# US 10,246,560 B2 · PLGA-modified polyethylenimine self-assembly nanotechnology for nucleic acid and drug delivery

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- Number: US 10,246,560 B2
- Document ID: US10246560B2
- Status: Granted
- Kind: B2
- Application number: 14/911,399
- Filed: 2014-08-13
- Published: 2016-06-30
- Granted: 2019-04-02
- Earliest claimed: 2013-08-13
- Assignees: Baylor College of Medicine
- Applicants: Baylor College of Medicine
- Inventors: Jian-Ming Lu; Qizhi Yao; Changyi Chen
- Web page: https://patentgrep.com/patent/US10246560B2

## CPC

- C08G 81/00: Macromolecular compounds obtained by interreacting polymers in the absence of monomers, e.g. block polymers (involving only carbon-to-carbon unsaturated bond reactions C08F299/00 {; polyester-amides C08G69/44; polyester-imides C08G73/16; polyamides-imides C08G73/14; block- or graft polymers containing polysiloxane sequences C08G77/42})
- A61K 47/59: obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K 47/593: {Polyesters, e.g. PLGA or polylactide-co-glycolide}
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61K 47/6929: {the form being a nanoparticle, e.g. an immuno-nanoparticle}
- A61K 47/6935: {the polymer being obtained otherwise than by reactions involving carbon to carbon unsaturated bonds, e.g. polyesters, polyamides or polyglycerol}
- A61K 47/6937: {the polymer being PLGA, PLA or polyglycolic acid}
- A61K 48/0041: {the non-active part being polymeric}
- A61K 48/005: {characterised by an aspect of the 'active' part of the composition delivered, i.e. the nucleic acid delivered}
- A61P 35/00: Antineoplastic agents
- C08G 63/6852: {derived from hydroxy carboxylic acids}
- C08G 63/912: {derived from hydroxycarboxylic acids}
- C08G 73/0206: {Polyalkylene(poly)amines}
- C08G 81/027: {containing polyester or polycarbonate sequences}
- C12N 15/88: using microencapsulation, e.g. using {amphiphile} liposome vesicle
- C12N 2310/14: interfering nucleic acids [NA]
- C12N 2310/141: MicroRNAs, miRNAs
- C12N 2320/32: Special delivery means, e.g. tissue-specific
- C08G: MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

Embodiments of the invention concern copolymers and nanoparticles for use as delivery agents for one or more agents for therapy for a medical condition of humans and animals. Some of embodiments of the invention provide new reagents for biomedical research in cell culture, animal models and plants, for example. The copolymers comprise PLGA and PEI and, in some embodiments, also comprise 1-(3-aminopropyl)-4-methylpiperazine (APMP), Fc binding peptide and/or antibody. In certain embodiments, APMP-PLGA-PEI, Fc binding peptide/antibody-PLGA-PEI or Fc binding peptide/antibody-AP-MP-PLGA-PEI nanoparticles comprising one or more therapeutic agents are delivered to an individual in need thereof or used for biomedical research in cell cultures, animal models and plants.

## Claims

### Claim 1

A composition comprising a copolymer consisting of lactide-co-glycolide and PEI, wherein single lactide-co-glycolide units are each conjugated to primary amines of PEI through an amide linkage, wherein the w/w ratio of LGA to PEI is 0.5:1 to 5:1,
wherein the composition further comprises at least one therapeutic and/or diagnostic agent and wherein the composition is in the form of a nanoparticle.

### Claim 2

A copolymer composition comprising lactide-co-glycolide and PEI, wherein single lactide-co-glycolide units are each conjugated to primary amines of PEI through an amide linkage, and wherein the primary amine concentration is about 40% to about 55%.

### Claim 3 (depends on 2)

The composition of claim 2, wherein the primary amine concentration is about 45% to about 55%, about 45% to about 52%, or about 46% to about 52%.

### Claim 4 (depends on 1)

The composition of claim 1, wherein when the ratio of LGA to PEI is 0.5:1 w/w, and a nanoparticle loaded with at least one therapeutic and/or diagnostic agent has an effective diameter between 100 and 130 nm.