**Appendix A**

**Figure A1.** Experimental determination of siRNA binding to self-assembling dendrons **1** (gray), **2** (light green), **3** (purple), **4** (red), **5** (black), and **6** (yellow) by EB assay. Non-self-assembling dendrons **7** (cyan) and **8** (orange) were used as negative controls. Adapted from [7] with the permission of John Wiley and Sons, 2016.

**Figure A2.** Pathology of major organs from treated mice (HES staining). Columns (from left to right): control, siRNA, **AD**, **AD**/siRNA. Rows (from to bottom): heart, kidney, liver, lung, spleen. Adapted from [6] with the permission of John Wiley and Sons, 2014.

**Figure A3.** Confocal microscopy images of the successful endosomal escape of the siRNA/**AD**/ E16G6RGDK nanoparticles in PC-3 cells after incubation times 0 (control), 0.5, 1, and 2 h Red channel images show the cy5-labeled siRNA/AD/E16G6RGDK nanoparticles, the green channel images reveal the Lyso Tracker red-marked endosomes, and the blue channel images show the cell nuclei stained with Hoechst 33342. In all these experiments, the siRNA/**AD**/E16G6RGDK nanoassemblies were prepared using 50 nM siRNA, siRNA/**AD** N/P = 10, and **AD**/E16G6RGDK molar ratio = 5. Adapted from [8] with the permission of the American Chemical Society, 2018.

**Figure A4.** *Cont*.

**Figure A4.** (**a**) Toxicity assessment using the MTT assay in prostate cancer PC-3 cells (solid bars) and in human embryonic kidney (HEK293) cells (patterned bars) of the **AD** micelles alone, **AD** in complex with a non-silencing siRNA (nssiRNA/**AD**) and the targeting peptide-decorated **AD** in complex with a non-silencing siRNA (nssiRNA/**AD**/E16G6RGDK). (**b**) Toxicity assessment using the LDH assay in prostate cancer PC-3 cells (solid bars) and in human embryonic kidney (HEK293) cells (patterned bars) of the **AD** micelles alone, **AD** in complex with a non-silencing siRNA (nssiRNA/**AD**) and the targeting peptide-decorated **AD** in complex with a non-silencing siRNA (nssiRNA/**AD**/E16G6RGDK). (**c**) Hemolysis effect measured via UV absorption at 540 nm for the **AD** micelles alone, **AD** in complex with a non-silencing siRNA (nssiRNA/**AD**) and the targeting peptide-decorated **AD** in complex with a non-silencing siRNA (nssiRNA/**AD**/E16G6RGDK) at different **AD** concentrations (corresponding to nssiRNA concentrations of 10, 20, 50, 100, and 200 nM, respectively). In all these experiments, the siRNA/**AD**/E16G6RGDK nanoassemblies were prepared using 50 nM siRNA, siRNA/**AD** N/P = 10, and **AD**/E16G6RGDK molar ratio = 5. Adapted from [8] with the permission of the American Chemical Society, 2018.

#### **References**


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