	US 12,214,076 B2
	Drug delivery vehicles for atherosclerosis nanomedicine
Samuel I. Stupp, Chicago, IL (US); Melina R. Kibbe, Chapel Hill, NC (US); Mark R. Karver, Chicago, IL (US); Erica B. Peters, Durham, NC (US); Miranda So, Highland Park, NJ (US); Neel Anand Mansukhani, Chicago, IL (US); Mazen Albaghdadi, Brookline, MA (US); and Nick D. Tsihlis, Durham, NC (US)
Assigned to Northwestern University, Evanston, IL (US); and The University of North Carolina at Chapel Hill, Durham, NC (US)
Filed by Northwestern University, Evanston, IL (US); and The University of North Carolina at Chapel Hill, Durham, NC (US)
Filed on Feb. 17, 2020, as Appl. No. 16/792,474.
Claims priority of provisional application 62/807,092, filed on Feb. 18, 2019.
Prior Publication US 2020/0289416 A1, Sep. 17, 2020
Int. Cl. A61K 9/127 (2006.01); A61K 31/195 (2006.01); A61K 38/17 (2006.01); A61K 47/65 (2017.01); A61P 9/10 (2006.01); C07K 14/775 (2006.01)

CPC A61K 9/127 (2013.01) [A61K 31/195 (2013.01); A61K 38/1709 (2013.01); A61K 47/65 (2017.08); A61P 9/10 (2018.01); C07K 14/775 (2013.01)]

6 Claims

1. A peptide amphiphile comprising a hydrophobic tail, a structural peptide segment, a charged peptide segment, and a therapeutic agent for the treatment of atherosclerosis in a subject, wherein:

a) the hydrophobic tail comprises an 8-24 carbon alkyl chain (C_8-24),

b) the structural peptide segment comprises V₂A₂(SEQ ID NO: 8),

c) the charged peptide segment comprises EE, EEE, or EEEE (SEQ ID NO: 11),

d) the therapeutic agent is attached to the charged peptide segment by a cleavable linker selected from a ROS-sensitive proline linker, a glutathione-sensitive disulfide linker, and an MMP2/9-sensitive linker, and

e) the therapeutic agent comprises an annexin A1 protein derivative or an LXR agonist, wherein the annexin A1 protein derivative is Ac2-26 or wherein the LXR agonist is selected from hypocholamide, T0901317, GW3965, N,N-dimethyl-3beta-hydroxy-cholenamide (DMHCA), T0901317, 22(R)-hydroxycholesterol and 24(S)-hydroxycholesterol.