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EXP001884

Paper

Fine Tuning of Core–Shell Structure of Hyaluronic Acid/Cell-Penetrating Peptides/siRNA Nanoparticles for Enhanced Gene Delivery to Macrophages in Antiatherosclerotic Therapy (2018)

Peptide

Penetratin — NPs-1 (HA 8 kDa shell)

Sequence: RQIKIWFQNRRMKWKK

RNA

siRNA

All experiment fields

Experiment Id EXP001884
Paper Fine Tuning of Core–Shell Structure of Hyaluronic Acid/Cell-Penetrating Peptides/siRNA Nanoparticles
Peptide Penetratin — NPs-1 (HA 8 kDa shell)
Delivery Success Class yes
In Vivo Flag yes
Uptake Confirmed yes
Label Confidence high
In Vitro Functional Effect
Endosomal Escape Evidence
Peptide Concentration
Rna Concentration
Mixing Ratio CPP/siRNA N/P = 4:1 (complete complexation); HA coated by adsorption to produce NPs-1/NPs-2/NPs-3.
Formulation Format Core–shell nanoparticle (Penetratin/siRNA core; hyaluronic acid shell for NPs)
Formulation Components Core: penetratin-condensed LOX-1 siRNA (NCs). Shell: HA 8 kDa shell; HAase-responsive de-shielding in plaques/macrophage environment.
Size Nm 140.70
Zeta Mv 22.20
Model Scope in_vivo
Model Type in vivo
Cell Lines Or Primary Cells
Animal Model Male apoE-deficient mice on high-cholesterol diet (16 weeks induction) followed by 12-week treatment.
Administration Route Tail vein (i.v.) injection; 1.5 mg/kg siRNA, twice per week for 12 weeks (pharmacodynamic efficacy).
Output Type In vivo functional delivery: anti-atherosclerotic efficacy (lesion area, lipid, inflammation markers)
Output Value LOX-1 siRNA formulations reduced aortic root lesion area and lipid accumulation; NPs-3 showed the strongest reduction and decreased CD68+ macrophage content and MCP-1 vs controls.
Output Units
Output Notes HA-coated NCs using 8 kDa HA. In vivo ex vivo imaging (Cy5-siRNA 1 mg/kg) showed higher aorta plaque accumulation for HA-coated NPs (highest for NPs-3) vs free siRNA/NCs; therapeutic study shows best efficacy for NPs-3.
Toxicity Notes
Curation Notes