Cisplatin and paclitaxel co-delivered by folate-decorated lipid carriers for the treatment of head and neck cancer

Figures & data

Figure 1. (1) Scheme graph of the construction of FA-DDP/PTX NLCs; (2) TEM image of FA-DDP/PTX NLCs.

Table 1. Decoration ratio determination.

Weight of ligands (g)	0.1	0.2	0.3	0.4	0.5
Zeta potential (mV)	+36.3 ± 2.6	+ 31.9 ± 2.3	+ 26.6 ± 1.9	+ 26.4 ± 2.1	+ 26.8 ± 2.4
Particle size (nm)	118.3 ± 2.9	121.3 ± 3.1	126.9 ± 3.2	128.4 ± 3.6	618.3 ± 54.6

Figure 2. (1) Changes in size in the presence of serum: (1) FA-DDP/PTX NLCs, (2) DDP/PTX NLCs, (3) PTX NLCs, (4) DDP NLCs; (2-2) changes in DEE in the presence of serum: (1) DDP DEE of FA-DDP/PTX NLCs, (2) PTX DEE of FA-DDP/PTX NLCs, (3) DDP DEE of DDP/PTX NLCs, (4) PTX DEE of DDP/PTX NLCs, (5) PTX DEE of PTX NLCs, and (6) DDP DEE of DDP NLCs.

Table 2. Characterization.

Formulations	NLCs	DDP NLCs	PTX NLCs	DDP/PTX NLCs	FA-DDP/PTX NLCs
Particle size (nm)	96.7 ± 2.6	100.2 ± 3.5	99.8 ± 3.7	101.9 ± 4.8	127.1 ± 5.1
Size distribution (PDI)	0.13 ± 0.03	0.17 ± 0.04	0.19 ± 0.05	0.21 ± 0.06	0.23 ± 0.07
Zeta potential (mV)	31.9 ± 3.4	39.5 ± 3.6	36.7 ± 3.1	43.7 ± 4.1	26.7 ± 2.2
DEE of DDP (%)	N/A	85.6 ± 3.9	N/A	84.9 ± 2.9	82.1 ± 3.4
DEE of PTX (%)	N/A	N/A	80.6 ± 2.8	81.6 ± 3.3	79.2 ± 3.1
DLC of DDP (%)	N/A	13.2 ± 1.2	N/A	9.1 ± 0.9	5.2 ± 0.6
DLC of PTX (%)	N/A	N/A	10.6 ± 1.4	8.3 ± 1.0	4.7 ± 0.5

Figure 3. (1) In vitro DDP and PTX release at pH 7.4; (2) in vitro DDP and PTX release at pH 5.0: (1) DDP releases from FA-DDP/PTX NLCs, (2) DDP release from DDP/PTX NLCs, (3) PTX release from FA-DDP/PTX NLCs, and (4) PTX release from DDP/PTX NLCs.

Figure 4. In vitro cell viabilities: (1) FA-DDP/PTX NLCs, (2) DDP/PTX NLCs, (3) PTX NLCs, (4) DDP NLCs, (5) PTX solutions, and (6) DDP solutions.

Table 3. The IC₅₀ values and CI₅₀.

Formulations	DDP solutions	PTX solutions	DDP NLCs	PTX NLCs	DDP/PTX NLCs	FA-DDP/PTX NLCs
IC50 of DDP (μM)	46.5 ± 3.1	N/A	4.7 ± 0.8	N/A	1.1 ± 0.3	0.6 ± 0.1
IC50 of PTX (μM)	N/A	36.9 ± 3.6	N/A	6.1 ± 0.7	1.1 ± 0.3	0.6 ± 0.1
CI50	N/A	N/A	N/A	N/A	0.81	0.57

Figure 5. (1) In vivo DDP tissue distribution of FA-DDP/PTX NLCs; (2) in vivo PTX tissue distribution of FA-DDP/PTX NLCs.

Figure 6. (1) The tumor growth curves; (2) body weight change curves: (1) FA-DDP/PTX NLCs, (2) DDP/PTX NLCs, (3) PTX NLCs, (4) DDP NLCs, (5) PTX solutions, (6) DDP solutions, and (7) 0.9% saline.

Table 4. The tumor growth inhibition ratio (TGI).

Formulations	DDP solutions	PTX solutions	DDP NLCs	PTX NLCs	DDP/PTX NLCs	FA-DDP/PTX NLCs
TGI (%)	9.3	11.0	41.7	48.8	70.4	81.1