Figure 2.
UCH-L1 inhibitor LDN-57444 can be effectively loaded into polymeric micellar system based on amphiphilic polyoxazoline block copolymer. (A) Loading efficiency (LE) and loading capacity (LC) of LDN-POx micelles at LDN:POx w/w ratios of 2:10, 4:10, 6:10 and 8:10. LE of LDN-POx micelles remained close to 100% up to 6:10 LDN:POx ratio, resulting in LC of 35% w/w. (B) Particles size and particles size distribution of LDN-POx micelles at LDN:POx w/w ratios of 2:10, 4:10, 6:10 and 8:10. LDN-POx micelles formed small (50–70 nm), homogenous particles (polydispersity index (PDI) approx. 0.2) up to 6:10 LDN:POx ratio. (C) Stability of LDN-POx micelles stored at 4 °C overtime as determined by changes in drug loading, particles size and particles size distribution. LDN-POx micelles prepared at LDN:POx ratio of up to 6:10 were stable during incubation for up to 7 days.