Poly(β-amino ester)-co-polyethylene glycol (PEG-PBAE-PEG) polymers for gene and drug delivery
Inventors
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Assignees
MemberJohns Hopkins UniversityJohns Hopkins UniversityFounded in 1876, Johns Hopkins University is recognized as the first research university in the United States. It advances interdisciplinary education, high-impact research, and global outreach, supporting knowledge translation, technological innovation, and community partnerships. The university fosters academic excellence, innovation incubation, outreach, and inclusion across multiple campuses in Baltimore, integrating into the city's social, economic, and cultural life.
Founded in 1876, Johns Hopkins University is recognized as the first research university in the United States. It advances interdisciplinary education, high-impact research, and global outreach, supporting knowledge translation, technological innovation, and community partnerships. The university fosters academic excellence, innovation incubation, outreach, and inclusion across multiple campuses in Baltimore, integrating into the city's social, economic, and cultural life.
Publication Number
US-12643980-B2
Publication Date
2026-06-02
Expiration Date
Abstract
Polyethylene glycol (PEG)-b-poly(β-amino ester) (PBAE) co-polymers (PEG-PBAE) and blends of PEG-PBAEs and PBAEs and their use for delivering drugs, genes, and other pharmaceutical or therapeutic agents safely and effectively to different sites in the body and to different cells, such as cancer cells, are disclosed.
Core Innovation
The invention relates to polyethylene glycol (PEG)-b-poly(b2-amino ester) (PBAE) copolymers of Formula (I), including pharmaceutically acceptable salts thereof, wherein each n and n is independently an integer in specified ranges, R is a C2 to C8 substituted or unsubstituted linear or branched alkylene, and R is a C1 to C5 substituted or unsubstituted linear or branched alkylene. The copolymers are defined by these structural variables and by the selection of pharmaceutically acceptable salts.
The invention further includes particles comprising a blend of the PEG-b-PBAE copolymer of Formula (I) and a poly(b2-amino ester) (PBAE), optionally wherein the PBAE component is an unmodified poly(b2-amino ester) (PBAE). The particles can comprise a cargo, including a drug or a gene, and in particular can include DNA or siRNA as the cargo.
The invention also includes a method for preparing a PEG-b-PBAE copolymer of Formula (I) by synthesizing an acrylate-terminated poly(b2-amino ester) (PBAE) via Michael addition of a diacrylate monomer and a primary amine-containing monomer, and then reacting the acrylate-terminated PBAE with a functionalized PEG molecule to form the PEG-b-PBAE co-polymer. The method is described with variants in which the functionalized PEG molecule is PEG-SH and where a catalyst is used, including 1-(3-aminopropyl)-4-methyl-piperazine.
Claims Coverage
The independent claims cover four inventive areas: (i) the PEG-b-PBAE copolymer of Formula (I), (ii) a particle made from a blend including that PEG-b-PBAE copolymer and PBAE and optionally a cargo, (iii) a method of preparing the PEG-b-PBAE copolymer by Michael addition followed by coupling to a functionalized PEG, and (iv) a delivery method that uses the Formula (I) compound/composition to form particles, micelles, or polyplexes containing a therapeutic agent and administer or contact them with a target. A total of four independent claims are identified in the provided partial content.
PEG-b-PBAE copolymer of Formula (I)
A polyethylene glycol (PEG)-b-poly(b2-amino ester) (PBAE) co-polymer (PEG-PBAE) of Formula (I) with each n and n in specified integer ranges and with R as C2 to C8 alkylene and R as C1 to C5 alkylene, including pharmaceutically acceptable salts thereof.
Blended particle comprising PEG-PBAE of Formula (I) and PBAE
A particle comprising a blend of a PEG-b-PBAE co-polymer of Formula (I) as defined by the specified ranges for n and n and the specified definitions of R and R, including pharmaceutically acceptable salts thereof, and a poly(b2-amino ester) (PBAE).
Method for preparing PEG-b-PBAE of Formula (I)
A method for preparing a PEG-b-PBAE co-polymer of Formula (I) including synthesizing an acrylate-terminated poly(b2-amino ester) (PBAE) via Michael addition of a diacrylate monomer and a primary amine-containing monomer, and reacting the acrylate-terminated PBAE with a functionalized PEG molecule to form the PEG-b-PBAE co-polymer.
Delivery method using Formula (I) to form particles, micelles, or polyplexes
A method for delivering a therapeutic agent to a cell, specific cell line, tissue, or organism by associating the agent with a compound of Formula (I) (or a pharmaceutical composition thereof) to form particles, micelles, or polyplexes containing both, and then administering or contacting them with the target.
Across the independent claims, the coverage centers on PEG-b-PBAE copolymers of Formula (I) defined by structural ranges, on particles formed from blending that copolymer with PBAE and optionally carrying cargo, on preparing the copolymer by forming an acrylate-terminated PBAE via Michael addition and coupling to a functionalized PEG molecule, and on delivering therapeutic agents by forming particles, micelles, or polyplexes with the Formula (I) compound/composition and administering or contacting the target.
Stated Advantages
Documented Applications
No documented applications found
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