Which one performs better for targeted lung cancer combination therapy: pre- or post-bombesin-decorated nanostructured lipid carriers?

Figures & data

Figure 1. Schematic representation of the synthesis of BN-PEG-SA ligands.

Figure 2. Schematic diagrams showing the preparation of Pre-BN-DOX-DNA-NLC (A) and Post-BN-DOX-DNA-NLC (B).

Table 1. Quantification of conjugation of BN to NLC surface.

Formulations	Particle size (nm)	Size distribution (PDI)	Zeta potential (mV)	Conjugation efficiency (%)	Conjugation ratio (μg/mg)
DOX-DNA-NLC	86.61 ± 2.35	0.096 ± 0.019	+8.6 ± 1.1	–	–
Post-NLC1	109.23 ± 3.28	0.123 ± 0.023	+16.8 ± 2.3	95.68 ± 1.46	8.0 ± 0.3
Post-NLC2	115.36 ± 3.51	0.147 ± 0.022	+21.4 ± 2.8	91.34 ± 2.97	15.2 ± 0.7
Post-NLC3	126.76 ± 2.69	0.102 ± 0.021	+28.8 ± 1.9	85.68 ± 2.52	28.6 ± 0.6
Post-NLC4	128.14 ± 4.15	0.184 ± 0.028	+29.1 ± 3.6	43.12 ± 3.09	28.7 ± 0.8

Table 2. Characterization of different NLC formulations.

Formulations	Particle size (nm)	Size distribution (PDI)	Zeta potential (mV)	DNA EE (%)	DOX EE (%)	DNA DL (%)	DOX DL (%)
Blank NLC	82.55 ± 2.19	0.097 ± 0.011	+21.5 ± 3.3	–	–	–	–
DOX-DNA-NLC	85.97 ± 2.28	0.112 ± 0.018	+8.7 ± 0.9	91.5 ± 2.6	86.7 ± 3.3	8.3 ± 1.5	2.3 ± 0.6
Post-BN-DOX-DNA-NLC	128.03 ± 2.31	0.165 ± 0.021	+28.4 ± 1.8	90.8 ± 2.3	85.3 ± 2.9	5.2 ± 0.9	1.4 ± 0.4
Pre-BN-DOX-DNA-NLC	101.36 ± 2.31	0.134 ± 0.020	+23.7 ± 2.5	91.7 ± 2.1	86.2 ± 3.1	5.7 ± 1.1	1.6 ± 0.3
Lipo-DNA complexes	178.64 ± 8.76	0.153 ± 0.032	+26.4 ± 2.1	90.2 ± 3.2	–	6.2 ± 1.2	–

Figure 3. In vitro DOX release profile of Post-BN-DOX-DNA-NLC (A), Pre-BN-DOX-DNA-NLC (B), DOX-DNA-NLC (C), and Free DOX (D).

Figure 4. In vitro DNA release profile of Post-BN-DOX-DNA-NLC (A), Pre-BN-DOX-DNA-NLC (B), and DOX-DNA-NLC (C).

Figure 5. In vitro cytotoxicity of blank control (A), blank NLC (B), free DOX (C), DOX-DNA-NLC (D), Pre-BN-DOX-DNA-NLC (E), and Post-BN-DOX-DNA-NLC (F).

Figure 6. In vitro gene transfection of blank NLC (A), naked DNA solution (B), Lipo-DNA (C), DOX-DNA-NLC (D), Pre-BN-DOX-DNA-NLC (E), and Post-BN-DOX-DNA-NLC (F).

Figure 7. In vivo gene transfection of blank NLC (A), naked DNA solution (B), Lipo-DNA (C), DOX-DNA-NLC (D), Pre-BN-DOX-DNA-NLC (E), and Post-BN-DOX-DNA-NLC (F).

Figure 8. Effects of different formulations on tumor growth in lung cancer bearing mice. Note: (A), 0.9% sodium chloride solution; (B), free DOX; (C), DOX-DNA-NLC; (D), Pre-BN-DOX-DNA-NLC; and (E), Post-BN-DOX-DNA-NLC.

Figure 9. Body weight changes after treatment with different formulations in lung cancer bearing mice. Note: (A), 0.9% sodium chloride solution; (B), free DOX; (C), DOX-DNA-NLC; (D), Pre-BN-DOX-DNA-NLC; and (E), Post-BN-DOX-DNA-NLC.