Magnetic polycarbonate microspheres for tumor-targeted delivery of tumor necrosis factor

Figures & data

Scheme 1. Synthetic routes of polycarbonate copolymer and conjugate T₉-TNF.

Figure 1. ¹H NMR spectrum of P(TMC-co-DTC).

Figure 2. ¹C NMR spectrum of P(TMC-co-DTC).

Figure 3. IR spectrum of P(TMC-co-DTC).

Figure 4. GPC spectrum of P(TMC-co-DTC) (Mn: 7.615 × 10⁴, Mw/Mn: 3.10).

Figure 5. SEM photograph of T₉-TNF-PC-M.

Figure 6. Release profiles of TNF from anti-cancer magnetic polymer microspheres T₉-TNF-PC-M in PBS at 37 °C.

Table 1. In vitro anti-tumor activity of microspheres to human hepatocellular carcinoma Bel-7402 cells.

Microsphere	Dose (U)	OD^a (X ± S)	Inhibition^a (%)
Blank test (0.9% NaCl)	–	0.346 ± 0.049	–
PC-M	–	0.328 ± 0.014	5.2 ± 0.21
TNF	5000	0.148 ± 0.006	57.3 ± 2.29
T9-TNF	5000	0.130 ± 0.027	62.4 ± 2.49
T9-TNF-PC	500	0.094 ± 0.044	70.6 ± 2.82
T9-TNF-PC-M	500	0.102 ± 0.007	72.8 ± 2.91

^aThe data points denote the means with standard error bars for fine cases.

Table 2. In vivo inhibitory effect of microspheres on nude mice-bearing human hepatocellular carcinoma.

Group	Dose of TNF (U)	Mice number (start/end)	Weight of cancer^a (g)	Inhibition^a (%)
Blank test  (0.9% NaCl)	–	6/6	4.130 ± 0.261	–
PC-M	–	6/6	4.170 ± 0.348	–
TNF	10 000	6/5	3.022 ± 0.340	26.9 ± 1.08
T9-TNF	10 000	6/5	1.621 ± 0.476	60.8 ± 2.43
T9-TNF-PC	1000	6/5	1.539 ± 0.548	62.7 ± 2.51
T9-TNF-PC-M	1000	6/5	1.305 ± 0.382	68.4 ± 2.73

^aThe data points denote the means with standard error bars for fine cases.

Figure 7. Inhibitory effects of T₉-TNF-PC and T₉-TNF-PC-M microspheres on human hepatocellular carcinoma.