Table 4.
Examples of active pharmaceutical ingredients with improved solubility in PMeOx-b-PBuOx-b-PMeOx micelles ranked by LE and LC. (Modified from Ref.[116]. Reprinted with permission from AAAS).
| Compound | Aqueous solubility (mg/mL)a | logPa | Solubility in POx micelle (10 mg/mL POx) | Fold increased | LE % (mean) | LC % (mean) |
|---|---|---|---|---|---|---|
| ABT-263 | 0.000212 | 7.77 | 8.00 | 37736 | 100.0 | 44.4 |
| Podophyllotoxin | 0.114 | 1.5 | 7.62 | 67 | 95.2 | 43.2 |
| Etoposide | 0.1b | 0.60c | 7.34 | 73 | 91.8 | 42.3 |
| Simvastatin | 0.0122 | 4.68c | 6.98 | 572 | 87.2 | 41.1 |
| Efavirenz | 0.00855 | 4.6c | 6.90 | 807 | 86.2 | 40.8 |
| Cisplatin prodrug (C6) | insoluble | - | 6.78 | - | 84.8 | 40.4 |
| VE-822 | 0.0401 | 3.1 | 6.42 | 160 | 80.2 | 26.7 |
| Paclitaxel | 0.00556 | 3c | 5.05 | 908 | 63.1 | 30.4a |
| AZD5363 | insoluble | 1.31 | 4.98 | - | 62.3 | 33.3 |
| Cisplatin prodrug (C4) | insoluble | - | 4.68 | - | 58.5 | 31.9 |
| Teniposide | 0.0598 | 1.24c | 4.58 | 77 | 57.2 | 31.4 |
| Cisplatin prodrug (C10) | insoluble | - | 4.30 | - | 53.7 | 23.9 |
| AZD8055 | 0.241 | 2.87 | 4.06 | 17 | 50.8 | 28.9 |
| Docetaxel | 0.0127 | 2.4 | 3.71 | 292 | 46.4 | 19.0 |
| Rutin | 0.125 | 0.15 | 3.61 | 29 | 45.1 | 26.5 |
a
Data obtained from drugbank (https://www.drugbank.ca/) and predicted by either ALOGPS (http://www.vcclab.org/lab/alogps/) or ChemAxon (https://chemaxon.com/) when available, in other cases we refer to compounds “insoluble” if their solubility is less than 0.1 mg/ml.
b
US patent (US4772589A).
c
Experimental data obtained from drugbank (https://www.drugbank.ca/), The experimental value is from [22] and is different from that listed in [116], which was a mean of several values obtained for different conditions of micelle preparation.