Prostate-specific membrane antigen targeted, glutathione-sensitive nanoparticles loaded with docetaxel and enzalutamide for the delivery to prostate cancer

Figures & data

Figure 1. GUL-PEG-SS-OA was synthesized by conjugating PEG, OA with GUL. The formation of PEG-SS-OA was determined by using hydrogen-1 nuclear magnetic resonance (¹H NMR) analysis (1–8 in the ¹H NMR are marked one by one on the structure of GUL-PEG-SS-OA).

Figure 2. TEM image of GUL-SS DTX/EZL-NPs (A); In vitro drug release of DTX (B) and EZL (C) from GUL-SS DTX/EZL-NPs were evaluated in phosphate buffer solution (PBS) with or without GSH (10 mM) by a dialysis method. Results are presented as means ± SD. *p < .05.

Table 1. The particle size, PDI, zeta potential, DL, and EE of NPs.

				DL (%)		EE (%)
NPs	Diameter (nm)	PDI	Zeta potential (mV)	DTX	EZL	DTX	EZL
GUL-SS DTX/EZL-NPs	143.7 ± 4.1	0.162 ± 0.037	+ 29.1 ± 2.4	6.3 ± 0.7	6.1 ± 0.6	90.9 ± 2.7	89.5 ± 2.9
GUL-SS NPs	141.6 ± 3.8	0.145 ± 0.022	+ 27.9 ± 2.7	/	/	/	/
SS DTX-NPs	121.9 ± 3.7	0.169 ± 0.029	+ 19.1 ± 2.1	9.1 ± 0.7	/	90.3 ± 3.3	/
SS EZL-NPs	118.6 ± 4.1	0.178 ± 0.031	+ 20.2 ± 1.8	/	7.5 ± 1.1	/	88.3 ± 2.6

Figure 3. The cellular uptake efficiency of C6-loaded NPs. *p < .05.

Figure 4. The cytotoxicity of NPs was determined by MTT assay. Results are presented as means ± SD. *p < .05.

Figure 5. In vivo tissue distribution of DTX after 1 h (A) and 48 h (B) of administration; tissue distribution of EZL after 1 h (C) and 48 h (D) of administration. Results are presented as means ± SD. *p < .05.

Figure 6. In vivo tumor inhibition effect (A) and body weight changes (B). Results are presented as means ± SD. *p < .05.