Table 1.
Composition and characterization data of besifloxacin liposomes produced by lipid film hydration.
| Formulation | PC (mmol/L) | CH (mmol/L) | SA (mmol/L) | SPM (mmol/L) | Drug (mg) | Drug solubilization phase | DR (%) | EE (%) |
|---|---|---|---|---|---|---|---|---|
| Drug solubilization medium | ||||||||
| F1 | 140 | – | – | – | 2 | Lipid phase | 63 ± 1.9 | 26 ± 5.18 |
| F2 | 140 | – | – | – | 2 | Aqueous phase | 83 ± 1.5 | 37 ± 0.94 |
| pH of solubilization medium | ||||||||
| LP PC | 140 | – | – | – | 2 | Aqueous acid phase | 93 ± 0.5 | 51 ± 1.92 |
| Drug loading dose | ||||||||
| F4 | 140 | – | – | – | 1 | Aqueous acid phase | 97 ± 0.8 | 52 ± 1.03 |
| F5 | 140 | – | – | – | 3 | Aqueous acid phase | 83 ± 0.5 | 41 ± 2.19 |
| F6 | 140 | – | – | – | 4 | Aqueous acid phase | 74 ± 1.0 | 45 ± 1.35 |
| Phospholipids concentration and cholesterol addition | ||||||||
| F7 | 200 | – | – | – | 2 | Aqueous acid phase | 59 ± 0.9 | 55 ± 1.48 |
| F8 | 40 | 10 | – | – | 2 | Aqueous acid phase | 56 ± 2.9 | 27 ± 8.86 |
| F9 | 30 | 20 | – | – | 2 | Aqueous acid phase | 40 ± 1.9 | 30 ± 12.74 |
| F10 | 20 | 10 | – | – | 2 | Aqueous acid phase | 60 ± 3.8 | 28 ± 12.19 |
| Cationic amines addition | ||||||||
| F11 | 150 | – | – | 50 | 2 | Aqueous basic phase | 53 ± 0.8 | 21 ± 5.60 |
| LP PC: SPM | 150 | – | – | 90 | 2 | Aqueous basic phase | 68 ± 2.5 | 63 ± 1.86 |
| F13 | 150 | – | 50 | – | 2 | Aqueous basic phase | 48 ± 1.3 | 13 ± 7.74 |
| F14 | 150 | – | 90 | – | 2 | Aqueous basic phase | 65 ± 3.4 | 25 ± 0.66 |
DR drug recovery, EE% entrapment efficiency, PC phosphatidylcholine, CH cholesterol, SA sterilamine, SPM spermine.