The size distribution of QD-micelles formed entirely with PL-PEG (PS (0)) were 198.3 ± 3.7 nm (Figure 1, Additional file 1: Figure S3). Up to Fosbretabulin price 50 mol% occupancy of PEG, the results are consistent with prior reports demonstrating the linear relationship between the hydrodynamic diameter of nanoparticles and PEG density . However, with further decrease in PL-PEG, the size of PS micelles increased. The mean hydrodynamic diameter of PS (60) micelles was 133.6 ± 17.9
nm and that of PS (100) micelles with no PEG was 127.3 ± 23.3 nm. Transmission electron microscopy (TEM) was performed to further characterize the morphology of the PS (50) micelles. Negatively stained PS (50) micelles appear as small unilamellar vesicular structures
with a size of approximately 50 nm with about 2 to 3 QDs seen within each micelle (Additional file 1: Figure S2). With increasing PS, the surface charge of PS-QD micelles increased from -14.5 ± 7.5 mV for PS (50) micelles, -16.4 ± 6.9 mV for PS (60) micelles, to -32.5 ± 7.8 mV for PS (100) micelles (Figure 1). Another important consideration when preparing nanoparticles for in vivo use is their colloidal stability in serum. The aggregation GDC 0032 property of the micelles was studied by monitoring the change in their hydrodynamic diameter after 24 h of incubation with 10% (v/v) serum-containing media. The stability of PS-QD micelles decreases with increasing concentration of PS, PS (40) > PS (50) > PS (60) > PS (100) (Additional file 1: Figure selleck products S4). The results suggest that an amount
of 50 to 60 mol% PEG for PS-PL-PEG micelles with 6- to 8-nm hydrophobic Y-27632 2HCl QD core is optimal for generating uniformly small micelles, for further evaluation. In vitro cytotoxicity of various PS-QD micelle preparations was also evaluated in J774A.1 cells. Up to 50 nM, all preparations of PS-QD micelles were found to be non-toxic to macrophages when incubated for 24 h, as assessed by MTT cell viability assay (Additional file 1: Figure S7). Figure 1 Physico-chemical characterization of PS-QD micelles by dynamic light scattering. The mean hydrodynamic diameters of micelles with varying PL-PEG/PS mole ratio. PS (0, 40, 50, 60, 100) micelles were 198.3 ± 3.7, 104.6 ± 9.7, 40.9 ± 0.5, 133.6 ± 17.9, and 127.3 ± 23.3 nm, respectively. The zeta potential values were -14.5 ± 7.5mV for PS (50) micelles, -16.4 ± 6.9mV for PS (60) micelles, to -32.5 ± 7.8mV for PS (100) micelles, respectively. To demonstrate the ability of PS-QD micelles to target and subsequently phagocytosed by macrophages, J774A.1 cells were incubated with PS-QD micelles containing variable amount of PS (40, 50, 60, and 100 mol% PS). The extent of micelle uptake by macrophages was quantified by fluorescence-activated cell sorting (FACS). It was hypothesized that increasing PS mol% and decreasing PL-PEG packing density on micelles would determine the rate of internalization of PS-QD micelles by macrophages.