Pretreatment was with either α-mannosidase (green line) or with β

Pretreatment was with either α-mannosidase (green line) or with β … 3.7.

Possible Application of ESA as Sarcoma-Targeting Ligand Immobilized on Span 80 Vesicles To test whether ESA could be used as osteosarcoma-targeting ligand on a vesicular DDS, Span 80 vesicles with surface bound ESA were prepared, and the interaction of these vesicles Inhibitors,research,lifescience,medical with OST cells was compared with the interaction of vesicles that did not have surface bound ESA. Three types of Span 80 vesicles were prepared and tested (see Section 2.9): CV (control vesicles, no ESA), EV (vesicles with immobilized ESA), and EPV (PEGylated vesicles with immobilized ESA). All these vesicles contained encapsulated FITC as fluorescent probe. The vesicles were then mixed with OST cells and incubated, as mentioned in Section 2.9. Then, flow cytometric measurements were performed. As shown Inhibitors,research,lifescience,medical in Figure 7, the fluorescence intensity in both cases was higher than for cells treated with CV containing FITC. This means

that both types of vesicles with surface bound ESA, EPV, and EV bind to OST cells stronger than CV does. Furthermore, the fluorescence intensity of the cells treated with EPV containing FITC was found to be almost equal to the fluorescence intensity of the cells that were treated with EV containing FITC. Therefore, PEGylation Inhibitors,research,lifescience,medical did not hinder the binding of ESA to the sugar chains on the surface of the cells. Thus, Span 80 vesicles with immobilized ESA may be well suited for the development of a DDS for targeting osteosarcoma cells. Figure 7 Flow cytometric analysis of the interaction Inhibitors,research,lifescience,medical between OST cells and different types of Span 80 vesicles containing entrapped FITC: control vesicles (CV, black line), vesicles with immobilized ESA (EV, green line), and PEGylated vesicles with immobilized … 3.8. Cytotoxic Effects of EPV against OST Cells In a final investigation, the

anticancer activity of EPV against osteosarcoma cells was examined in vitro. The variation of the OST cells Selleck U0126 viability as a function of the concentration of added ESA (incubation time was 48 hours) is shown in Figure 8. EPV also clearly showed a strong Inhibitors,research,lifescience,medical anticancer activity against OST cells, inhibiting proliferation of OST cells completely in a culture medium that contained 2μg/mL ESA. This result is promising as it shows that PEGylated Span 80 vesicles with immobilized ESA are potentially useful as drug carrier system with endogenous antitumor activity against osteosarcoma. In the ESA concentration Methisazone range above about 2μg/mL complete death of the OST cells was observed, as shown in Figure 8. This demonstrates that EPV not only can function as targeting unit (see Section 3.7), but also efficiently inhibit OST cell growth. Figure 8 Cytotoxic effect of ESA in EPV on OST cells. The cell viability was evaluated with the propidium iodide staining. The OST cells were incubated during 48 hours at 37°C with EPV at the given concentration in D-MEM containing 10% FBS in a humidified … 4.

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