Table 2. Effect of the lipid-to-drug ratio on the degree of drug incorporation into lipid-drug nanoparticles and the particle size.
| Lipid-drug nanoparticlesa | lipid : drug (mol/mol) | Incorporation efficiency (%)b | Particle sizec (nm) |
|---|---|---|---|
| Control (no drug) | 1 : 0 | ——— | 35.4 ± 4.4 |
|
| |||
| Atazanavir (ATV) | 20 : 1 | 97.4 ± 1.8 | 34.6 ± 3.1 |
| 8 : 1 | 96.2 ± 3.8 | 56.3 ± 4.1 | |
| 5 : 1 | 96.5 ± 2.6 | 68.2 ± 7.1 | |
|
| |||
| Darunavir (DRV) | 20 : 1 | 96.6 ± 4.8 | 35.6 ± 3.7 |
| 8 : 1 | 94.4 ± 2.8 | 35.6 ± 3.9 | |
| 5 : 1 | 88.1 ± 3.8 | 33.6 ± 3.1 | |
a
Lipid-drug nanoparticles containing ATV or DRV with different lipid-to-drug molar ratios were prepared as described in Materials and Methods.
b
Drug incorporation efficiency was determined based on % of drug bound to particles after removal of free, unincorporated drugs; data were expressed as mean ± SD of 4 replicates.
c
Lipid-drug particle diameters were determined using PCS and the data were expressed as mean ± SD of 4 replicates.