Modulating Lipoprotein Transcellular Transport and Atherosclerotic Plaque Formation in ApoE^-/- Mice via Nanoformulated Lipid-Methotrexate Conjugates.

ABSTRACT: Macrophage inflammation and maturation into foam cells, following the engulfment of oxidized low-density lipoproteins (oxLDL), are major hallmarks in the onset and progression of atherosclerosis. Yet, chronic treatments with anti-inflammatory agents, such as methotrexate (MTX), failed to modulate disease progression, possibly for the limited drug bioavailability and plaque deposition. Here, MTX-lipid conjugates, based on 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (DSPE), were integrated in the structure of spherical polymeric nanoparticles (MTX-SPNs) or intercalated in the lipid bilayer of liposomes (MTX-LIP). Although, both nanoparticles were colloidally stable with an average diameter of ∼200 nm, MTX-LIP exhibited a higher encapsulation efficiency (>70%) and slower release ra

SUBMITTER: Di Francesco V 

PROVIDER: S-EPMC7453397 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature