systems.

## Claims

### Claim 1

A nanoparticle comprising a polymer containing a polyol comprising one or more of at least one of the following structural units of Formula (I), (II), or (III):
wherein:
A comprises a polyol having 4 or 6 adjacent hydroxyl groups; and
B comprises a neutral, cationic, or anionic organic moiety having a chemical backbone comprising —CmH2m— linkages, where m≥1, and optionally one or more:
(a) polyglycol linkage, —(CH2—CH2—O)p—, in the chemical backbone, where p is from 20 to 200; and/or
(b) amidinium, quaternary ammonium, or imidazolium functional group in the chemical backbone; and/or
(c) sulfonate, nitrate, carboxylate, phosphonate, or primary or secondary amine bonded to the chemical backbone; and
wherein A and B are covalently linked by amide or ester linkages.

### Claim 2 (depends on 1)

The nanoparticle of claim 1, wherein A comprises glucose, fructose, mannitol, sucrose, galactose, sorbitol, xylose, galactose, or mucic acid.

### Claim 3 (depends on 1)

The nanoparticle of claim 1, wherein A comprises mucic acid.

### Claim 4 (depends on 1)

The nanoparticle of claim 1, wherein A further comprises a polyglycol linkage, —(CH2—CH2—O)n—, where n is from 1 to 20

### Claim 5 (depends on 1)

The nanoparticle of claim 1, wherein B comprises an amidinium, quaternary ammonium, or imidazolium functional group in the chemical backbone.

### Claim 6 (depends on 1)

The nanoparticle of claim 1, wherein B comprises a sulfonate, nitrate, carboxylate, phosphonate, or primary or secondary bonded to the chemical backbone.

### Claim 7 (depends on 1)

The nanoparticle of claim 1, wherein the polymer containing the polyol is derived from the coupling of a compound:
with a compound of:
wherein n, q, and p are independently 1-20.

### Claim 8 (depends on 1)

The nanoparticle of claim 1, wherein the polymer containing the polyol comprises a structural unit of:
wherein n is 1-20.

### Claim 9 (depends on 1)

The nanoparticle of claim 1, comprising a structural unit of:

### Claim 10 (depends on 1)

The nanoparticle of claim 1, comprising a structural unit of:

### Claim 11 (depends on 1)

The nanoparticle of claim 1, further comprising one or more targeting ligand molecules per nanoparticle, each one or more targeting ligand molecules bonded to the nanoparticle via a linker comprising at least one of an amide, a borate ester, carboxylate ester, or a disulfide linkage.

### Claim 12 (depends on 11)

The nanoparticle of claim 11, wherein the one or more targeting ligand molecule per nanoparticle comprises a ligand for a cellular receptor, a cellular receptor protein, a ligand for a cellular receptor, or cellular receptor protein.

### Claim 13 (depends on 11)

The nanoparticle of claim 11, wherein the one or more targeting ligand molecule per nanoparticle comprises a vitamin, a protein, a protein fragment, a monosaccharide, a peptide, a peptide aptamer, an oligopeptide, a polypeptide or fragment thereof, a polysaccharide, a polynucleotide, an antibody, or an antibody fragment.

### Claim 14 (depends on 11)

The polymer conjugate of claim 11, wherein the one or more targeting ligand molecule per nanoparticle comprises an antibody or antibody fragment against a surface cell receptor.

### Claim 15 (depends on 11)

The nanoparticle of claim 11, wherein the one or more targeting ligand molecule per nanoparticle comprises transferrin, folic acid, or galactose

### Claim 16 (depends on 1)

The nanoparticle of claim 1, further comprising at least one therapeutic agent incorporated therein or coupled thereto.

### Claim 17 (depends on 16)

The nanoparticle of claim 16, wherein the at least one therapeutic agent comprises a chemotherapeutic agent.

### Claim 18 (depends on 16)

The nanoparticle of claim 16, wherein the at least one therapeutic agent comprises an epothilone, a camptothecin-based drug, doxorubicin, taxol, or a nucleic acid, or a combination thereof

### Claim 19 (depends on 16)

The nanoparticle of claim 16, wherein the at least one therapeutic agent comprises camptothecin, an epothilone, a taxane or a combination thereof.

### Claim 20 (depends on 16)

The nanoparticle of claim 16, wherein at least one therapeutic agent comprises a plasmid, a genomic DNA, siRNA, shRNA, miRNA, antisense oligonucleotide, a chimeric nucleotide, an aptamer, or a combination thereof.

### Claim 21 (depends on 1)

The nanoparticle of claim 1, further comprising:
(a) at least one targeting ligand molecule per nanoparticle, wherein each targeting ligand molecule is bonded to the nanoparticle via a linkage comprising at least one of an amide, a borate ester, carboxylate ester, or a disulfide linkage, wherein the at least one targeting ligand molecule comprises a ligand for a cellular receptor, a cellular receptor protein, a ligand for a cellular receptor, or cellular receptor protein; and
(b) at least one therapeutic agent.

### Claim 22 (depends on 21)

The nanoparticle of claim 21, wherein:
(a) the polymer containing the polyol comprises a structural unit of:
wherein n is 1-20;
(b) the targeting ligand molecule is transferrin, and
(c) the therapeutic agent comprises camptothecin and an optional antibody.

### Claim 23 (depends on 1)

An aqueous solution comprising a plurality of nanoparticles of claim 1.

### Claim 24 (depends on 21)

An aqueous solution comprising a plurality of nanoparticles of claim 21.

### Claim 25 (depends on 21)

A method of treating a functional disorder in a human patient's body, the method comprising administering to the human patient a plurality of nanoparticles of claim 21.

### Claim 26 (depends on 25)

The method of claim 25, wherein the functional disorder is a mental disorder.

### Claim 27 (depends on 25)

The method of claim 25, wherein the functional disorder is a physical disorder.

### Claim 28 (depends on 25)

The method of claim 25, wherein the functional disorder is a cancer and the therapeutic agent is at least one chemotherapeutic agent.

### Claim 29 (depends on 25)

The method of claim 25, wherein:
(a) the functional disorder is a cancer,
(b) the nanoparticles comprise polymer containing the polyol comprising a structural unit of:
wherein n is 1-20;
(c) the targeting ligand molecule is transferrin, and
(d) the therapeutic agent comprises camptothecin and an optional antibody.