Cell penetrating peptide-mediated systemic siRNA delivery to the liver (2011)
Sequence: RRRRRRRR
| Experiment Id | EXP001405 |
|---|---|
| Paper | Cell penetrating peptide-mediated systemic siRNA delivery to the liver |
| Peptide | Octaarginine (R8) |
| Delivery Success Class | yes |
| In Vivo Flag | yes |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | |
| Endosomal Escape Evidence | yes |
| Peptide Concentration | Encoded in formulation (18 mol% STR-R8 of total lipids); injected as nanoparticles |
| Rna Concentration | 25–100 µg siRNA per mouse (single IV injection; measured at 24 h for knockdown) |
| 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_vivo |
| Model Type | in vivo |
| Cell Lines Or Primary Cells | |
| Animal Model | C57BL/6 mice (6–7 weeks old); liver knockdown after tail-vein injection |
| Administration Route | Intravenous (tail vein) |
| Output Type | In vivo liver SR-BI mRNA knockdown (qRT-PCR; 24 h post-injection) |
| Output Value | |
| Output Units | |
| Output Notes | Dose-dependent SR-BI silencing reported (≈45% at 25 µg; ≈75% at 100 µg). Minimal liver toxicity (GPT/GOT) and low innate immune response (IL-6/IFN-γ). |
| Toxicity Notes | GPT/GOT not significantly increased vs controls; IL-6 slightly elevated at 6 h (much lower than poly I:C), IFN-γ not detectable. |
| Curation Notes |