Targeted delivery of etoposide to cancer cells by folate-modified nanostructured lipid drug delivery system

Figures & data

Table 1. The Box–Behnken design of FA-ETP-NLCs and evaluated response parameters.

Formulation codes	Lipid/drug ratio (X1)	Surfactant (X2) (%w/v)	FA-PEG-DSPE (X3) (%w/v)	Particle size (nm)	PDI	EE (%)
1	15	3	0.4	126.87	0.172	77.28
2	10	2	0.4	126.23	0.143	82.47
3	10	3	0.2	142.01	0.201	75.26
4	10	2	0.4	124.25	0.138	82.61
5	15	2	0.2	118.16	0.183	78.95
6	15	1	0.4	202.73	0.329	75.33
7	5	1	0.4	119.37	0.188	76.24
8	10	1	0.2	125.57	0.19	80.11
9	5	3	0.4	258.19	0.4	68.32
10	10	2	0.4	123.45	0.141	82.76
11	10	2	0.4	125.32	0.136	82.64
12	5	2	0.6	309.21	0.247	76.27
13	5	2	0.2	137.78	0.203	77.34
14	15	2	0.6	273.15	0.19	82.31
15	10	3	0.6	312.46	0.248	78
16	10	2	0.4	122.77	0.146	82.81
17	10	1	0.6	274.38	0.206	78.38

Figure 1.Response surface analyses plotted in three-dimensional model graphs for depicting the effects of the predetermined factors on the PS, PDI or EE.

Figure 2. TEM image of FA-ETP-NLCs.

Table 2. Serum stability of NLCs.

Samples	Particle size (nm)		Size distribution (PDI)		EE (%)
	Milli-Q water	50% FBS	Milli-Q water	50% FBS	Milli-Q water	50% FBS
Blank NLCs	81.74 ± 2.31	82.35 ± 3.86	0.091 ± 0.009	0.112 ± 0.019	/	/
ETP-NLCs	82.16 ± 2.87	83.94 ± 3.17	0.116 ± 0.013	0.136 ± 0.016	84.71 ± 2.14	83.59 ± 3.76
FA-ETP-NLCs	120.91 ± 3.59	122.13 ± 4.41	0.139 ± 0.026	0.181 ± 0.033	83.86 ± 3.21	82.92 ± 4.18

Figure 3. The in vitro release profiles of FA-ETP-NLCs, ETP-NLCs and ETP solution.

Table 3. IC₅₀ values (μg/ml) of various formulations in different cells.

Cells	ETP solution	ETP-NLCs	FA-ETP-NLCs
CT26	11.81 ± 0.86	2.13 ± 0.34	0.58 ± 0.11
SGC7901	57.2 ± 3.15	10.46 ± 0.98	3.87 ± 0.59
NCI-H209	41.75 ± 4.37	12.37 ± 1.08	4.42 ± 0.85

Figure 4. Tissue distribution results of FA-ETP-NLCs.

Figure 5. Tissue distribution results of ETP-NLCs.

Figure 6. Tissue distribution results of ETP solution.

Figure 7. In vivo antitumor efficacy of different formulations in gastric tumor-bearing mice.