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. 2013 Oct 17;8(1):420.
doi: 10.1186/1556-276X-8-420.

Paclitaxel-loaded nanoparticles of star-shaped cholic acid-core PLA-TPGS copolymer for breast cancer treatment

Xiaolong Tang, Shuyu Cai, Rongbo Zhang, Peng Liu, Hongbo Chen, Yi Zheng  1 , Leilei Sun
Affiliations

Paclitaxel-loaded nanoparticles of star-shaped cholic acid-core PLA-TPGS copolymer for breast cancer treatment

Xiaolong Tang et al. Nanoscale Res Lett. .

Abstract

A system of novel nanoparticles of star-shaped cholic acid-core polylactide-d-α-tocopheryl polyethylene glycol 1000 succinate (CA-PLA-TPGS) block copolymer was developed for paclitaxel delivery for breast cancer treatment, which demonstrated superior in vitro and in vivo performance in comparison with paclitaxel-loaded poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles and linear PLA-TPGS nanoparticles. The paclitaxel- or couramin 6-loaded nanoparticles were fabricated by a modified nanoprecipitation method and then characterized in terms of size, surface charge, surface morphology, drug encapsulation efficiency, and in vitro drug release. The CA-PLA-TPGS nanoparticles were found to be spherical in shape with an average size of around 120 nm. The nanoparticles were found to be stable, showing no change in the particle size and surface charge during 90-day storage of the aqueous solution. The release profiles of the paclitaxel-loaded nanoparticles exhibited typically biphasic release patterns. The results also showed that the CA-PLA-TPGS nanoparticles have higher antitumor efficacy than the PLA-TPGS nanoparticles and PLGA nanoparticles in vitro and in vivo. In conclusion, such nanoparticles of star-shaped cholic acid-core PLA-TPGS block copolymer could be considered as a potentially promising and effective strategy for breast cancer treatment.

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Figures

Figure 1
Figure 1
1H NMR and FTIR spectra. (A) Typical 1H NMR spectrum of the CA-PLA-TPGS copolymer. (B) FTIR spectra of the CA-PLA-TPGS copolymer (black) and TPGS (blue).
Figure 2
Figure 2
Size distribution and zeta potential distribution. (A) Size distribution of the star-shaped CA-PLA-TPGS nanoparticles detected by DLS. (B) Zeta potential distribution of the star-shaped CA-PLA-TPGS nanoparticles.
Figure 3
Figure 3
FESEM image of the star-shaped CA-PLA-TPGS nanoparticles.
Figure 4
Figure 4
In vitro stability of the PTX-loaded nanoparticles. (A) The size distribution of PTX-loaded PLGA, PLA-TPGS, and CA-PLA-TPGS NPs for 90-day storage at 4°C. (B) The zeta potential of PTX-loaded PLGA, PLA-TPGS, and CA-PLA-TPGS NPs for 90-day storage at 4°C.
Figure 5
Figure 5
In vitro release profiles of the PTX-loaded linear PLGA nanoparticles, linear PLA-TPGS nanoparticles, and star-shaped CA-PLA-TPGS nanoparticles.
Figure 6
Figure 6
CLSM images of MCF-7 cells after 4 h of incubation with the coumarin 6-loaded CA-PLA-TPGS nanoparticles. The coumarin 6-loaded nanoparticles were green, and the cells were stained by DAPI (blue). The cellular uptake was visualized by overlaying images obtained using the EGFP filter and DAPI filter: (A) EGFP channel, green; (B) DAPI channel, blue; and (C) combined EGFP channel and DAPI channel.
Figure 7
Figure 7
Cellular uptake efficiency of the coumarin 6-loaded nanoparticles.
Figure 8
Figure 8
Cell viability of PTX-loaded nanoparticles compared with that of Taxol® at equivalent PTX dose and nanoparticle concentration. (A) 24 h. (B) 48 h. (C) 72 h.
Figure 9
Figure 9
Tumor growth curve of the mice after injection of the PTX-loaded CA-PLA-TPGS nanoparticles, Taxol®, and saline ( n = 5 ).
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