Table 2.
EC50 and EC90 values of single and combinatorial poly(HPMA)–GFLG-conjugates against L. donovani amastigotes in peritoneal exudate macrophages, for one representative experiment
| Conjugate | AmB (wt %) | Al. acid (wt %) | EC50 (μg/ml) | EC90 (μg/ml) |
|---|---|---|---|---|
| Amphotericin B | >95 | N/A | 0.06 (0.04–0.09) | 0.44 (0.20–0.68) |
| Fungizone® | N/A | N/A | 0.07 (0.04–0.10) | 0.13 (0.11–0.15) |
| CIR1668 | 9.63 | 0 | 0.09 (0.08–0.10) | 0.68 (0.30–1.06) |
| CIR1790 | 0 | 7.88 | n.o. | n.o. |
| CIR1791 | 8.15 | 5.49 | 0.18 (0.09–0.27) | 1.18 (0.60–1.76) |
| CIR1792 | 13.43 | 3.92 | 0.13 (0.09–0.17) | 0.36 (0.20–0.52) |
| CIR1793 | 19.55 | 1.83 | 0.05 (0.03–0.07) | 0.22 (0.13–0.31) |
| CIR1783 | 16.93 | 0 | 0.06 (0.04–0.08) | 0.21 (0.14–0.28) |
| CIR1465 | 0 | 0 | n.o. | n.o. |
| CIR1466 | 0 | 0 | n.o. | n.o. |
The infection level in untreated controls was 77%. Values are given as amphotericin B equivalent in μg/ml with 95% confidence intervals in brackets (n = 4). Drug loading is given in weight% (wt %). N/A not applicable, n.o. not obtained as CIR1465,11 CIR146611 and CIR1790 were inactive within the concentration range tested. No toxicity to the macrophages was observed at the concentrations of copolymer used.