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

Xiaolong Tang12, Shuyu Cai1, Rongbo Zhang1, Peng Liu1, Hongbo Chen3, Yi Zheng3* and Leilei Sun34*

Author Affiliations

1 Stem Cell Engineering and Technology Research Center, School of Medicine, Anhui University of Science and Technology, Huainan 232001, China

2 Nankai Hospital, Nankai Clinical School, Tianjin Medical University, Tianjin 300100, China

3 The Shenzhen Key Laboratory of Gene and Antibody Therapy, Division of Life Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, China

4 Northeastern University, Boston, MA 02115, USA

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Nanoscale Research Letters 2013, 8:420  doi:10.1186/1556-276X-8-420

Published: 17 October 2013


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.

Paclitaxel; Breast cancer; Nanoparticles; Drug delivery; Star-shaped copolymer