Table 1.
Liposomal formulations. Hydrodynamic diameter (Dh) and polydispersity index (PDI) were measured by dynamic light scattering (DLS). ζ–potential was measured by laser Doppler electrophoresis (LDE). Experiments were performed in three independent replicates. Results are the average of five measurements per replicate (mean ± standard deviation).
| Form. | Composition | Short Name | Procedure | Tm | Dh | PDI | ZP |
|---|---|---|---|---|---|---|---|
| 1 | DOPC/DSPEmPEG2000 (7/3 molar ratio) |
– | Extrusion 50 nm/Sonication | 37 °C | 58.96 ± 1.21 | 0.369 ± 0.02 | −0.57 ± 0.03 |
| 2 | PC/DSPEmPEG2000 (7/6 molar ratio) |
– | Extrusion 50 nm/Sonication | 45 °C | 55.20 ± 2.25 | 0.363 ± 0.09 | −1.59 ± 0.20 |
| 3 | DOPC/DSPEmPEG2000 (7/5 molar ratio) |
– | Extrusion 50 nm/Sonication | 45 °C | 55.5 ± 2.1 | 0.340 ± 0.03 | −2.15 ± 0.30 |
| 4 | DOPC/DSPEmPEG2000 (7/6 molar ratio) |
– | Extrusion 50 nm/Sonication | 37 °C | 45.33 ± 1.2 | 0.476 ± 0.12 | 0.858 ± 0.10 |
| 5 | PC/DSPEmPEG2000 (7/6 molar ratio) |
– | Extrusion 50 nm/Sonication | 45 °C | 52.95 ± 2.1 | 0.467 ± 0.10 | −1.59 ± 0.20 |
| 6 | PC/DSPEmPEG2000 (7/5 molar ratio) |
– | Extrusion 50 nm/Sonication | 45 °C | 53.46 ± 2.10 | 0.377 ± 0.09 | −4.83 ± 1.10 |
| 7 | DOPC/DSPEmPEG2000 (7/6 molar ratio) |
– | Extrusion 50 nm/Sonication | 37 °C | 45.22 ± 1.90 | 0.471 ± 0.12 | −6.87 ± 1.30 |
| 8 | PC/DSPEmPEG2000 (7/6 molar ratio) |
– | Extrusion 50 nm/Sonication | 45 °C | 53.03 ± 0.90 | 0.491 ± 0.13 | −8.72 ± 0.90 |
| 9 | PC/DSPEmPEG2000 (7/5 molar ratio) |
– | Extrusion 30 nm | 45 °C | 52.93 ± 1.25 | 0.271 ± 0.12 | −9.47 ± 1.70 |
| 10 | PC/DSPEmPEG2000 (7/6 molar ratio) |
– | Extrusion 30 nm | 45 °C | 47.76 ± 3.90 | 0.273 ± 0.09 | −15.0 ± 2.10 |
| 11 | DPPC/Chol/PE/DSPEmPEG2000 (7/7/4/1 molar ratio) |
– | Extrusion 50 nm/Sonication | 50 °C | 55.58 ± 1.90 | 0.194 ± 0.09 | −12.63 ± 1.23 |
| 12 | PC/Chol/PE/DSPEmPEG2000
(7/7/4/1 molar ratio) |
– | Extrusion 50 nm/Sonication | 50 °C | 54.16 ± 2.10 | 0.197 ± 0.08 | −11.06 ± 0.30 |
| 13 | DOPC/DPPC/DSPEmPEG2000
(7/4/3 molar ratio) |
– | Extrusion 50 nm/30 nm | 40 °C | 51.5 ± 8.90 | 0.172 ± 0.10 | −5.40 ± 5.0 |
| 14 | DPPC/DPPS/Chol (7/4/7 molar ratio) |
– | Extrusion 50 nm | 50 °C | 64.93 ± 1.21 | 0.053 ± 0.02 | −41.94 ± 2.90 |
| 15 | DSPC/DSPEmPEG2000 (7/3 molar ratio) |
DS | Extrusion 30 nm | 60 °C | 26.3 ± 1.2 | 0.578 ± 0.02 | −10.51 ± 0.18 |
| 16 | DSPC/DOPC/DSPEmPEG2000
(7/1/2 molar ratio) |
DO | Extrusion 30 nm | 60 °C | 54.46 ± 3.03 | 0.209 ± 0.03 | −9.84 ± 0.40 |
| 4 oxa | DOPC/DSPEmPEG2000 (7/6 molar ratio) + oxa |
– | Extrusion 30 nm | 42 °C | 64.5 ± 1.1 | 0.239 ± 0.91 | −6.17 ± 1.23 |
| 10 oxa | PC/DSPEmPEG2000 (7/6 molar ratio) + oxa |
– | Extrusion 30 nm | 50 °C | 75.2 ± 1.2 | 0.365 ± 0.14 | −4.25 ± 1.60 |
| 13 oxa | DOPC/DPPC/DSPEmPEG2000 (7/4/3 molar ratio) + oxa |
– | Extrusion 30 nm | 50 °C | 64.65 ± 5.15 | 0.098 ± 0.01 | −5.35 ± 2.40 |
| 15 oxa | DSPC/DSPEmPEG2000 (7/3 molar ratio) + oxa |
DS-oxa | Extrusion 30 nm | 60 °C | 44.25 ± 4.25 | 0.315 ± 0.04 | −10.95 ± 0.4 |
| 16 oxa | DSPC/DOPC/DSPEmPEG2000 (7/1/2 molar ratio) + oxa |
DO-oxa | Extrusion 30 nm | 60 °C | 42.60 ± 3.80 | 0.251 ± 0.01 | −9.41 ± 1.95 |
Abbreviations: Form—formulation; PC—chicken egg L-α-phosphatidylcholine; Chol—cholesterol; PE—1,2-dipalmitoyl-sn-glycero-3-phosphatidylethanolamine; DSPEmPEG2000—1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000]; DOPC—1,2-dioleoyl-sn-glycero-3-phosphocholine; DPPC—1,2-dipalmitoyl-sn-glycero-3-phosphocholine; DSPC—1,2-distearoyl-sn-glycero-3-phosphocholine; oxa—oxaliplatin; Dh—hydrodynamic diameter (nm); ZP—ζ–potential (mV); MSV—multistage vector; oxa—oxaliplatin. DS—selected liposomal formulation containing DSPC as main lipid. DO—selected liposomal formulation containing DSPC and DOPC as main lipids.