Table 1.
Formulations with 3% BRP-201 | Purified NP suspension | Lyophilized NPs | Yield | PVA | EE | LC | |||
---|---|---|---|---|---|---|---|---|---|
dH (nm) | PDI | dH (nm) | PDI | ζ (mV) | (%) | (%, w/w) | (%) | (%, w/w) | |
PLGA | 158 ± 5 | 0.11 ± 0.02 | 166 ± 12 | 0.07 ± 0.02 | − 24 ± 4 | 67 | 2 ± 0 | − | − |
PLGA[BRP-201] 3% | 174 ± 5 | 0.15 ± 0.02 | 182 ± 7 | 0.13 ± 0.02 | − 22 ± 3 | 71 | 1 ± 0 | 75 ± 11 | 2.2 ± 0.3 |
PLGA-Rho | 177 ± 11 | 0.13 ± 0.00 | 168 ± 11 | 0.09 ± 0.01 | − 25 ± 1 | 59 | 18 ± 1 | − | − |
PLGA-Rho[BRP-201] 3% | 201 ± 6 | 0.14 ± 0.01 | 191 ± 7 | 0.12 ± 0.03 | − 23 ± 2 | 51 | 15 ± 1 | 79 ± 5 | 2.3 ± 0.2 |
Ace-DEX | 140 ± 20 | 0.10 ± 0.05 | 172 ± 17 | 0.23 ± 0.08 | − 19 ± 6 | 41 | 3 ± 1 | − | − |
Ace-DEX[BRP-201] 3% | 154 ± 27 | 0.08 ± 0.02 | 128 ± 32 | 0.09 ± 0.03 | − 24 ± 6 | 39 | 1 ± 0 | 69 ± 16 | 2.0 ± 0.5 |
Ace-DEX-Rho | 185 ± 21 | 0.10 ± 0.02 | 391 ± 49 | 0.43 ± 0.05 | − 16 ± 1 | 58 | 10 ± 1 | − | − |
Ace-DEX-Rho[BRP-201] 3% | 214 ± 11 | 0.08 ± 0.01 | 182 ± 7 | 0.08 ± 0.01 | − 27 ± 1 | 56 | 6 ± 0 | 70 ± 1 | 2.1 ± 0.1 |
BRP-201 precipitates | 336 ± 79 | 0.23 ± 0.15 | 317 ± 44 | 0.18 ± 0.09 | − 23 ± 2 | − | − | − | − |
dH (Z-average), PDI and zeta-potential (ζ) measured by DLS and ELS, where n represents number of batches (PLGA and Ace-DEX n = 8; Rho-labeled NPs n = 3; BRP-201 precipitates n = 5); EE and LC determined by UV–VIS spectroscopy (n = 9)