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 | EXP001024 |
|---|---|
| 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 | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| 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_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | A549, MCF-7, PANC-1 tumor cells (pH 6.5 vs 7.4) |
| Animal Model | |
| Administration Route | |
| Output Type | in vitro functional RNA effect (survivin knockdown by RT-qPCR) |
| Output Value | Highest/near-highest knockdown at pH 6.5 (e.g., mRNA down-regulation: 94.0% in MCF-7; 68.49% in A549; 66.6% in PANC-1). |
| Output Units | |
| Output Notes | pH-triggered charge reversal: zeta from −12 mV (pH 7.4) to +10.8 mV (pH 6.5) correlated with increased uptake at pH 6.5. |
| Toxicity Notes | MTT: formulations loaded with scrambled siRNA (siN.C.) showed >80% cell viability at pH 7.4 and pH 6.5. |
| Curation Notes |