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Articles

Synthesis and cellular characterization of various nano-assemblies of cell penetrating peptide-epirubicin-polyglutamate conjugates for the enhancement of antitumor activity

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Pages 1572-1585 | Received 09 Jul 2017, Accepted 09 Sep 2017, Published online: 21 Sep 2017

Figures & data

Figure 1. The schematic peptide synthesis of K3W4K3 (a), the schematic synthesis of FITC-labeled K3W4K3 (b) and the schematic synthesis of K3W4K3-EPR conjugate (c).

Figure 1. The schematic peptide synthesis of K3W4K3 (a), the schematic synthesis of FITC-labeled K3W4K3 (b) and the schematic synthesis of K3W4K3-EPR conjugate (c).

Table 1. Different cell penetrating peptide amphiphiles (CPPs) synthesized in the present study.

Table 2. The percentage of drug (EPR) loading for different peptide-EPR conjugates (CPPs-EPR).

Figure 2. MTT-based cytotoxicity of different CPPs (a), CPPs-E4 nanoparticles (b) and CPPs-E8 nanoparticles (c) at various concentrations (5, 10 and 25 µM) after 48 h incubation in MCF-7 cell line at 37 °C. Data represent Mean ± SD for six replicates.

Figure 2. MTT-based cytotoxicity of different CPPs (a), CPPs-E4 nanoparticles (b) and CPPs-E8 nanoparticles (c) at various concentrations (5, 10 and 25 µM) after 48 h incubation in MCF-7 cell line at 37 °C. Data represent Mean ± SD for six replicates.

Figure 3. Fluorescence microscopy images of MCF-7 cells incubated with FITC-labeled CPPs and their corresponding nanoparticles (CPPs-E8) at concentration of 10 (a) and 50 µM (b), respectively after 2 h incubation at 37 °C.

Figure 3. Fluorescence microscopy images of MCF-7 cells incubated with FITC-labeled CPPs and their corresponding nanoparticles (CPPs-E8) at concentration of 10 (a) and 50 µM (b), respectively after 2 h incubation at 37 °C.

Figure 4. Cellular uptake (%) of FITC-CPPs and the corresponding nanoparticles (FITC-CPPs-E8) at different concentration of 10, 25 and 50 µM, respectively after 2 h incubation in MCF-7 cell at 37 °C. Data represent Mean ± SD for three replicates. FITC-CPPs and FITC-CPPs and FITC-CPPs-E8 nanoparticles are presented by solid lines with the symbol of ▪ and dashed lines with the symbol of •, respectively.

Figure 4. Cellular uptake (%) of FITC-CPPs and the corresponding nanoparticles (FITC-CPPs-E8) at different concentration of 10, 25 and 50 µM, respectively after 2 h incubation in MCF-7 cell at 37 °C. Data represent Mean ± SD for three replicates. FITC-CPPs and FITC-CPPs and FITC-CPPs-E8 nanoparticles are presented by solid lines with the symbol of ▪ and dashed lines with the symbol of •, respectively.

Figure 5. Flow cytometry histograms of MCF-7 cells treated for 2 h with K3W4K3 (left) and K3W4K3-E8 (right) at various concentrations of 10 (a and d), 25 (b and e) and 50 (c and f) µM, respectively. First peak corresponds to untreated control cells.

Figure 5. Flow cytometry histograms of MCF-7 cells treated for 2 h with K3W4K3 (left) and K3W4K3-E8 (right) at various concentrations of 10 (a and d), 25 (b and e) and 50 (c and f) µM, respectively. First peak corresponds to untreated control cells.

Figure 6. MTT-based anti-proliferative activity of different CPPs-EPR (a), CPPs-E4-EPR (b) and CPPs-E8-EPR (c) in comparison with free drug (EPR) at various concentrations (1, 5, 10 and 25 µM) after 48 h incubation in MCF-7 cells at 37° C. Data represent Mean ± SD for six replicates.

Figure 6. MTT-based anti-proliferative activity of different CPPs-EPR (a), CPPs-E4-EPR (b) and CPPs-E8-EPR (c) in comparison with free drug (EPR) at various concentrations (1, 5, 10 and 25 µM) after 48 h incubation in MCF-7 cells at 37° C. Data represent Mean ± SD for six replicates.
Supplemental material

Samaneh_et_al._Supplementary_material.doc

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