Reducible Micelleplexes are Stable Systems for Anti-miRNA Delivery in Cerebrospinal Fluid (2016)
R15 (polyarginine 15-mer) in PEG-PLA micelleplex
Sequence: Ac-CRRRRRRRRRRRRRRR-NH2 (CR15; poly(L-arginine)15 with N-terminal Cys, C-terminal amide)
anti-miRNA (single-stranded inhibitor)
| Experiment Id | EXP001717 |
|---|---|
| Paper | Reducible Micelleplexes are Stable Systems for Anti-miRNA Delivery in Cerebrospinal Fluid |
| Peptide | R15 (polyarginine 15-mer) in PEG-PLA micelleplex |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| Endosomal Escape Evidence | |
| Peptide Concentration | Comparable micelleplex formulation; charge ratio 30; anti-miRNA ~100 nM in cellular assays. |
| Rna Concentration | Typically 100 nM anti-miRNA for dissociation/association assays; activity assessed in dual-luciferase assay after 4 h exposure in CSF. |
| Mixing Ratio | Charge ratio (+/−) = 30 (arginine guanidinium : anti-miRNA phosphate). |
| Formulation Format | Polymeric micelleplex (PEG-PLA-(linker)-R15 micelles complexed with anti-miRNA) |
| Formulation Components | Nonreducible triblock copolymer PEG-PLA-R15 (stable linker) forming micelleplexes with anti-miRNA |
| Size Nm | 23.30 |
| Zeta Mv | 3.11 |
| Model Scope | in_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | U251 human glioblastoma cells |
| Animal Model | |
| Administration Route | |
| Output Type | in vitro functional anti-miRNA activity + uptake/association |
| Output Value | High cellular association (~89.7% cells by flow cytometry at charge ratio 30). Lower intracellular dissociation (~50% associated at 24 h) and lower anti-miR-21 activity vs reducible system in dual-luciferase assay. |
| Output Units | |
| Output Notes | Used as nonreducible control micelleplex; anti-miRc negative control showed no reporter increase. |
| Toxicity Notes | No significant toxicity reported under assay conditions (similar to reducible). |
| Curation Notes |