A one-pot modular assembly strategy for triple-play enhanced cytosolic siRNA delivery (2019)
Octreotide (N3-Oct) + Tat(49–57) CPP (N3-CPP) (with Glu charge-reversal module)
Sequence: Octreotide: DPhe-Cys-Phe-DTrp-Lys-Thr-Cys-Thr-ol (disulfide between Cys); Tat49–57: RKKRRQRRR
| Experiment Id | EXP001026 |
|---|---|
| Paper | A one-pot modular assembly strategy for triple-play enhanced cytosolic siRNA delivery |
| Peptide | Octreotide (N3-Oct) + Tat(49–57) CPP (N3-CPP) (with Glu charge-reversal module) |
| Delivery Success Class | yes |
| In Vivo Flag | yes |
| Uptake Confirmed | no |
| Label Confidence | high |
| In Vitro Functional Effect | |
| Endosomal Escape Evidence | |
| Peptide Concentration | |
| Rna Concentration | 100 nM (in vitro uptake and gene silencing assays); 1 mg/kg (Cy5-siRNA biodistribution in vivo); 1.2 mg/kg (cpusiRNA2 efficacy in vivo) |
| Mixing Ratio | N:P (lipid nitrogen:siRNA phosphate) = 3:1; module:ADIBO (mol:mol) varies per formulation |
| Formulation Format | liposome/siRNA complex with click-assembled azide modules (copper-free click) |
| Formulation Components | Cationic liposome (SPC:LG2C14:ADIBO-DSPE:Chol = 5:3:2:3, w/w/w/w) complexed with siRNA at N:P = 3:1; modules added via azide–ADIBO copper-free click |
| Size Nm | 7.40 |
| Zeta Mv | 7.40 |
| Model Scope | in_vivo |
| Model Type | in vivo |
| Cell Lines Or Primary Cells | |
| Animal Model | Orthotopic luci-MCF-7 breast tumor-bearing female BALB/c nude mice |
| Administration Route | Intravenous (tail vein) injection |
| Output Type | in vivo functional RNA delivery (tumor growth inhibition + survivin knockdown in tumors) |
| Output Value | Highest in vivo survivin silencing in tumors (RT-qPCR: 59.42% decrease in survivin mRNA) with significant tumor inhibition. |
| Output Units | |
| Output Notes | Cy5-siRNA imaging: superior tumor accumulation vs naked Cy5-siRNA and OC-CC (signal detectable up to 24 h). |
| Toxicity Notes | No significant differences vs saline in plasma ALP/ALT/AST/BUN; H&E of major organs showed no pathological changes. |
| Curation Notes |