Table 2. Summary of Experimental Conditions Used to Modulate Particle Size and Results Obtained.
| drug | experimental conditions used to generate particlesa | results |
|||
|---|---|---|---|---|---|
| Z-average (nm) | diffusion coefficient Dp (×10–8 cm2/s) | permeability (×10–6 cm/s, free drug, Pappf) | permeability (×10–6 cm/s, particles, Pappp) | ||
| ATZ | drug stock solution 5 mg/mL, 1000 rpm, 37 °C | 193 ± 4 | 3.43 ± 0.07 | 56.0 ± 2.0 | 47.7 ± 2.8 |
| drug stock solution 20 mg/mL, 1000 rpm, 37 °C | 460 ± 23 | 1.44 ± 0.07 | 51.7 ± 8.1 | 22.9 ± 1.3 | |
| LPV | drug stock solution 5 mg/mL, 1000 rpm, 25 °C | 254 ± 3 | 1.94 ± 0.00 | 25.1 ± 3.6 | 7.9 ± 0.2 |
| drug stock solution 12 mg/mL, 300 rpm, 25 °C | 454 ± 10 | 1.09 ± 0.00 | 27.9 ± 2.2 | 2.1 ± 0.1 | |
| drug stock solution 20 mg/mL, 300 rpm, 25 °C | 839 ± 15 | 0.59 ± 0.01 | 19.6 ± 0.1 | 1.6 ± 0.1 | |
a
At typical experimental conditions, where mixing is moderate and stabilizers are in excess (particle size being independent of stabilizer concentration), the final particle size depends mainly on the mixing time and coalescence time, with the latter determined by the initial solute mass concentration.61