Table 1.
Characteristics of HPMA copolymer conjugates
| Polymer | Description | ----- Feed composition - (mol%) ----- | Apparent Mwb (kDa) |
Mw /Mn |
Drug contentc wt% (% conversion) |
RGDfK contentd wt % (% conversion) |
||||
|---|---|---|---|---|---|---|---|---|---|---|
| HPMA | MA- GG- ONp |
MA-GG- RGDfK |
MA- GFLG- Xa |
MA- Tyr- CONH2 |
||||||
| p-AHGDM | Non-targeted AHGDM conjugate | 83 | 10 | - | 5 | 2 | 23 | 1.7 | 13.9 (85%) | - |
| p-AHGDM-RGDfK | αvβ3targeted AHGDM conjugate | 83 | 10 | - | 5 | 2 | 27 | 1.7 | 10.6 (84%) | 19.3 (82%) |
| p-DOC | Non-targeted DOC conjugate | 95.5 | - | - | 2.5 | 2 | 20 | 1.8 | 7.2 (62%) | - |
| p-DOC-RGDfK | αvβ3targeted DOC conjugate | 85.5 | - | 10 | 2.5 | 2 | 23 | 1.9 | 6.2 (73%) | 17.1 (67%) |
| HPMA | Control copolymer | 88 | 10 | - | - | 2 | 18 | 1.6 | - | - |
| p-RGDfK | Control αvβ3targeted copolymer | 88 | 10 | - | - | 2 | 21 | 1.6 | - | 21.2 (74%) |
a
Where X is either AHGDM or DOC;
b
Estimated by size exclusion chromatography;
c
Determined by UV spectroscopy for AHGDM and enzymatic release / HPLC for DOC;
d
Determined by amino acid analysis (HPLC).