Table 2.
Overview of various batches of bortezomib-encapsulated liposomes by passive and remote loading methods.
| Loading method | Entrapping agent | Particle size |
Bortezomib concentration µg/mL (%EE) |
||
|---|---|---|---|---|---|
| Mean ± SD | Mode ± SD | 10% DMSO | 20% DMSO | ||
| Passive loading into aqueous core | NA | 97 ± 0.8 | 85 ± 1.0 | 39 (3.9%) | 31 (3.1%) |
| Passive loading into bilayer | NA | 125 ± 3.9 | 112 ± 7.0 | 150 (15%) | |
| Remote loading | Sorbitol 10% | 109 ± 0.8 | 95 ± 0.7 | 17 (1.7%), 10 (1%) | |
| Sorbitol 20% | 99 ± 0.6 | 86 ± 1.2 | 59 (5.9%) | ||
| Sorbitol 30% | 122 ± 1.0 | 109 ± 1.2 | 8.6 (0.9%), 19 (2%) | ||
| Sorbitol 40% | 120 ± 0.9 | 109 ± 1.4 | 6.6 (0.7%) | ||
| PVA 6 K (1% w/v) | n.d. | 60 (6%) | |||
| PVA 6 K (5% w/v) | 125 ± 2.7 | 111 ± 0.7 | 147 (14.7%) | ||
| PVA 6 K (10% w/v) | 124.1 ± 3.0 (PDI = 0.04 ± 0.04)* |
20 (2%), 172 (17.2%) | |||
| PVA 6 K (0.2% w/v) | 113 ± 1.6 | 95 ± 2.2 | 124 (12.4%), 94 (9.4%) | ||
| PVA 6 K (0.7% w/v) | 112 ± 4.0 | 97 ± 5.0 | 653 (65.3%), 357 (35.7%), 334 (33.4%) | ||
| PVA 6 K (2% w/v) | 107 ± 1.9 | 95 ± 3.8 | 381 (38.1%), 559 (55.9%) | ||
| Loading to PVA coated liposomes | PVA 6 K (2%) | 94 ± 2.1 | 85 ± 4.8 | 326 (32.6%), 445 (44.5%) | |
NA = not applicable; n.d. = not done; %EE = percentage encapsulation efficiency; PDI = polydispersity index; PVA, poly(vinyl alcohol).
*
Measured by dynamic light scattering (DLS).