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EXP001953

Paper

A Dual-Ligand Liposomal System Composed of a Cell-Penetrating Peptide and a Mitochondrial RNA Aptamer Synergistically Facilitates Cellular Uptake and Mitochondrial Targeting (2016)

Peptide

MRP/R8-modified MITO-Porter (2.5 mol% Chol-MRP)

Sequence: RRRRRRRR

RNA

RNA aptamer (2′-O-methyl, cholesterol-conjugated) [ligand; not therapeutic payload]

All experiment fields

Experiment Id EXP001953
Paper A Dual-Ligand Liposomal System Composed of a Cell-Penetrating Peptide and a Mitochondrial RNA Aptame
Peptide MRP/R8-modified MITO-Porter (2.5 mol% Chol-MRP)
Delivery Success Class no
In Vivo Flag no
Uptake Confirmed yes
Label Confidence high
In Vitro Functional Effect no
Endosomal Escape Evidence
Peptide Concentration R8 at 10 mol% of total lipids (surface attachment after liposome formation).
Rna Concentration Chol-RNA aptamer at 2.5 mol% of total lipids (dual-ligand variants); NBD-DOPE used as tracer.
Mixing Ratio DOPE/sphingomyelin/NBD-DOPE (9:2:0.1) with ± 2.5 mol% Chol-aptamer; then add stearylated R8 to 10 mol% total lipid.
Formulation Format Liposome (MITO-Porter) with peptide + RNA aptamer dual-ligand surface
Formulation Components DOPE/sphingomyelin/NBD-DOPE (9:2:0.1 molar). R8 device ± Chol-RNA aptamer (RP/MRP/D-arm).
Size Nm 123.00
Zeta Mv 31.00
Model Scope in_vitro
Model Type in vitro
Cell Lines Or Primary Cells HeLa (human cervix carcinoma) cells
Animal Model
Administration Route
Output Type Uptake + mitochondrial targeting (flow cytometry MFI; confocal colocalization with mitochondria)
Output Value Dual-ligand (aptamer/R8) increases cellular uptake vs R8-only and improves mitochondrial targeting/occupancy; RP/R8 at 2.5 mol% reported as optimal among tested aptamers.
Output Units
Output Notes Readouts: flow cytometry of NBD-labeled liposomes after 3 h; CLSM colocalization with Mitofluor-stained mitochondria; mechanistic inhibitor studies (sucrose/amiloride; FCCP/oligomycin) probe uptake/targeting pathways.
Toxicity Notes
Curation Notes