Development of a peptide-siRNA nanocomplex targeting NF-κB for efficient cartilage delivery (2019)
Sequence: VLTTGLPALISWIRRRHRRHC
| Experiment Id | EXP001699 |
|---|---|
| Paper | Development of a peptide-siRNA nanocomplex targeting NF-κB for efficient cartilage delivery |
| Peptide | p5RHH |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| Endosomal Escape Evidence | |
| Peptide Concentration | For cell culture: 20 mM stock diluted 1:400 (~50 µM peptide) then mixed with siRNA; for explants: mixed to peptide:siRNA 1:10 (HBSS) |
| Rna Concentration | 50 nM siRNA (cell culture); 500 nM siRNA (cartilage explants) |
| Mixing Ratio | Peptide:siRNA 100:1 (cell culture); 1:10 (explant formulation in HBSS) |
| Formulation Format | Self-assembling peptide/siRNA nanocomplex (NP) |
| Formulation Components | p5RHH peptide + p65 siRNA smart pool (Dharmacon); self-assembled NP |
| Size Nm | 55.00 |
| Zeta Mv | 12.00 |
| Model Scope | in_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | HUVECs; human primary chondrocytes; human articular cartilage explants (IL-1β-stimulated OA cartilage) |
| Animal Model | |
| Administration Route | |
| Output Type | in vitro functional knockdown / pathway suppression |
| Output Value | Marked suppression of p65 expression in HUVECs (WB) and suppression of IL-1β-induced phospho-p65 activation in human cartilage explants persisting up to ~3 weeks after 48 h exposure. |
| Output Units | |
| Output Notes | NP prepared with peptide:siRNA ratio 100:1 for cell culture (50 nM siRNA final); for explants, peptide:siRNA ratio 1:10 in HBSS (500 nM siRNA final) incubated 10 min on ice; deep penetration of siRNA signal into cartilage up to ≥700 µm reported. |
| Toxicity Notes | Cartilage surface viability unaffected by NP exposure (TUNEL, Fig. S1). |
| Curation Notes |