Table 1.
Polymers prepared and evaluated.
| Name | Conjugate | Total ManN (% w/w)a | Total AmB (% w/w)b | Free AmB (% total drug)c |
|---|---|---|---|---|
| HPMA-GFLG-ONp | – | – | – | |
| CIR1592 | HPMA-GFLG-AmB | – | 27.5 | <0.5 |
| CIR1668 | HPMA-GFLG-AmB | – | 9.6 | <0.1 |
| CIR1669 | HPMA-GFLG-ManN-AmB | 5.9 | 10.4 | <1.0 |
| CIR1770 | HPMA-GFLG-ManN | 5.9 | – | – |
| CIR1465 | HPMA-GFLG-COOH | – | – | – |
| CIR1466 | HPMA-GFLG-AP |
ManN, mannosamine; AmB, amphotericin B; HPMA, N-(2-hydroxypropyl)methacrylamide; GFLG, GlyPheLeuGly linker; ONp, para-nitrophenol ester; AP, 1-amino-2-propanol.
a
The content of ManN in the conjugates CIR1669 and CIR1770 was determined by a modified Morgan and Elson method.
b
The content of total Am B in the conjugates (CIR1592, CIR1668 and CIR1669) was determined by UV-Vis analysis.
c
Free residual AmB, reported as weight % of the total loaded drug, was determined by high-performance liquid chromatography (HPLC) analysis.