Cell penetrating peptide-mediated systemic siRNA delivery to the liver (2011)
Sequence: RRRRRRRR
| Experiment Id | EXP001404 |
|---|---|
| Paper | Cell penetrating peptide-mediated systemic siRNA delivery to the liver |
| Peptide | Octaarginine (R8) |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| Endosomal Escape Evidence | yes |
| Peptide Concentration | Encoded in formulation (18 mol% STR-R8 of total lipids); applied as nanoparticles |
| Rna Concentration | 25–100 nM (dose-response; 24 h incubation) in primary hepatocytes |
| Mixing Ratio | siRNA complexed with PEI at N/P=1.8; lipid composition STR-R8/DOPE/Cho-GALA = 18/77.5/4.5 (mol%) |
| Formulation Format | R8-modified lipid nanoparticles (lipid envelope over siRNA/PEI core; MEND-like) |
| Formulation Components | siRNA/PEI core (N/P 1.8) coated with lipids: STR-R8, DOPE, Cho-GALA (18:77.5:4.5 mol%) |
| Size Nm | 162.00 |
| Zeta Mv | 38.00 |
| Model Scope | in_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | Mouse primary hepatocytes (from ICR mice) |
| Animal Model | |
| Administration Route | |
| Output Type | SR-BI mRNA knockdown (qRT-PCR; normalized to beta-actin) |
| Output Value | |
| Output Units | |
| Output Notes | Significant SR-BI mRNA reduction observed at ≥25 nM SR-BI siRNA; luciferase siRNA control showed no significant knockdown. |
| Toxicity Notes | No detectable cytotoxicity reported previously for similar R8-MEND siRNA system; this study focuses on liver toxicity in vivo. |
| Curation Notes |