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EXP000516

Paper

Dual stimulus of hyperthermia and intracellular redox environment triggered release of siRNA for tumor-specific therapy (2016)

Peptide

NGR motif peptide + CPP (penetratin-derived)

Sequence: CYGGRGNG ; CKRRMKWKK

RNA

siRNA

All experiment fields

Experiment Id EXP000516
Paper Dual stimulus of hyperthermia and intracellular redox environment triggered release of siRNA for tum
Peptide NGR motif peptide + CPP (penetratin-derived)
Delivery Success Class yes
In Vivo Flag yes
Uptake Confirmed no
Label Confidence high
In Vitro Functional Effect
Endosomal Escape Evidence
Peptide Concentration
Rna Concentration Dose: 1.2 mg/kg siRNA (as Cy3-siRNA-CPPs formulations) for imaging and therapy studies
Mixing Ratio
Formulation Format Thermosensitive liposome (TSL) with NGR targeting; encapsulated siRNA-CPP conjugate; heat-triggered release
Formulation Components DPPC:MSPC:DSPE-PEG2000-NGR (87:3:10, w/w); encapsulated siRNA-CPP conjugate; hyperthermia 42°C 30 min to trigger release/activate CPP; intracellular GSH reduces disulfide
Size Nm 90.23
Zeta Mv -18.98
Model Scope in_vivo
Model Type in vivo
Cell Lines Or Primary Cells
Animal Model Female BALB/c nude mice; HT-1080 xenograft tumor model
Administration Route IV (tail vein); local hyperthermia 42°C for 30 min after each injection
Output Type Tumor growth inhibition; in vivo c-myc knockdown (qRT-PCR/western); biodistribution imaging; TUNEL apoptosis
Output Value Superior tumor accumulation, c-myc silencing, delayed tumor progression with hyperthermia
Output Units
Output Notes Compared against free siRNA-CPPs (under hyperthermia) and NGR-TSL without hyperthermia; NGR-TSL + hyperthermia showed strongest antitumor efficacy and gene silencing.
Toxicity Notes No pronounced body weight loss reported for liposomal groups; free siRNA-CPPs caused body weight loss (off-target toxicity).
Curation Notes