Targeting the innate immune system to induce long-term tolerance and to resolve macrophage accumulation in atherosclerosis
a technology of atherosclerosis and innate immune system, which is applied in the direction of immunosuppressive agents, drug compositions, microcapsules, etc., can solve the problems of no alternative regimen seriously challenged the almost universal use of immunosuppressive agents, and all immunosuppressive agents have serious adverse effects, so as to prolong the survival of allografts and reduce the stimulatory capacity of dendritic cells
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[0190]Development of mTOR-HDL Nanoparticles
[0191]mTOR-HDL nanoparticles (see FIG. 1A) were synthesized by hydrating a lipid film, containing rapamycin and phospholipids, with APOA1 in PBS. Subsequently, and after vigorous homogenization, the sample was sonicated to generate mTOR-HDL nanoparticles with 62±11% rapamycin encapsulation efficiency and a mean hydrodynamic diameter of 12.7±4.4 nm, as determined by high performance liquid chromatography and dynamic light scattering, respectively. The size of the nanoparticles can vary, but will typically be from about 10 nm to about 250 nm.
[0192]As revealed by transmission electron microscopy (FIG. 4), the mTOR-HDL had the discoidal structure that is typical of HDL-based nanoparticles16. The biodistribution and cellular specificity of 1,1′-Dioctadecyl-3,3,3′,3′-Tetramethylindotricarbocyanine Iodide (DiR)-labeled mTOR-HDLs were evaluated in C57Bl / 6 wild type mice using ex vivo near infrared fluorescence (NIRF) imaging and flow cytometry. mTO...
example 2
Targeted CD40-TRAF6 Inhibition Resolves Macrophage Accumulation in Atherosclerosis
[0285]In atherosclerosis, macrophage accumulation is directly linked to destabilization and rupture of plaque, causing acute atherothrombotic events. Circulating monocytes enter the plaque and differentiate into macrophages, where they are activated by CD4+ T lymphocytes through CD40-CD40 ligand signaling. Here we show that interruption of this signaling pathway in monocytes / macrophages exerts rapid anti-inflammatory effects in an ApoE− / − mouse model of atherosclerosis. For this purpose we developed an infusible reconstituted high-density lipoprotein nanoparticle carrying a small molecule inhibitor of the interaction of CD40 and tumor necrosis factor receptor-associated factor 6. We show monocyte / macrophage specific targeting of our nanoimmunotherapy, which impairs their migratory capacity. Rapid reduction of plaque inflammation by this therapy represents a novel strategy in the treatment of atheroscle...
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