Table 1.
Liposome characteristics describing the fluorescent label and mean/mode diameter (nm) of each prepared liposome batch, and if applicable, the VLA-4 coupling efficiency and loaded drug concentration
| Sr no | Liposome batch | Label | Diameter (nm) Mean ± SD | Diameter (nm) Mode ± SD | VLA-4 peptide coupling efficiency (%)Mean ± SD | Loaded drug concentration (µM) Mean ± SD |
|---|---|---|---|---|---|---|
| 1. | Untargeted (small) | DiD | 102.1±7.1 | 73.1±7.2 | – | – |
| 2. | Untargeted (intermediate) | DiD | 116.2±1.6 | 97.0±5.8 | – | – |
| 3. | Untargeted (large) | DiD | 179.1±30.1 | 68±10a 105±5 143±9 220±12 359±45 |
– | – |
| 4. | VLA-4 targeted (intermediate) | Rhod | 134.2±2.4 | 110.5±3.8 | 79.0±3.3 | – |
| 5. | Untargeted (intermediate) | Rhod | 135.0±0.7 | 107.9±7.3 | – | – |
| 6. | Untargeted/VLA-4 targeted (small) Empty/Bort loaded | DiD | 84.6±1.1 | 74.5±1.2 | 31.0 (n=1) | 15.9±14.2/21.9±3.6 |
| 7. | Untargeted/VLA-4 targeted (small) Dox loaded | DiD | 103.0±3.2 | 78.4±3.2 | 77.4 (n=1) | 376 (n=1)/247±190 |
Note:
a
Multiple peaks were observed in the large liposomes resulting in a heterogeneous size distribution.
Abbreviations: Bort, bortezomib; Dox, doxorubicin; Rhod, rhodamine; VLA-4, very late antigen 4.