F7 and topotecan co-loaded thermosensitive liposome as a nano-drug delivery system for tumor hyperthermia

Figures & data

Figure 1. Schematic illustration of the fabrication process and structure of F7-TPT-TSL and its applications in chemotherapy combined with hyperthermia.

Table 1. Physicochemical properties of different liposome preparations.

Code	Encapsulation efficiency (%)		Particle size (nm)	PDI	Potential (mV)
	F7	TPT
Blank TSL	–	–	89.86 ± 3.34	0.173 ± 0.016	–8.62 ± 1.01
F7-TSL	99.97 ± 2.27	–	111.63 ± 8.81	0.201 ± 0.020	–15.48 ± 6.20
TPT-TSL	–	98.73 ± 0.39	105.64 ± 8.68	0.200 ± 0.020	–16.91 ± 3.32
F7-TPT-TSL	97.42 ± 0.74	95.15 ± 4.23	103.00 ± 9.84	0.194 ± 0.015	–14.28 ± 4.02

Figure 2. TEM image (a), particle size distribution (b), and potential distribution (c) of F7-TPT-TSL.

Figure 3. Differential scanning calorimetry phase transition temperature map.

Figure 4. Temperature-triggered release behaviors of F7-TPT-TSL at 41 °C and 37 °C (n = 3).

Figure 5. Transmission and backscattering profiles of liposome preparation by using a Turbiscan Lab@ Expert. The stability image (a) TSL, (b) F7-TPT-TSL, (c) F7 solution, (d) TPT solution diluted with water for 24 h at 25 °C, (e) TSL, (f) F7-TPT-TSL, (g) F7 solution, and (h) TPT solution diluted with serum for 24 h at 37 °C. Data are reported as a function of time and sample height (20–34 mm).

Figure 6. Cellular uptake of Cou6-DOX-solution and CD-TSL by H460 cells after 4 h incubation at 37 °C. Images of bright field, nuclei stained with DAPI (blue), 6-coumarin (green), DOX (red), and merged. Scale bar: 100 μm.

Figure 7. Apoptosis analysis of MCF-7 cells induced by F7 solution and F7-TSL for 24 h.

Figure 8. Interaction between F7 and TPT affects H460 cell growth. The graph shows CI values after treatment. CI < 1 represents a synergistic effect and CI > 1 indicates a less than additive effect of combined treatment. CI = 1 indicates that the effect is additive. CI values for the combination of F7 and TPT were calculated using CompuSyn software.

Figure 9. Cell viability of different preparations and concentrations. F7-TPT-TSL with TPT + F7 solution (p < .001); F7 – TPT-TSL/H with TPT + F7 solution (p < .001); and F7-TPT-TSL/H with F7 + TPT-TSL (p < .001).

Table 2. IC₅₀ values of different formulations.

Different formulations	TPT solution	F7 solution	F7 + TPT solution	TPT-TSL	F7-TSL	F7-TPT-TSL	F7-TPT-TSL/H
IC50 (μΜ)	0.8184	0.4426	0.3052	0.3951	0.1828	0.2154	0.07524

Figure 10. (a) Anticancer efficacy in MCF-7 xenografts in female nude mice after treatment with varying formulations; (b) weights of dissected tumors at the end of treatment; (c) relative weight change of varying formulations in tumor-bearing nude mice; (d) tumor inhibition rate of varying formulations in tumor-bearing nude mice. **p < .01 (n = 6).

Table 3. Relative weight change of different formulations.

Different formulations	Control	F7-solution	TPT-solution	F7-TPT-solution	F7-TPT-solution/H	F7-TSL	TPT-TSL	F7-TPT-TSL	F7-TPT-TSL/H
Tumor weight (g)	2.25 ± 0.28	1.64 ± 0.12	1.82 ± 0.11	1.32 ± 0.08	1.18 ± 0.18	1.05 ± 0.16	1.71 ± 0.12	0.74 ± 0.02	0.33 ± 0.08
Body weight (g)/0 d	20.82 ± 0.56	20.88 ± 0.96	20.86 ± 0.74	20.78 ± 0.22	20.68 ± 0.15	20.92 ± 0.45	21.04 ± 0.33	20.78 ± 0.42	20.85 ± 0.53
Body weight (g)/22 d	24.86 ± 1.61	19.23 ± 1.12	21.34 ± 1.14	19.64 ± 1.52	20.52 ± 0.86	20.42 ± 0.76	21.74 ± 0.84	20.68 ± 0.56	20.60 ± 0.88
Relative weight change (%)	8.60 ± 1.23	–15.76 ± 1.26	–6.42 ± 1.22	–11.84 ± 1.04	–6.48 ± 0.65	–7.41 ± 0.32	–4.80 ± 0.46	–4.04 ± 0.57	–2.78 ± 0.22