Table 2.
Nanocarrier design criteria for delivery of LY294002.
| Criterion | Discussion |
|---|---|
| Cell type(s) affected by drug (LY294002) | All human cells |
| Mode of administration | Intravenous, intraperitoneal |
| Drug dosage | IC50: 1.4 µM Mouse study: 20 mg/kg Human: unknown |
| Location of therapeutic effect | Intracellular |
| Cellular membrane transport limitation? | No |
| Intracellular processing of NPs | Lysosomal release |
| Polymer carrier | PDLLA-PEG |
| Drug loading range | 10 (mg NP)/mL IP injection at 50 wt% LY loading to reach 20 mg/kg dosage |
| Drug Log P at drug release pH | 3.64 (Log P) |
| Drug pKa | 3.47 |
| Hydrophobic ion pairing agent | HDPA (pKa: 1.81) PA (pKa: 4.95) |
| Solvent(s) suitable for drug dissolution in FNP process | Tetrahydrofuran, dimethylformamide |
| Drug release kinetics | Burst release phase followed by slow, sustained release |
| Importance of triggered release | pH-triggered release below pH 6.5 |