Table 3.
Drug loading of traditional FDA-approved micro/nano-DDS.
| Brand Name | Size | API | Carrier Excipient | Drug Loading (% w/w)† |
|---|---|---|---|---|
| Optison™ Microsphere |
3–4.5 μm | C3F8 (0.22 mg) | Human Albumin (10 mg) | 2.1% |
| Definity® Lipid Microsphere |
1–3.3 μm | C3F8 (6.52 mg/mL) | DPPA (0.045 mg/mL) DPPC (0.401 mg/mL) DPPE-mPEG5k (0.304 mg/mL) Propylene glycol (103.5 mg/mL) Glycerin (126.2 mg/mL) |
2.83% |
| Marqibo® Liposome |
100–140 nm |
Vincristine sulfate (5 mg) | Sphingomyelin (73.5 mg) Chol (29.5 mg) Trapping Agent: Citric Acid (33.6 mg/mL) Sodium Citrate (35.4 mg/mL) |
2.9% |
| Diprivan® Emulsion |
<200 nm | Propofol (10 mg/mL) | Soybean Oil (100 mg/mL) Glycerol (22.5 mg/mL) Egg Lecithin (12 mg/mL) |
7.43% |
| Onpattro® Lipid Complex | N/A | Patisiran siRNA (2 mg/mL) | Chol (6.2 mg/mL) DLin-MC3-DMA (13 mg/mL) DMG-mPEG2K (1.6 mg/mL) |
9.6% |
| Abraxane® | 130 nm | Paclitaxel (5 mg/mL) | Human Albumin (45 mg/mL) | 11.1% |
| Doxil® Liposome |
100 nm | Doxorubicin HCl (2 mg/mL) | HSPC (9.58 mg/mL) Chol (3.19 mg/mL) DSPE-mPEG (3.19 mg/mL) Trapping Agent: (NH4)2SO4 (2 mg/mL) |
11.1% |
| AmBisome® Liposome |
100 nm | Amphotericin B (50 mg) | HSPC (213 mg) DSPG (84 mg) Chol (52 mg) α-Tocopherol (0.64 mg) |
14.3% |
| Vyxeos® Liposome |
100 nm | Daunorubicin (44 mg) Cytarabine (100 mg) 1: 5 (m/m) |
DSPC (454 mg) DSPG (132 mg) Chol (32 mg) Trapping Agent: Copper Gluconate (100 mg) Triethanolamine (4 mg) |
19.9% |
| Onivyde® Liposome |
110 nm | Irinotecan free base (4.3 mg/mL) | DSPC (6.8 mg/mL) Chol (2.22 mg/mL) DSPE-mPEG2k (0.12 mg/mL) Trapping Agent: Sucrosofate potassium (2.02 mg/mL) |
37.1% |
†
Drug loading % (w/w) = API/(API + Carrier, excluding Trapping Agent) x 100 %