Amphiphilic Dendron-Coils, Micelles Thereof and Uses

Patent metadata

Field	Value
Publication number	US-2016331685-A1
Application number	US-201514968867-A
Country	US
Kind code	A1
Filing date	Dec 14, 2015
Priority date	Feb 23, 2011
Publication date	Nov 17, 2016
Grant date	—

Abstract

The invention generally relates to the fields of drug delivery and cell capture. In particular, the invention relates to amphiphilic dendron-coils, micelles thereof and their use for drug delivery vehicles and/or cell capture.

First claim

1 . A micelle comprising amphiphilic dendron-coils, wherein each amphiphilic dendron-coil comprises a non-peptidyl, hydrophobic core-forming block, a polyester dendron and a poly(ethylene) glycol (PEG) moiety.

2 . The micelle of claim 1 wherein the the non-peptidyl, hydrophobic core-forming block comprises polycaprolactone (PCL), poly(lactic acid) (PLA), poly(glycolic acid) (PGA) or poly(lactic-co-glycolic acid) (PLGA); wherein the polyester dendron is a generation 3 to generation 5 polyester dendron with either an acetylene or carboxylate core; and wherein the PEG moiety is a methoxy PEG (mPEG) moiety, amine-terminated PEG (PEG-NH 2 ) moiety, acetylated PEG (PEG-Ac) moiety, carboxylated PEG (PEG-COOH) moiety, thiol-terminated PEG (PEG-SH) moiety, N-hydroxysuccinimide-actived PEG (PEG-NHS) moiety, NH 2 -PEG-NH 2 moiety or NH 2 -PEG-COOH moiety.

3 - 8 . (canceled)

9 . The micelle of claim 1 or wherein the non-peptidyl, hydrophobic core-forming block has a molecular weight from about 0.5 kDa to about 20 kDa.

10 - 18 . (canceled)

19 . The micelle of claim 1 wherein the polyester dendron is a generation 3 (G3) dendron.

20 . The micelle of claim 1 wherein the polyester dendron is a generation 4 (G4) dendron.

21 . The micelle of claim 1 wherein the polyester dendron is a generation 5 (G5) dendron.

22 . The micelle of claim 19 wherein the polyester dendron is a generation 3 polyester-8-hydroxyl-1-acetylene bis-MPA dendron.

23 . The micelle of claim 1 wherein the PEG moiety is a methoxy PEG (mPEG) moiety, amine-terminated PEG (PEG-NH 2 ) moiety, acetylated PEG (PEG-Ac) moiety, carboxylated PEG (PEG-COOH) moiety, thiol-terminated PEG (PEG-SH) moiety, N-hydroxysuccinimide-actived PEG (PEG-NHS) moiety, NH 2 -PEG-NH 2 moiety or NH 2 -PEG-COOH moiety.

22 - 26 . (canceled)

27 . The micelle of claim 23 wherein the PEG moiety has a molecular weight from about 0.2 kDa to about 5 kDa.

28 - 31 . (canceled)

32 . The micelle of claim 1 further comprising one or more ligands conjugated to one or more PEG moieties.

33 . (canceled)

34 . The micelle of claim 1 further comprising a drug.

35 . The micelle of claim 34 wherein the drug is a cancer drug.

36 - 37 . (canceled)

38 . A composition comprising a micelle comprising amphiphilic dendron-coils, wherein each amphiphilic dendron-coil comprises a non-peptidyl, hydrophobic core-forming block, a polyester dendron and a poly(ethylene) glycol (PEG) moiety.

39 - 74 . (canceled)

75 . A method of delivering a drug to a patient comprising administering a composition comprising a micelle and a pharmaceutically acceptable carrier,
wherein the micelle comprises amphiphilic dendron-coils and encapsulates the drug, and wherein each amphiphilic dendron-coil comprises a non-peptidyl, hydrophobic core-forming block, a polyester dendron and a poly(ethylene) glycol (PEG) moiety.

76 - 111 . (canceled)

112 . A method of capturing a cell from a sample comprising the steps of:
exposing the sample to an immobilized amphiphilic dendron-coil comprising a non-peptidyl, hydrophobic core-forming block, a polyester dendron and a poly(ethylene) glycol (PEG) moiety with a ligand conjugated to the PEG, wherein the ligand binds to the cell; and capturing the cell by binding of the ligand to the cell.

113 - 145 . (canceled)

146 . An amphiphilic dendron-coil comprising a non-peptidyl, hydrophobic core-forming block, a polyester dendron and a poly(ethylene) glycol (PEG) moiety.

147 - 176 . (canceled)

177 . The amphiphilic dendron-coil of claim 146 further comprising a ligand conjugated to the PEG moiety.

178 . (canceled)

Assignees

• Univ Illinois

Inventors

• Hong Seungpyo
• Bae Jin Woo

Classifications

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61K47/34

  Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) · CPC title

• C08G83/003

  Dendrimers · CPC title

• A61K31/405

  Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin · CPC title

• A61K9/1075 Primary

  Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence) · CPC title