Figure 1.
Schematic illustration of DTX-PCL-PEG-SMLP micelles targeted to PSMA.
Figure 2.
The gel permeation chromatography graphs of four copolymers (A) and SMLP,PCL4.8K-PEG2K-SMLP and PCL12K-PEG5K-SMLP (D), the representative 1H NMR spectra of SMLP (B), copolymers PCL12K-PEG5K-SMLP (C) containing SMLP (black arrows) and PCL12K-PEG5K-COOH (E) with the peaks of PCL12k-PEG5k segment (a-e) and Infrared spectra graph of PCL12k-PEG5k-SMLP (F) and PCL12K-PEG5K-COOH (G) copolymers.
Table 1.
Characterization data of block copolymers and DTX-PMs.
Figure 3.
Synthetic representation of the chemical reaction for preparation of PCL-PEG-SMLP copolymer.
Figure 4.
The representative DLS graphs of the DTX-PMs1 (A), and DTX-PMs2 (B), respectively.
TEM graphs of DTX-PMs1 (A1) and DTX-PMs2 (B2).
Figure 5.
The short-term stability of the DLC of four DTX-PMs stored at room temperature for 7 days.
(n = 3).
Figure 6.
In vitro release profile of DTX from the four types of PMs solution at 37°C in PBS (10 mM, pH 7.4) or PBS(10 mM,pH 5.5), in comparison with Taxotere. (n = 3).
Figure 7.
Different concentrations of PMs1 and PMs2 in LNCaP cells (A) and in PC3 cells (B) after incubation for 72 h.
(n = 5).
Figure 8.
In vitro cytotoxicity determination of different concentrations of DSD, DTX-PMs1 and DTX-PMs2 in LNCaP cells and PC3 cells after incubation for 48 h, 72 h, respectively, using MTT assay.
(*) significantly different from DSD; (#) significantly different from PMs1; (n = 5). Note: *P<0.01, #P<0.01.
Table 2.
IC50 analysis of DSD, DTX-PMs1 and DTX-PMs2 on LNCaP and PC3 cells after 48 h, 72 h incubation, respectively (n = 5).
Figure 9.
HCSS images of LNCaP (A) and PC3 cells (B) following a 4 h incubation at 37°C with coumarin 6-loaded PMs1 and PMs2, respectively.
The cell nuclei were stained with Hoechst 33342 with the blue channel, the coumarin 6-loaded PMs are the green channel. The cellular uptake was visualized by overlaying images displayed by the nuclei channel and the PMs channel. The fluorescence intensity/cell graph of 100 µg/ml coumarin 6-loaded PMs1 and PMs2 with a concentration of 200 µg/ml after 4 h incubation with LNCaP cells and PC3 cells (C).
Figure 10.
Competitive inhibition analysis of free SMLP (A) and fluorescence intensity/cell on LNCaP cells after 4 h incubation (B).