Tat-Conjugated PAMAM Dendrimers as Delivery Agents for Antisense and siRNA Oligonucleotides (2005)
Sequence: RKKRRQRRRPPQGGC
| Experiment Id | EXP001673 |
|---|---|
| Paper | Tat-Conjugated PAMAM Dendrimers as Delivery Agents for Antisense and siRNA Oligonucleotides |
| Peptide | Tat-PAMAM G5 dendrimer (BPT) |
| Delivery Success Class | no |
| In Vivo Flag | no |
| Uptake Confirmed | yes |
| Label Confidence | high |
| In Vitro Functional Effect | yes |
| Endosomal Escape Evidence | no |
| Peptide Concentration | Dendrimer (BPT) 10–80 µg/mL used for complexation; functional assays emphasized 10–30 µg/mL (4 h transfection) |
| Rna Concentration | 100 nM oligonucleotide (antisense or siRNA) in Opti-MEM for complex formation and cell treatment |
| Mixing Ratio | Charge ratio (positive/negative) for BPT: antisense 8.7–69.7; siRNA 4.9–38.9 (varied with dendrimer dose 10–80 µg/mL) |
| Formulation Format | Electrostatic dendrimer/oligonucleotide complexes (20 min complexation in Opti-MEM) |
| Formulation Components | BODIPY-labeled PAMAM G5 dendrimer conjugated with Tat (BPT) + oligonucleotide (antisense or siRNA) |
| Size Nm | |
| Zeta Mv | |
| Model Scope | in_vitro |
| Model Type | in vitro |
| Cell Lines Or Primary Cells | NIH 3T3 MDR cells (mouse 3T3 stably expressing human MDR1/P-gp) |
| Animal Model | |
| Administration Route | |
| Output Type | MDR1 functional inhibition (P-glycoprotein expression) |
| Output Value | Partial inhibition of P-glycoprotein expression in viable NIH 3T3 MDR cells at nontoxic dendrimer levels (less effective than Lipofectamine 2000 at low doses). |
| Output Units | |
| Output Notes | Confocal imaging (24 h) showed antisense delivered but largely in intracellular vesicles; only a small fraction released from complexes. Tat conjugation did not improve functional delivery vs unconjugated PAMAM. |
| Toxicity Notes | Dose-dependent toxicity: BPT complexes ~50% cytotoxic at 30 µg/mL with 100 nM oligo; low toxicity (~10–20%) at 10 µg/mL. |
| Curation Notes |