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EXP002473

Paper

PEGylation of the GALA Peptide Enhances the Lung-Targeting Activity of Nanocarriers That Contain Encapsulated siRNA (2017)

Peptide

GALA/PEG2000-MENDssPalmE / anti-CD31 siRNA

Sequence: WEAALAEALAEALAEHLAEALAEALEALAA

RNA

siRNA

All experiment fields

Experiment Id EXP002473
Paper PEGylation of the GALA Peptide Enhances the Lung-Targeting Activity of Nanocarriers That Contain Enc
Peptide GALA/PEG2000-MENDssPalmE / anti-CD31 siRNA
Delivery Success Class yes
In Vivo Flag yes
Uptake Confirmed yes
Label Confidence high
In Vitro Functional Effect
Endosomal Escape Evidence yes
Peptide Concentration GALA/PEG2000 post-modification optimized at 2 mol% on MENDssPalmE
Rna Concentration 0.01–0.5 mg/kg for dose response; 0.5 mg/kg in optimization experiment
Mixing Ratio siRNA encapsulated in MENDssPalmE; GALA/PEG2000 surface ligand density varied 0.5–2 mol%
Formulation Format lipid nanoparticle / multifunctional envelope-type nano device (MEND)
Formulation Components ssPalmE and cholesterol 7:3; DMG-PEG2000 3 mol%; GALA/PEG2000 post-modification; anti-CD31 siRNA encapsulated
Size Nm 169.00
Zeta Mv -10.20
Model Scope in_vivo
Model Type in vivo lung endothelium gene silencing
Cell Lines Or Primary Cells
Animal Model C57BL/6N male mice; lung endothelial CD31 knockdown assay
Administration Route intravenous tail-vein injection
Output Type in vivo target-gene knockdown
Output Value CD31 mRNA knockdown in lung; ED50 approximately 0.21 mg/kg for 2 mol% GALA/PEG2000-MENDssPalmE; marginal nonspecific liver silencing at optimized condition
Output Units
Output Notes GALA/PEG2000-MENDssPalmE enhanced lung-endothelium CD31 silencing compared with unmodified MENDssPalmE; sequence-dependent knockdown confirmed by scramble control; no separate in vitro RNA-function row included because in vitro GALA/PEG liposome uptake assays used no siRNA cargo.
Toxicity Notes No body-weight changes reported for CD31 siRNA-encapsulating GALA/PEG2000-MENDssPalmE; authors note further translational safety study is needed
Curation Notes