Cholesterol-DP7-ACP-T7 (DAT) (dual-functional peptide on liposome)
Sequence: cholesterol-VQWRIRVAVIRK-ACP-HAIYPRH
siRNA (duplex, 21-mer with 3′ TT overhangs)
| Experiment Id | EXP002002 |
|---|---|
| Paper | A blood–brain barrier- and blood–brain tumor barrier-penetrating siRNA delivery system targeting gli |
| Peptide | Cholesterol-DP7-ACP-T7 (DAT) (dual-functional peptide on liposome) |
| Delivery Success Class | yes |
| In Vivo Flag | yes |
| Uptake Confirmed | no |
| Label Confidence | high |
| In Vitro Functional Effect | |
| Endosomal Escape Evidence | |
| Peptide Concentration | DAT-modified LNP prepared with DAT 250 μg/mL; DOTAP 2 mg/mL. |
| Rna Concentration | 1 mg/kg siRNA for biodistribution (cy5-siRNA) and for therapy (si slit2) via i.v. injection. |
| Mixing Ratio | DAT-LNP:siRNA mass ratio 6:1 for complexation. |
| Formulation Format | DAT-modified DOTAP:cholesterol liposome (DAT-LNP) electrostatically adsorbing siRNA |
| Formulation Components | DOTAP:cholesterol (1:1 molar; DOTAP 2 mg/mL) liposome + DAT peptide (250 μg/mL for modification; dialysis) + siRNA (complexed at 6:1 mass ratio LNP:siRNA). |
| Size Nm | 130.10 |
| Zeta Mv | |
| Model Scope | in_vivo |
| Model Type | in vivo |
| Cell Lines Or Primary Cells | |
| Animal Model | Orthotopic GL261 glioma model in female C57BL/6J mice (6–8 weeks); GL261 intracranial injection (1×10^5 cells/10 μL) day 0. |
| Administration Route | Intravenous (i.v.) dosing every 2 days from day 7 to day 25 post-implantation; 1 mg/kg siRNA per dose. |
| Output Type | In vivo functional delivery: tumor growth suppression and survival benefit in orthotopic glioma; histology (HE), proliferation/angiogenesis markers (Ki67, CD31), apoptosis (TUNEL), immune microenvironment activation. |
| Output Value | DAT-LNP/si slit2: smaller tumor volume; increased apoptosis (TUNEL); reduced Ki67 and CD31; improved survival (reported 100% survival at day 27 vs controls). |
| Output Units | |
| Output Notes | Also increased mature DCs, M1 macrophages, and cytotoxic CD8+ IFN-γ+ T cells; decreased Tregs in tumor microenvironment. |
| Toxicity Notes | No significant organ pathology (HE) and no significant liver/kidney blood chemistry changes vs PBS reported after i.v. dosing. |
| Curation Notes |