TABLE 1.
Physical characterization of the DQ HME formulations (F1–F15)a
| Formulations | PS (nm) | PDI | Drug load (%) | % of drug in AS | Drug/formulation (g/g) | Medium and pH |
|---|---|---|---|---|---|---|
| F1 | 1011 | 0.202 | 10 | 93.10 | 18.62/180 | PBS (pH 7.4) |
| F2 | 1097 | 0.055 | 20 | 97.20 | 38.88/160 | PBS (pH 7.4) |
| F3 | 4385 | 0.220 | 10 | 97.70 | 19.54/180 | PBS (pH 7.4) |
| F4 | 2232 | 0.185 | 20 | 98.10 | 39.24/160 | PBS (pH 7.4) |
| F5 | 898 | 0.255 | 20 | 94.70 | 28.41/120 | PBS (pH 7.4) |
| F6 | 762 | 0.204 | 20 | 93.70 | 28.11/120 | PBS (pH 7.4) |
| F7 | 588 | 0.235 | 25 | 93.72 | 34.68/113 | PBS (pH 7.4) |
| F8 | 227 | 0.108 | 25 | 98.92 | 36.60/113 | PBS (pH 7.4) |
| F9 | 820 | 0.233 | 25 | 99.32 | 49.66/150 | PBS (pH 7.4) |
| F10 | 627 | 0.238 | 25 | 98.20 | 29.46/120 | HCl (pH 4.0) |
| F11 | 891 | 0.343 | 25 | 84.40 | 42.20/150 | HCl (pH 4.0) |
| F12 | 505 | 0.352 | 10 | 95.70 | 19.14/180 | Saline (≈pH 5.5) |
| F13 | 345 | 0.184 | 20 | 91.25 | 36.50/160 | Saline (≈pH 5.5) |
| F14 | 317 | 0.235 | 20 | 93.60 | 28.08/121 | Saline (≈pH 5.5) |
| F15 | 209 | 0.154 | 25 | 96.52 | 48.26/150 | Saline (≈pH 5.5) |
a
Formulations were suspended in the solutions indicated in the right and stirred at room temperature for at least 24 h for evaluation. Decoquinate (DQ) in AS measured by high-performance liquid chromatography and divided by drug load gave the drug percentage (%) present in AS. The ratio of drug/formulation components (excipients) represent how much added drug was fused with formulation particles through hot-melt extrusion (HME) process. AS, aqueous suspension; PDI, polydispersity index; PS, particle size.