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EXP002541

Paper

A Multifunctional Lipid-Based Nanodevice for the Highly Specific Codelivery of Sorafenib and Midkine siRNA to Hepatic Cancer Cells (2019)

Peptide

STR-R8

Sequence: R8 (RRRRRRRR)

RNA

siRNA

All experiment fields

Experiment Id EXP002541
Paper A Multifunctional Lipid-Based Nanodevice for the Highly Specific Codelivery of Sorafenib and Midkine
Peptide STR-R8
Delivery Success Class no
In Vivo Flag no
Uptake Confirmed yes
Label Confidence high
In Vitro Functional Effect yes
Endosomal Escape Evidence
Peptide Concentration 10 mol% STR-R8 (surface)
Rna Concentration 400 nM (typical; also 200 nM when SOR=5 µM)
Mixing Ratio siRNA:drug molar ratio 1:25 (0.4 µM siRNA : 10 µM SOR); siRNA/lipid ~1:500; PEI N/P=0.5 core
Formulation Format Lipid nanoparticles (LNPs); siRNA/PEI core + lipid film hydration; sonication; ultrafiltration
Formulation Components YSK05/EPC/cholesterol/STR-R8 = 4:3:2:1 (molar ratio); siRNA complexed with PEI (N/P=0.5); SOR co-loaded
Size Nm 180.00
Zeta Mv 49.00
Model Scope in_vitro
Model Type in vitro
Cell Lines Or Primary Cells HepG2 (human HCC); Hepa 1-6 (mouse HCC); HeLa; FL83B (normal mouse hepatocytes)
Animal Model
Administration Route
Output Type MK mRNA knockdown EC50 (qRT-PCR) + cytotoxicity readouts
Output Value Optimized formulation reduced MK knockdown EC50 to ~30 nM in HepG2; nonselective uptake/cytotoxicity higher in FL83B vs HepG2 (uptake ~5.26×; viability FL83B ~8% vs HepG2 ~25% at SOR 10 µM + MK-siRNA 400 nM)
Output Units
Output Notes FACS + CLSM uptake; qRT-PCR MK knockdown; MTT viability. STR-R8 improves uptake and is linked to endosomal escape; YSK05 described as pH-sensitive with endosomal escape properties.
Toxicity Notes Nonselective: higher uptake and cytotoxicity in normal FL83B than HepG2; empty carrier toxicity reduced after optimization (empty LNP viability ~86%).
Curation Notes