Table 1. Solid carrier screening for the solidification of SuSMEDDS.
| Silica-based adsorbents | Cellulose-based diluents | Saccharide-based diluents | |||||||
|---|---|---|---|---|---|---|---|---|---|
| Sylysia® 350 | Neusilin® US2 | Florite® PS-10 | HPC | Vivapur® 105 | L-HPC | Lactose | Starch® 1500 | Maltodextrin | |
| Composition (mg) | |||||||||
| SuSMEDDSa | 224.8 | 224.8 | 224.8 | 224.8 | 224.8 | 224.8 | 224.8 | 224.8 | 224.8 |
| Solid carrier | 112.3 | 110.1 | 89.9 | 606.6 | 404.4 | 381.9 | 1347.9 | 808.7 | 898.6 |
| Total | 337.1 | 334.9 | 314.7 | 831.4 | 629.2 | 606.7 | 1572.7 | 1033.5 | 1123.4 |
| Physical characteristicsb | |||||||||
| Droplet size (nm) | 147.7 ± 9.1 | 120.0 ± 7.1 | 146.4 ± 1.1 | 130.5 ± 4.4 | 151.9 ± 9.4 | 168.1 ± 8.2 | 151.5 ± 3.6 | 145.6 ± 2.2 | 121.2 ± 56.6 |
| PDI | 0.36 ± 0.05 | 0.41 ± 0.05 | 0.42 ± 0.11 | 0.57 ± 0.09 | 0.21 ± 0.03 | 0.47 ± 0.05 | 0.52 ± 0.55 | 0.49 ± 0.06 | 0.74 ± 0.07 |
| Drug content (%) | 93.7 ± 1.0 | 94.5 ± 2.5 | 94.1 ± 3.1 | 101.4 ± 6.6 | 98.6 ± 4.0 | 102.4 ± 2.6 | 99.6 ± 5.6 | 104.9 ± 3.4 | 98.2 ± 2.9 |
| CSR (g/mL) | 0.5 | 0.49 | 0.4 | 2.7 | 1.8 | 1.7 | 6 | 3.6 | 4 |
| DE (%)c | 40.6 ± 2.5 | 46.3 ± 1.7 | 46.5 ± 2.5 | 56.3 ± 1.6 | 66.3 ± 2.1 | 55.4 ± 0.5 | 48.1 ± 1.1 | 48.9 ± 2.1 | 50.4 ± 2.8 |
aSuSMEDDS composed of VST (80 mg), Capmul® MCM (13.2 mg), Tween® 80 (59.2 mg), Transcutol® P (59.2 mg), and Poloxamer 407 (13.2 mg) was formulated based on the earlier report [1]. bValues are presented as the mean ± SD (n = 3). cDissolution efficiency (DE) was calculated using the trapezoidal rule as follows: , where y is the percentage of dissolved product [42].
Abbreviations: SuSMEDDS, supersaturable self-microemulsifying drug delivery system; HPC, hydroxypropyl cellulose; L-HPC, low-substituted hydroxypropyl cellulose; PDI, polydispersity index; CSR, critical solidifying ratio.