Table 1. Drug loading properties of nanocarrier library.
DBM (rank-ing) | DOX | PEG5KDBM8 (G1) | PEG5KCA4DBM4 (G2) | PEG5KCA4-L-DBM4 (G3) | |||||||
---|---|---|---|---|---|---|---|---|---|---|---|
CMC (μM) | Size (nm) | DOX LE (%)a LE0 - LE1 - LE7 | CMC (μM) | Size (nm) | DOX LE (%)a LE0 - LE1 - LE7 | CMC (μM) | Size (nm) | DOX LE (%)a LE0 - LE1 - LE7 | |||
AQ(1) | 0 | 2.84 | PPT | N/A | 2.1 | MP | N/A | 2.36 | MP | N/A | |
10% | - | PPT | 49- - | - | 24±7 | 100-100-91 | - | 27±7 | 100-94-100 | ||
20% | - | - | - | - | 25±6 | 100-87-93 | - | 29±9 | 100-96-100 | ||
30% | - | - | - | - | 20 ±5 | 100-84-61 | - | 30±8 | 100-71-58 | ||
40% | - | - | - | - | MP | 94-54-66 | - | - | - | ||
Rh(2) | 0 | ND | PPT | N/A | 0.93 | 17±5 | N/A | 2.7 | 32±8 | N/A | |
10% | - | PPT | - | 0.89 | 20±5 | 100-100-100 | 1.1 | 30±8 | 100- 100-100 | ||
20% | - | - | - | - | 24±7 | 100-98-100 | - | 28±7 | 100-78-86 | ||
30% | - | - | - | - | 19±4 | 100-85-95 | - | 21±5 | 100-56-64 | ||
40% | - | - | - | - | 15±4 | 100-75-97 | - | - | - | ||
LiCA(4) | 0 | 1.18 | 36±11 | N/A | 1.45 | 17±4 | N/A | 1.2 | 17±4 | N/A | |
10% | - | 350/49 b | 100-100-87 | - | 14±3 | 100-100-57 | 15±3 | 100- 93-59 | |||
20% | - | 59/33 b | 99-70-52 | - | 16±4 | 100-64-29 | Mp | 98-46-19 | |||
Cho(5) | 0 | 0.89 | PPT | N/A | 0.75 | 17±4 | N/A | 1.2 | 18±4 | N/A | |
10% | - | MP | 100-100-87 | - | 39±12 | 100-100-42 | - | 23±7 | 100-84-33 | ||
20% | - | - | - | - | 41±16 | 100-72-30 | - | 24±8 | 93-63-18 | ||
Co(8) | 0 | 2.59 | 35 ± 12 | N/A | 1.99 | 14 ± 4 | N/A | 1.7 | 36 ± 13 | N/A | |
10% | - | 28 ± 9 | 100-100-92 | - | 13 ± 2 | 100-97-97 | - | 36 ± 13 | 100-100-85 | ||
20% | - | 27 ± 8 | 100-94-73 | - | 385/133 b | 99-82-84 | - | 38 ± 13 | 100-68-80 | ||
30% | - | 32 ± 10 | 100-75-65 | - | - | - | - | 342/32 b | 99-60-74 | ||
Phe (11) | 0 | 1.77 | 42±19 | N/A | 2.86 | 13±3 | N/A | 2.9 | 103±39 | N/A | |
10% | - | 34±9 | 100-100-92 | - | 185/14 | 100-75-36 | - | 240/22 b | 100-91-36 | ||
20% | - | 34±14 | 100- 95-100 | - | - | - | - | 17±4 | 92-45-13 | ||
30% | - | 29 ±8 | 100-53-40 | - | - | - | - | - | - | ||
VE(12) | 0 | 2.5 | MP | N/A | 1.6 | MP | N/A | 1.4 | 25±6 | N/A | |
10% | MP | 78-64-55 | - | 38±15 | 100-90-65 | - | 23±6 | 100-85-61 | |||
20% | N/A | N/A | - | 36±12 | 96-50-34 | - | 24±6 | 84-46-25 | |||
C17 (13) | 0 | 1.66 | PPT | N/A | 1.33 | 13±4 | N/A | 2.7 | MP | N/A | |
10% | - | 408/61 | 86- - | - | 14±2 | 100-92-32 | - | 196±99 | 100-92-43 | ||
20% | - | - | - | - | 14±3 | 85-61-24 | - | MP | 90-44-17 |
Note:
DOX loading efficiency (LE) were measured by fluorescence (λex=470 nm, λem=590 nm) measurements of samples before and after spin at the speed of 13,000g for 5 min; The drug loading efficiencies were measured right after drug loading process (LE0) and after a storage at 4 °C overnight (LE1) or after a storage at room temperature for one week (LE7). Therefore drug loading efficiencies were presented as LE0 - LE1 - LE7.
Two peaks were detected in DLS particle size analysis; N/A: not applicable; ND: not detected; MP: multiple peaks; PPT: precipitation; -: not tested