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. 2017 Oct 9;12(21):1759–1767. doi: 10.1002/cmdc.201700466

Table 4.

Release of APIs from formulations with (CG)4TBA (1) or (CG)4TOA (2) into serum, as measured after 24 h.

Hybrid API Molar ratio: API/hybrid Amount of API in preparation [nmol] Medium[a] API release after 24 h [nmol] (% of API)
1 daunomycin 8:1 400 FBS 35 (9)
1 doxorubicin 12:1 620 FBS 26 (4)
1 epirubicin 12:1 117 FBS[b] 10 (9)
1 proflavine 10:1 100 FBS[b] 24 (24)
1 mitoxantrone 5:1 50 FBS[b] 10 (20)
1 imatinib 8:1 84 69 H2O FBS 15 (18) 55 (79)
1 tetracycline 5:1 38 H2O 15 (40)
1 streptomycin H2O n.d.[c]
1 methotrexate 1.2:1 180 H2O[d] 35 (20)
1 gramicidin A 0.5:1 5 H2O[e] 5 (quant.)
1 cyclosporin A 1:1 10 H2O[e] 10 (quant.)
2 doxorubicin 13:1 130 FBS 19 (15)
2 [f] doxorubicin 11:1 110 FBS 22 (20)
2 imatinib 20:1 120 FBS 82 (68)
2 [f] imatinib 6:1 60 FBS 60 (quant.)

[a] Treated with 100 μL medium at 37 °C for 1 d, unless otherwise noted. [b] Treated with 200 μL. [c] Solid was treated with H2O at 50 °C; streptomycin was detected by TLC. [d] Solid was treated at 50 °C for 15 min. [e] Solid was treated with 200 μL at 70 °C for 10 min and stored at 37 °C for 1 d, after which time it had dissolved quantitatively. [f] Inclusion compound had been prepared at a mixing temperature of 37 °C. All other inclusion compounds had been prepared at a mixing temperature of 70 °C.