Octaarginine (R8) in DSPE-PEG2000-R8 (post-inserted)
Sequence: Ac-Cys-βAla-(Arg)8-H (R8 peptide used to synthesize DSPE-PEG2000-R8)
| Experiment Id | EXP001694 |
|---|---|
| Paper | In Vitro Investigations of the Efficacy of Cyclodextrin-siRNA Complexes Modified with Lipid-PEG-Octa |
| Peptide | Octaarginine (R8) in DSPE-PEG2000-R8 (post-inserted) |
| Delivery Success Class | no |
| In Vivo Flag | yes |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| Endosomal Escape Evidence | |
| Peptide Concentration | 20 mol% DSPE-PEG2000-R8 relative to CD in complexes (post-inserted; incubated ~18 h at 38°C) |
| Rna Concentration | 50 nM (uptake + luciferase knockdown); 100 nM (GAPDH knockdown + toxicity) |
| Mixing Ratio | CD:siRNA mass ratio (MR) = 20; DSPE-PEG2000-R8 added at 20 mol% (relative to CD) |
| Formulation Format | Cyclodextrin/siRNA nanoparticles with post-inserted DSPE-PEG2000-R8 (R8-PEG-lipid surface layer) |
| Formulation Components | SC12CDclickpropylamine (amphiphilic cationic β-CD) + siRNA; DSPE-PEG2000-R8 micelles post-inserted |
| Size Nm | 113.70 |
| Zeta Mv | 38.90 |
| Model Scope | in_vivo |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | mHypoE N41 (mouse embryonic hypothalamic neuronal cell line) |
| Animal Model | |
| Administration Route | |
| Output Type | uptake + gene knockdown |
| Output Value | Uptake: 69.3±0.2% FAM+ cells (50 nM, 24 h). Luciferase: ~80% knockdown (50 nM). GAPDH: ~40% reduction (100 nM). |
| Output Units | |
| Output Notes | Complexes stable to salt (OptiMEM) vs unmodified CD complexes; serum (FBS) induced aggregation remained. Controls included NH2-PEG-DSPE (no R8) which did not significantly knock down luciferase. |
| Toxicity Notes | MTT: ~74% dehydrogenase activity for MR20 20% R8 (100 nM siRNA, 24 h); higher R8-PEG-DSPE caused more toxicity. |
| Curation Notes |