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 | EXP001716 |
|---|---|
| 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 | Micelleplexes prepared from 10 mg polymer films; working concentration for stability assay 100 µg/mL micelleplex; cellular assays used micelleplexes formed at charge ratio 30 with ~100 nM anti-miRNA. |
| Rna Concentration | Typically 100 nM anti-miRNA for confocal 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 | Reducible triblock copolymer PEG-PLA-SS-R15 (disulfide between PLA and R15) forming micelleplexes with anti-miRNA |
| Size Nm | 19.90 |
| Zeta Mv | 4.95 |
| 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 (~90% cells by flow cytometry at charge ratio 30). Enhanced intracellular dissociation (~90% dissociated by 24 h). Strong anti-miR-21 activity in U251 dual-luciferase reporter assay (higher firefly/Renilla vs nonreducible). |
| Output Units | |
| Output Notes | Cells incubated with micelleplexes in cerebrospinal fluid (CSF) for 4 h for activity assay; control anti-miRc showed no reporter increase. Confocal microscopy quantified dissociation using Mender’s coefficient and calculated dissociation efficiency εd. |
| Toxicity Notes | No significant toxicity reported under dual-luciferase assay exposure regimen (4 h in CSF + 48 h recovery). |
| Curation Notes |